DrugBank Version 5.1. The DrugBank database is a unique bioinformatics and cheminformatics resource that combines detailed drug (i.e. chemical, pharmacological and pharmaceutical) data with comprehensive drug target (i.e. sequence, structure, and pathway) information. The database contains 8250 drug entries including 2016 FDA-approved small molecule drugs, 229 FDA-approved biotech (protein/peptide) drugs, 94 nutraceuticals and over 6000 experimental drugs. This DataWarrior file is a subset of drugbank 5.0.3 downloaded from https://www.drugbank.ca.
DrugBank is offered to the public as a freely available resource. Use and re-distribution of the data, in whole or in part, for commercial purposes (including internal use) requires a license. We ask that users who download significant portions of the database cite the DrugBank paper in any resulting publications. Citing DrugBank: Wishart DS, Knox C, Guo AC, Shrivastava S, Hassanali M, Stothard P, Chang Z, Woolsey J. DrugBank: a comprehensive resource for in silico drug discovery and exploration. Nucleic Acids Res. 2006 Jan 1;34(Database issue):D668-72. 16381955
idcoordinates2D FragFp Drugbank-ID CAS Number Name Synonyms Drug Type UNII Average Mass Synthesis Reference MSDS State Description Affected Organism Dosage Form Dosage Route Dosage Indication Mechanism Of Action Target Action Target Name Target-ID Target Organism Target Reference Target Pubmed-ID Target Polypeptide ID Target Polypeptide Name Target Polypeptide Locus Target Polypeptide Organism Target Polypeptide GO-Classifier Description Target Polypeptide General Function Target Polypeptide Specific Function Protein Binding Toxicity Half-Life Absorption Metabolism Clearance Volume Of Distribution Route Of Elimination Pharmacodynamics Drug Interactions Description Drug Interactions Drugbank-IDs Drug Interactions Drug Names Food Interactions Exp. Property Exp. Property Value Exp. Property Source ATC Code ATC-Levels ATC-Level Codes Category Category Mesh-ID External Identifiers External Identifier Resource External Link Resource External Link URL FDA Label Citations Pubmed-IDs Group International Brand Company International Brand Name Classification Kingdom Classification Superclass Classification Class Classification Subclass Classification Description Classification Direct Parent Classification Alternative Parent Classification Substituent Patents Number Patents Country Patents Approved Patents Expires Patents Pediatric Extension Pathways Category Pathways Drugs Drugbank-ID Pathways Drugs Name Pathways Enzymes Uniprot-ID Pathways Name Pathways SMPDB-ID PDB-Entry Manufacturer Manufacturer Generic Mixture Ingredients Mixture Name Packagers Name Packagers Link Products Name Products Generic Products Labeller Products Over The Counter Products Route Products Dosage-Form Products Source Products Strength Products NDC-Product Code Products FDA Application No Products Approved Products DPD-ID Products Country Products Started Marketing Products Ended Marketing Prices Unit Prices Cost Prices Currency Prices Description Structure SMILES INCHI_IDENTIFIER INCHI_KEY FORMULA JCHEM_PKA JCHEM_PKA_STRONGEST_ACIDIC JCHEM_PKA_STRONGEST_BASIC JCHEM_POLAR_SURFACE_AREA JCHEM_REFRACTIVITY DB00001 138068-37-8 Lepirudin Hirudin variant-1Lepirudin recombinant biotech Y43GF64R34 //s3-us-west-2.amazonaws.com/drugbank/msds/DB00001.pdf?1368416245 liquid Lepirudin is identical to natural hirudin except for substitution of leucine for isoleucine at the N-terminal end of the molecule and the absence of a sulfate group on the tyrosine at position 63. It is produced via yeast cells. Bayer ceased the production of lepirudin (Refludan) effective May 31, 2012. Humans and other mammals Injection, solution, concentrateInjection, solution, concentratePowder, for solution IntravenousIntravenousIntravenous 20 mg50 mg50 mg For the treatment of heparin-induced thrombocytopenia Lepirudin forms a stable non-covalent complex with alpha-thrombin, thereby abolishing its ability to cleave fibrinogen and initiate the clotting cascade. The inhibition of thrombin prevents the blood clotting cascade. inhibitor Prothrombin BE0000048 Human Turpie AG: Anticoagulants in acute coronary syndromes. Am J Cardiol. 1999 Sep 2;84(5A):2M-6M.Warkentin TE: Venous thromboembolism in heparin-induced thrombocytopenia. Curr Opin Pulm Med. 2000 Jul;6(4):343-51.Eriksson BI: New therapeutic options in deep vein thrombosis prophylaxis. Semin Hematol. 2000 Jul;37(3 Suppl 5):7-9.Fabrizio MC: Use of ecarin clotting time (ECT) with lepirudin therapy in heparin-induced thrombocytopenia and cardiopulmonary bypass. J Extra Corpor Technol. 2001 May;33(2):117-25.Szaba FM, Smiley ST: Roles for thrombin and fibrin(ogen) in cytokine/chemokine production and macrophage adhesion in vivo. Blood. 2002 Feb 1;99(3):1053-9.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. 105055361091264411055889114674391180701211752352 P00734 Prothrombin 11p11-q12 Human blood microparticleextracellular matrixGolgi lumencytosolextracellular exosomeextracellular regionendoplasmic reticulum lumenplasma membraneextracellular spacethrombospondin receptor activitycalcium ion bindingserine-type endopeptidase activitygrowth factor activityreceptor bindingnegative regulation of platelet activationregulation of cell shaperegulation of gene expressionblood coagulationnegative regulation of proteolysisplatelet activationresponse to inactivitypositive regulation of blood coagulationresponse to woundingacute-phase responsepositive regulation of cell growthblood coagulation, intrinsic pathwayproteolysispositive regulation of cell proliferationpositive regulation of protein phosphorylationcell surface receptor signaling pathwaypositive regulation of collagen biosynthetic processcytosolic calcium ion homeostasispositive regulation of phosphatidylinositol 3-kinase signalingcellular response to mechanical stimulusfibrinolysispositive regulation of phospholipase C-activating G-protein coupled receptor signaling pathwayleukocyte migrationmulticellular organismal developmentpositive regulation of reactive oxygen species metabolic processcellular protein metabolic processnegative regulation of astrocyte differentiationpeptidyl-glutamic acid carboxylationpositive regulation of release of sequestered calcium ion into cytosolpost-translational protein modificationnegative regulation of fibrinolysisregulation of blood coagulation Thrombospondin receptor activity Thrombin, which cleaves bonds after Arg and Lys, converts fibrinogen to fibrin and activates factors V, VII, VIII, XIII, and, in complex with thrombomodulin, protein C. Functions in blood homeostasis, inflammation and wound healing. In case of overdose (eg, suggested by excessively high aPTT values) the risk of bleeding is increased. Approximately 1.3 hours Bioavailability is 100% following injection. Lepirudin is thought to be metabolized by release of amino acids via catabolic hydrolysis of the parent drug. However, con-clusive data are not available. About 48% of the administration dose is excreted in the urine which consists of unchanged drug (35%) and other fragments of the parent drug. * 164 ml/min [Healthy 18-60 yrs]* 139 ml/min [Healthy 65-80 yrs]* 61 ml/min [renal impaired]* 114 ml/min [HIT (Heparin-induced thrombocytopenia)] * 12.2 L [Healthy young subjects (n = 18, age 18-60 years)]* 18.7 L [Healthy elderly subjects (n = 10, age 65-80 years)]* 18 L [Renally impaired patients (n = 16, creatinine clearance below 80 mL/min)]* 32.1 L [HIT patients (n = 73)] Lepirudin is thought to be metabolized by release of amino acids via catabolic hydrolysis of the parent drug. About 48% of the administration dose is excreted in the urine which consists of unchanged drug (35%) and other fragments of the parent drug. Lepirudin is used to break up clots and to reduce thrombocytopenia. It binds to thrombin and prevents thrombus or clot formation. It is a highly potent, selective, and essentially irreversible inhibitor of thrombin and clot-bond thrombin. Lepirudin requires no cofactor for its anticoagulant action. Lepirudin is a recombinant form of hirudin, an endogenous anticoagulant found in medicinal leeches. The serum concentration of Ethinyl Estradiol can be decreased when it is combined with Lepirudin.The serum concentration of Mestranol can be decreased when it is combined with Lepirudin.The serum concentration of Estradiol can be decreased when it is combined with Lepirudin.The serum concentration of Estrone sulfate can be decreased when it is combined with Lepirudin.The serum concentration of Synthetic Conjugated Estrogens, A can be decreased when it is combined with Lepirudin.The serum concentration of Estrogens, esterified can be decreased when it is combined with Lepirudin.The serum concentration of Chlorotrianisene can be decreased when it is combined with Lepirudin.The serum concentration of Conjugated estrogens can be decreased when it is combined with Lepirudin.The serum concentration of Estramustine can be decreased when it is combined with Lepirudin.The serum concentration of Dienestrol can be decreased when it is combined with Lepirudin.The serum concentration of Diethylstilbestrol can be decreased when it is combined with Lepirudin.The serum concentration of Hexestrol can be decreased when it is combined with Lepirudin.The serum concentration of Methallenestril can be decreased when it is combined with Lepirudin.The serum concentration of Cyclosporine can be increased when it is combined with Lepirudin.The serum concentration of Lepirudin can be decreased when it is combined with Garlic.The metabolism of Tacrolimus can be decreased when combined with Lepirudin.The risk or severity of adverse effects can be increased when Lepirudin is combined with Pethidine.The serum concentration of Alprazolam can be increased when it is combined with Lepirudin.The serum concentration of Lepirudin can be decreased when it is combined with Boceprevir.The metabolism of Lepirudin can be increased when combined with Carbamazepine.The therapeutic efficacy of Clarithromycin can be decreased when used in combination with Lepirudin.The serum concentration of Delavirdine can be decreased when it is combined with Lepirudin.Estrone may decrease the anticoagulant activities of Lepirudin.Polyestradiol phosphate may decrease the anticoagulant activities of Lepirudin.Genistein may decrease the anticoagulant activities of Lepirudin.Quinestrol may decrease the anticoagulant activities of Lepirudin.Synthetic Conjugated Estrogens, B may decrease the anticoagulant activities of Lepirudin.Zeranol may decrease the anticoagulant activities of Lepirudin.Equol may decrease the anticoagulant activities of Lepirudin.Secoisolariciresinol may decrease the anticoagulant activities of Lepirudin.Daidzein may decrease the anticoagulant activities of Lepirudin.Epimestrol may decrease the anticoagulant activities of Lepirudin.Estriol may decrease the anticoagulant activities of Lepirudin.Promestriene may decrease the anticoagulant activities of Lepirudin.Moxestrol may decrease the anticoagulant activities of Lepirudin.Estradiol acetate may decrease the anticoagulant activities of Lepirudin.Estradiol cypionate may decrease the anticoagulant activities of Lepirudin.Estradiol valerate may decrease the anticoagulant activities of Lepirudin.The risk or severity of bleeding can be increased when Lepirudin is combined with Omacetaxine mepesuccinate.The serum concentration of Nefazodone can be increased when it is combined with Lepirudin.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Aprotinin.The therapeutic efficacy of Lepirudin can be increased when used in combination with Testosterone cypionate.The therapeutic efficacy of Lepirudin can be increased when used in combination with Testosterone enanthate.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Allylestrenol.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Etonogestrel.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Medroxyprogesterone acetate.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Progesterone.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Norethisterone.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Hydroxyprogesterone caproate.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Desogestrel.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Dydrogesterone.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Gestodene.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Altrenogest.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Gestrinone.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Medrogestone.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Nomegestrol.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Gestonorone.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Methylestrenolone.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Norgestrienone.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Promegestone.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Demegestone.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Megestrol acetate.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Levonorgestrel.The therapeutic efficacy of Lepirudin can be decreased when used in combination with Dienogest.The therapeutic efficacy of Lepirudin can be increased when used in combination with Testosterone undecanoate.The serum concentration of Riociguat can be increased when it is combined with Lepirudin.The serum concentration of Sildenafil can be increased when it is combined with Lepirudin.The risk or severity of adverse effects can be increased when Lepirudin is combined with Temsirolimus.The metabolism of Diltiazem can be decreased when combined with Lepirudin.The metabolism of Verapamil can be decreased when combined with Lepirudin.Pentosan Polysulfate may increase the anticoagulant activities of Lepirudin.The serum concentration of Amitriptyline can be increased when it is combined with Lepirudin.The serum concentration of Protriptyline can be increased when it is combined with Lepirudin.The serum concentration of Imipramine can be increased when it is combined with Lepirudin.The serum concentration of Nortriptyline can be increased when it is combined with Lepirudin.The serum concentration of Trimipramine can be increased when it is combined with Lepirudin.The serum concentration of Doxepin can be increased when it is combined with Lepirudin.The serum concentration of Desipramine can be increased when it is combined with Lepirudin.The serum concentration of Clomipramine can be increased when it is combined with Lepirudin.The serum concentration of Mirtazapine can be increased when it is combined with Lepirudin.The serum concentration of Cyclobenzaprine can be increased when it is combined with Lepirudin.The serum concentration of Amineptine can be increased when it is combined with Lepirudin.The serum concentration of Esmirtazapine can be increased when it is combined with Lepirudin.The serum concentration of Dosulepin can be increased when it is combined with Lepirudin.The serum concentration of Tianeptine can be increased when it is combined with Lepirudin.The serum concentration of Opipramol can be increased when it is combined with Lepirudin.The serum concentration of Dibenzepin can be increased when it is combined with Lepirudin.The serum concentration of Lofepramine can be increased when it is combined with Lepirudin.The serum concentration of Iprindole can be increased when it is combined with Lepirudin.The serum concentration of Amoxapine can be increased when it is combined with Lepirudin.The serum concentration of Abacavir can be decreased when it is combined with Lepirudin.The risk or severity of adverse effects can be increased when Lepirudin is combined with Cyclophosphamide.The serum concentration of Digoxin can be increased when it is combined with Lepirudin.The serum concentration of Enfuvirtide can be increased when it is combined with Lepirudin.The serum concentration of Etravirine can be decreased when it is combined with Lepirudin.Dasatinib may increase the anticoagulant activities of Lepirudin.The risk or severity of adverse effects can be increased when Lepirudin is combined with Deferasirox.The risk or severity of adverse effects can be increased when Lepirudin is combined with Deoxycholic Acid.The risk or severity of adverse effects can be increased when Lepirudin is combined with Ibritumomab tiuxetan.The risk or severity of adverse effects can be increased when Ibrutinib is combined with Lepirudin.The risk or severity of adverse effects can be increased when Lepirudin is combined with Nintedanib.The risk or severity of adverse effects can be increased when Lepirudin is combined with Obinutuzumab.The risk or severity of adverse effects can be increased when Lepirudin is combined with Collagenase clostridium histolyticum.Sugammadex may increase the anticoagulant activities of Lepirudin.The risk or severity of adverse effects can be increased when Limaprost is combined with Lepirudin.Tibolone may increase the anticoagulant activities of Lepirudin.Ketorolac may increase the anticoagulant activities of Lepirudin.Diclofenac may increase the anticoagulant activities of Lepirudin.Flurbiprofen may increase the anticoagulant activities of Lepirudin.Bromfenac may increase the anticoagulant activities of Lepirudin.Nepafenac may increase the anticoagulant activities of Lepirudin.Etanercept may increase the anticoagulant activities of Lepirudin.Masoprocol may increase the anticoagulant activities of Lepirudin.Adapalene may increase the anticoagulant activities of Lepirudin.Mesalazine may increase the anticoagulant activities of Lepirudin.Indomethacin may increase the anticoagulant activities of Lepirudin.Pimecrolimus may increase the anticoagulant activities of Lepirudin.Nabumetone may increase the anticoagulant activities of Lepirudin.Tenoxicam may increase the anticoagulant activities of Lepirudin.Celecoxib may increase the anticoagulant activities of Lepirudin.Tolmetin may increase the anticoagulant activities of Lepirudin.Rofecoxib may increase the anticoagulant activities of Lepirudin.Piroxicam may increase the anticoagulant activities of Lepirudin.Fenoprofen may increase the anticoagulant activities of Lepirudin.Valdecoxib may increase the anticoagulant activities of Lepirudin.Sulindac may increase the anticoagulant activities of Lepirudin.Chloroquine may increase the anticoagulant activities of Lepirudin.Mycophenolate mofetil may increase the anticoagulant activities of Lepirudin.Naftifine may increase the anticoagulant activities of Lepirudin.Zileuton may increase the anticoagulant activities of Lepirudin.Etodolac may increase the anticoagulant activities of Lepirudin.Olopatadine may increase the anticoagulant activities of Lepirudin.Mefenamic acid may increase the anticoagulant activities of Lepirudin.Naproxen may increase the anticoagulant activities of Lepirudin.Sulfasalazine may increase the anticoagulant activities of Lepirudin.Phenylbutazone may increase the anticoagulant activities of Lepirudin.Meloxicam may increase the anticoagulant activities of Lepirudin.Carprofen may increase the anticoagulant activities of Lepirudin.Diflunisal may increase the anticoagulant activities of Lepirudin.Suprofen may increase the anticoagulant activities of Lepirudin.Salicylic acid may increase the anticoagulant activities of Lepirudin.Meclofenamic acid may increase the anticoagulant activities of Lepirudin.Acetylsalicylic acid may increase the anticoagulant activities of Lepirudin.Azelastine may increase the anticoagulant activities of Lepirudin.Oxaprozin may increase the anticoagulant activities of Lepirudin.Ketoprofen may increase the anticoagulant activities of Lepirudin.Balsalazide may increase the anticoagulant activities of Lepirudin.Mycophenolic acid may increase the anticoagulant activities of Lepirudin.Ibuprofen may increase the anticoagulant activities of Lepirudin.Leflunomide may increase the anticoagulant activities of Lepirudin.Olsalazine may increase the anticoagulant activities of Lepirudin.Lumiracoxib may increase the anticoagulant activities of Lepirudin.Magnesium salicylate may increase the anticoagulant activities of Lepirudin.Salsalate may increase the anticoagulant activities of Lepirudin.Choline magnesium trisalicylate may increase the anticoagulant activities of Lepirudin.Antipyrine may increase the anticoagulant activities of Lepirudin.Tiaprofenic acid may increase the anticoagulant activities of Lepirudin.Etoricoxib may increase the anticoagulant activities of Lepirudin.Castanospermine may increase the anticoagulant activities of Lepirudin.Resveratrol may increase the anticoagulant activities of Lepirudin.Oxyphenbutazone may increase the anticoagulant activities of Lepirudin.Niflumic Acid may increase the anticoagulant activities of Lepirudin.Nimesulide may increase the anticoagulant activities of Lepirudin.Benoxaprofen may increase the anticoagulant activities of Lepirudin.Metamizole may increase the anticoagulant activities of Lepirudin.Zomepirac may increase the anticoagulant activities of Lepirudin.Pirfenidone may increase the anticoagulant activities of Lepirudin.SRT501 may increase the anticoagulant activities of Lepirudin.PTC299 may increase the anticoagulant activities of Lepirudin.Tarenflurbil may increase the anticoagulant activities of Lepirudin.Apremilast may increase the anticoagulant activities of Lepirudin.Andrographolide may increase the anticoagulant activities of Lepirudin.Icatibant may increase the anticoagulant activities of Lepirudin.Exisulind may increase the anticoagulant activities of Lepirudin.Lornoxicam may increase the anticoagulant activities of Lepirudin.Aceclofenac may increase the anticoagulant activities of Lepirudin.Zaltoprofen may increase the anticoagulant activities of Lepirudin.Seratrodast may increase the anticoagulant activities of Lepirudin.Azapropazone may increase the anticoagulant activities of Lepirudin.Felbinac may increase the anticoagulant activities of Lepirudin.Tranilast may increase the anticoagulant activities of Lepirudin.Ferulic acid may increase the anticoagulant activities of Lepirudin.Parecoxib may increase the anticoagulant activities of Lepirudin.Salicylamide may increase the anticoagulant activities of Lepirudin.Teriflunomide may increase the anticoagulant activities of Lepirudin.(4R)-limonene may increase the anticoagulant activities of Lepirudin.Kebuzone may increase the anticoagulant activities of Lepirudin.Isoxicam may increase the anticoagulant activities of Lepirudin.Indoprofen may increase the anticoagulant activities of Lepirudin.Ibuproxam may increase the anticoagulant activities of Lepirudin.Floctafenine may increase the anticoagulant activities of Lepirudin.Fenbufen may increase the anticoagulant activities of Lepirudin.Etofenamate may increase the anticoagulant activities of Lepirudin.Epirizole may increase the anticoagulant activities of Lepirudin.Loxoprofen may increase the anticoagulant activities of Lepirudin.Droxicam may increase the anticoagulant activities of Lepirudin.Tolfenamic Acid may increase the anticoagulant activities of Lepirudin.Clonixin may increase the anticoagulant activities of Lepirudin.Propacetamol may increase the anticoagulant activities of Lepirudin.Evening primrose oil may increase the anticoagulant activities of Lepirudin.Orgotein may increase the anticoagulant activities of Lepirudin.Tepoxalin may increase the anticoagulant activities of Lepirudin.Flunixin may increase the anticoagulant activities of Lepirudin.Curcumin may increase the anticoagulant activities of Lepirudin.E-6201 may increase the anticoagulant activities of Lepirudin.Anisodamine may increase the anticoagulant activities of Lepirudin.Duvelisib may increase the anticoagulant activities of Lepirudin.Triptolide may increase the anticoagulant activities of Lepirudin.Semapimod may increase the anticoagulant activities of Lepirudin.Bucillamine may increase the anticoagulant activities of Lepirudin.Lisofylline may increase the anticoagulant activities of Lepirudin.Nitroaspirin may increase the anticoagulant activities of Lepirudin.Nafamostat may increase the anticoagulant activities of Lepirudin.Mizoribine may increase the anticoagulant activities of Lepirudin.Apocynin may increase the anticoagulant activities of Lepirudin.Higenamine may increase the anticoagulant activities of Lepirudin.Tinoridine may increase the anticoagulant activities of Lepirudin.Parthenolide may increase the anticoagulant activities of Lepirudin.Serrapeptase may increase the anticoagulant activities of Lepirudin.Alclofenac may increase the anticoagulant activities of Lepirudin.Fentiazac may increase the anticoagulant activities of Lepirudin.Tribenoside may increase the anticoagulant activities of Lepirudin.Suxibuzone may increase the anticoagulant activities of Lepirudin.Bumadizone may increase the anticoagulant activities of Lepirudin.Alminoprofen may increase the anticoagulant activities of Lepirudin.Flunoxaprofen may increase the anticoagulant activities of Lepirudin.Bufexamac may increase the anticoagulant activities of Lepirudin.Feprazone may increase the anticoagulant activities of Lepirudin.Difenpiramide may increase the anticoagulant activities of Lepirudin.Nifenazone may increase the anticoagulant activities of Lepirudin.Lonazolac may increase the anticoagulant activities of Lepirudin.Tenidap may increase the anticoagulant activities of Lepirudin.Bendazac may increase the anticoagulant activities of Lepirudin.Pranoprofen may increase the anticoagulant activities of Lepirudin.Propyphenazone may increase the anticoagulant activities of Lepirudin.Proglumetacin may increase the anticoagulant activities of Lepirudin.Guacetisal may increase the anticoagulant activities of Lepirudin.Bevonium may increase the anticoagulant activities of Lepirudin.Ethenzamide may increase the anticoagulant activities of Lepirudin.Carbaspirin calcium may increase the anticoagulant activities of Lepirudin.Mofebutazone may increase the anticoagulant activities of Lepirudin.Proquazone may increase the anticoagulant activities of Lepirudin.Benorilate may increase the anticoagulant activities of Lepirudin.Pirprofen may increase the anticoagulant activities of Lepirudin.Imidazole salicylate may increase the anticoagulant activities of Lepirudin.Benzydamine may increase the anticoagulant activities of Lepirudin.Tipranavir may increase the anticoagulant activities of Lepirudin.Omega-3 fatty acids may increase the anticoagulant activities of Lepirudin.Vitamin E may increase the anticoagulant activities of Lepirudin.The risk or severity of adverse effects can be increased when Lepirudin is combined with Tositumomab.Lepirudin may increase the anticoagulant activities of Dabigatran etexilate.Lepirudin may increase the anticoagulant activities of Bivalirudin.Lepirudin may increase the anticoagulant activities of Abciximab.Lepirudin may increase the anticoagulant activities of Becaplermin.Lepirudin may increase the anticoagulant activities of Dicoumarol.Lepirudin may increase the anticoagulant activities of Argatroban.Lepirudin may increase the anticoagulant activities of Ardeparin.Lepirudin may increase the anticoagulant activities of Phenindione.Lepirudin may increase the anticoagulant activities of Fondaparinux sodium.Lepirudin may increase the anticoagulant activities of Warfarin.Lepirudin may increase the anticoagulant activities of Phenprocoumon.Lepirudin may increase the anticoagulant activities of Edetic Acid.Lepirudin may increase the anticoagulant activities of Heparin.Lepirudin may increase the anticoagulant activities of Enoxaparin.Lepirudin may increase the anticoagulant activities of Acenocoumarol.Lepirudin may increase the anticoagulant activities of Citric Acid.Lepirudin may increase the anticoagulant activities of Ximelagatran.Lepirudin may increase the anticoagulant activities of Ancrod.Lepirudin may increase the anticoagulant activities of Pentaerythritol Tetranitrate.Lepirudin may increase the anticoagulant activities of Sulodexide.Lepirudin may increase the anticoagulant activities of Idraparinux.Lepirudin may increase the anticoagulant activities of Otamixaban.Lepirudin may increase the anticoagulant activities of Danaparoid.Lepirudin may increase the anticoagulant activities of Dalteparin.Lepirudin may increase the anticoagulant activities of Ethyl biscoumacetate.Lepirudin may increase the anticoagulant activities of Nadroparin.Lepirudin may increase the anticoagulant activities of Dextran.Lepirudin may increase the anticoagulant activities of Reviparin.Lepirudin may increase the anticoagulant activities of Certoparin.Lepirudin may increase the anticoagulant activities of Dextran 70.Lepirudin may increase the anticoagulant activities of Desirudin.Lepirudin may increase the anticoagulant activities of Dextran 40.Lepirudin may increase the anticoagulant activities of Dextran 75.Lepirudin may increase the anticoagulant activities of Protocatechualdehyde.Lepirudin may increase the anticoagulant activities of Protein C.Lepirudin may increase the anticoagulant activities of Antithrombin III human.Lepirudin may increase the anticoagulant activities of Fondaparinux.Lepirudin may increase the anticoagulant activities of Letaxaban.Lepirudin may increase the anticoagulant activities of Darexaban.Lepirudin may increase the anticoagulant activities of Gabexate.Lepirudin may increase the anticoagulant activities of Troxerutin.Lepirudin may increase the anticoagulant activities of Fluindione.Lepirudin may increase the anticoagulant activities of Protein S human.Lepirudin may increase the anticoagulant activities of Melagatran.Aminosalicylic Acid may increase the anticoagulant activities of Lepirudin.Dersalazine may increase the anticoagulant activities of Lepirudin.Aloxiprin may increase the anticoagulant activities of Lepirudin.Hemoglobin crosfumaril may increase the anticoagulant activities of Lepirudin.Methyl salicylate may increase the anticoagulant activities of Lepirudin.Trolamine salicylate may increase the anticoagulant activities of Lepirudin.Alteplase may increase the anticoagulant activities of Lepirudin.Reteplase may increase the anticoagulant activities of Lepirudin.Anistreplase may increase the anticoagulant activities of Lepirudin.Tenecteplase may increase the anticoagulant activities of Lepirudin.Drotrecogin alfa may increase the anticoagulant activities of Lepirudin.Ticlopidine may increase the anticoagulant activities of Lepirudin.Tirofiban may increase the anticoagulant activities of Lepirudin.Cilostazol may increase the anticoagulant activities of Lepirudin.Defibrotide may increase the anticoagulant activities of Lepirudin.Tinzaparin may increase the anticoagulant activities of Lepirudin.Brinase may increase the anticoagulant activities of Lepirudin.Saruplase may increase the anticoagulant activities of Lepirudin.Streptokinase may increase the anticoagulant activities of Lepirudin.Anagrelide may increase the anticoagulant activities of Lepirudin.Rosiglitazone may increase the anticoagulant activities of Lepirudin.Desmoteplase may increase the anticoagulant activities of Lepirudin.Fibrinolysin may increase the anticoagulant activities of Lepirudin.Caplacizumab may increase the anticoagulant activities of Lepirudin.eplivanserine may increase the anticoagulant activities of Lepirudin.Astaxanthin may increase the anticoagulant activities of Lepirudin.Batroxobin may increase the anticoagulant activities of Lepirudin.Ozagrel may increase the anticoagulant activities of Lepirudin.Sarpogrelate may increase the anticoagulant activities of Lepirudin.Eplivanserin may increase the anticoagulant activities of Lepirudin.Eptifibatide may increase the anticoagulant activities of Lepirudin.Treprostinil may increase the anticoagulant activities of Lepirudin.Clopidogrel may increase the anticoagulant activities of Lepirudin.Dipyridamole may increase the anticoagulant activities of Lepirudin.Iloprost may increase the anticoagulant activities of Lepirudin.Epoprostenol may increase the anticoagulant activities of Lepirudin.Beraprost may increase the anticoagulant activities of Lepirudin.Prasugrel may increase the anticoagulant activities of Lepirudin.Cangrelor may increase the anticoagulant activities of Lepirudin.Triflusal may increase the anticoagulant activities of Lepirudin.Ticagrelor may increase the anticoagulant activities of Lepirudin.Ditazole may increase the anticoagulant activities of Lepirudin.Bemiparin may increase the anticoagulant activities of Lepirudin.Parnaparin may increase the anticoagulant activities of Lepirudin.Selexipag may increase the anticoagulant activities of Lepirudin.Indobufen may increase the anticoagulant activities of Lepirudin.Clorindione may increase the anticoagulant activities of Lepirudin.Picotamide may increase the anticoagulant activities of Lepirudin.Diphenadione may increase the anticoagulant activities of Lepirudin.Cloricromen may increase the anticoagulant activities of Lepirudin.Tioclomarol may increase the anticoagulant activities of Lepirudin.Milrinone may increase the anticoagulant activities of Lepirudin.Epinastine may increase the anticoagulant activities of Lepirudin.Alprostadil may increase the anticoagulant activities of Lepirudin.Pentoxifylline may increase the anticoagulant activities of Lepirudin.Ridogrel may increase the anticoagulant activities of Lepirudin.Sevoflurane may increase the anticoagulant activities of Lepirudin.Tesmilifene may increase the anticoagulant activities of Lepirudin.Ibudilast may increase the anticoagulant activities of Lepirudin.Icosapent ethyl may increase the anticoagulant activities of Lepirudin.Ifenprodil may increase the anticoagulant activities of Lepirudin.Trapidil may increase the anticoagulant activities of Lepirudin.Naftopidil may increase the anticoagulant activities of Lepirudin.Ifetroban may increase the anticoagulant activities of Lepirudin.Ketanserin may increase the anticoagulant activities of Lepirudin.Butylphthalide may increase the anticoagulant activities of Lepirudin.Hydroxytyrosol may increase the anticoagulant activities of Lepirudin.Ramatroban may increase the anticoagulant activities of Lepirudin.Linsidomine may increase the anticoagulant activities of Lepirudin.Buflomedil may increase the anticoagulant activities of Lepirudin.Relcovaptan may increase the anticoagulant activities of Lepirudin.The serum concentration of Ambroxol acefyllinate can be decreased when it is combined with Lepirudin.The serum concentration of Theophylline can be decreased when it is combined with Lepirudin.The serum concentration of Dyphylline can be decreased when it is combined with Lepirudin.The serum concentration of Aminophylline can be decreased when it is combined with Lepirudin.The serum concentration of Valproic Acid can be decreased when it is combined with Lepirudin.The serum concentration of Zidovudine can be decreased when it is combined with Lepirudin.The risk or severity of adverse effects can be increased when Lepirudin is combined with Azficel-T.The metabolism of Lepirudin can be increased when combined with St. John's Wort.The serum concentration of Alfuzosin can be increased when it is combined with Lepirudin.The risk or severity of bleeding can be increased when Lepirudin is combined with Acemetacin.Apixaban may increase the anticoagulant activities of Lepirudin.Edoxaban may increase the anticoagulant activities of Lepirudin.Lepirudin may increase the anticoagulant activities of Rivaroxaban.The serum concentration of Lovastatin can be increased when it is combined with Lepirudin.Urokinase may increase the anticoagulant activities of Lepirudin.The risk or severity of adverse effects can be increased when Vorapaxar is combined with Lepirudin.The serum concentration of Midazolam can be increased when it is combined with Lepirudin.The serum concentration of Simvastatin can be increased when it is combined with Lepirudin.The serum concentration of Cabergoline can be increased when it is combined with Lepirudin.The serum concentration of Bromocriptine can be increased when it is combined with Lepirudin.The serum concentration of Dihydroergotamine can be increased when it is combined with Lepirudin.The serum concentration of Ergotamine can be increased when it is combined with Lepirudin.The serum concentration of Ergoloid mesylate can be increased when it is combined with Lepirudin.The serum concentration of Ergonovine can be increased when it is combined with Lepirudin.The serum concentration of Methylergometrine can be increased when it is combined with Lepirudin.The serum concentration of Triazolam can be increased when it is combined with Lepirudin.Hemin may increase the anticoagulant activities of Lepirudin. 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Ethinyl EstradiolMestranolEstradiolEstrone sulfateSynthetic Conjugated Estrogens, AEstrogens, esterifiedChlorotrianiseneConjugated estrogensEstramustineDienestrolDiethylstilbestrolHexestrolMethallenestrilCyclosporineGarlicTacrolimusPethidineAlprazolamBoceprevirCarbamazepineClarithromycinDelavirdineEstronePolyestradiol phosphateGenisteinQuinestrolSynthetic Conjugated Estrogens, BZeranolEquolSecoisolariciresinolDaidzeinEpimestrolEstriolPromestrieneMoxestrolEstradiol acetateEstradiol cypionateEstradiol valerateOmacetaxine mepesuccinateNefazodoneAprotininTestosterone cypionateTestosterone enanthateAllylestrenolEtonogestrelMedroxyprogesterone acetateProgesteroneNorethisteroneHydroxyprogesterone caproateDesogestrelDydrogesteroneGestodeneAltrenogestGestrinoneMedrogestoneNomegestrolGestonoroneMethylestrenoloneNorgestrienonePromegestoneDemegestoneMegestrol acetateLevonorgestrelDienogestTestosterone undecanoateRiociguatSildenafilTemsirolimusDiltiazemVerapamilPentosan PolysulfateAmitriptylineProtriptylineImipramineNortriptylineTrimipramineDoxepinDesipramineClomipramineMirtazapineCyclobenzaprineAmineptineEsmirtazapineDosulepinTianeptineOpipramolDibenzepinLofepramineIprindoleAmoxapineAbacavirCyclophosphamideDigoxinEnfuvirtideEtravirineDasatinibDeferasiroxDeoxycholic AcidIbritumomab tiuxetanIbrutinibNintedanibObinutuzumabCollagenase clostridium histolyticumSugammadexLimaprostTiboloneKetorolacDiclofenacFlurbiprofenBromfenacNepafenacEtanerceptMasoprocolAdapaleneMesalazineIndomethacinPimecrolimusNabumetoneTenoxicamCelecoxibTolmetinRofecoxibPiroxicamFenoprofenValdecoxibSulindacChloroquineMycophenolate mofetilNaftifineZileutonEtodolacOlopatadineMefenamic acidNaproxenSulfasalazinePhenylbutazoneMeloxicamCarprofenDiflunisalSuprofenSalicylic acidMeclofenamic acidAcetylsalicylic acidAzelastineOxaprozinKetoprofenBalsalazideMycophenolic acidIbuprofenLeflunomideOlsalazineLumiracoxibMagnesium salicylateSalsalateCholine magnesium trisalicylateAntipyrineTiaprofenic acidEtoricoxibCastanospermineResveratrolOxyphenbutazoneNiflumic AcidNimesulideBenoxaprofenMetamizoleZomepiracPirfenidoneSRT501PTC299TarenflurbilApremilastAndrographolideIcatibantExisulindLornoxicamAceclofenacZaltoprofenSeratrodastAzapropazoneFelbinacTranilastFerulic acidParecoxibSalicylamideTeriflunomide(4R)-limoneneKebuzoneIsoxicamIndoprofenIbuproxamFloctafenineFenbufenEtofenamateEpirizoleLoxoprofenDroxicamTolfenamic AcidClonixinPropacetamolEvening primrose oilOrgoteinTepoxalinFlunixinCurcuminE-6201AnisodamineDuvelisibTriptolideSemapimodBucillamineLisofyllineNitroaspirinNafamostatMizoribineApocyninHigenamineTinoridineParthenolideSerrapeptaseAlclofenacFentiazacTribenosideSuxibuzoneBumadizoneAlminoprofenFlunoxaprofenBufexamacFeprazoneDifenpiramideNifenazoneLonazolacTenidapBendazacPranoprofenPropyphenazoneProglumetacinGuacetisalBevoniumEthenzamideCarbaspirin calciumMofebutazoneProquazoneBenorilatePirprofenImidazole salicylateBenzydamineTipranavirOmega-3 fatty acidsVitamin ETositumomabDabigatran etexilateBivalirudinAbciximabBecaplerminDicoumarolArgatrobanArdeparinPhenindioneFondaparinux sodiumWarfarinPhenprocoumonEdetic AcidHeparinEnoxaparinAcenocoumarolCitric AcidXimelagatranAncrodPentaerythritol TetranitrateSulodexideIdraparinuxOtamixabanDanaparoidDalteparinEthyl biscoumacetateNadroparinDextranReviparinCertoparinDextran 70DesirudinDextran 40Dextran 75ProtocatechualdehydeProtein CAntithrombin III humanFondaparinuxLetaxabanDarexabanGabexateTroxerutinFluindioneProtein S humanMelagatranAminosalicylic AcidDersalazineAloxiprinHemoglobin crosfumarilMethyl salicylateTrolamine salicylateAlteplaseReteplaseAnistreplaseTenecteplaseDrotrecogin alfaTiclopidineTirofibanCilostazolDefibrotideTinzaparinBrinaseSaruplaseStreptokinaseAnagrelideRosiglitazoneDesmoteplaseFibrinolysinCaplacizumabeplivanserineAstaxanthinBatroxobinOzagrelSarpogrelateEplivanserinEptifibatideTreprostinilClopidogrelDipyridamoleIloprostEpoprostenolBeraprostPrasugrelCangrelorTriflusalTicagrelorDitazoleBemiparinParnaparinSelexipagIndobufenClorindionePicotamideDiphenadioneCloricromenTioclomarolMilrinoneEpinastineAlprostadilPentoxifyllineRidogrelSevofluraneTesmilifeneIbudilastIcosapent ethylIfenprodilTrapidilNaftopidilIfetrobanKetanserinButylphthalideHydroxytyrosolRamatrobanLinsidomineBuflomedilRelcovaptanAmbroxol acefyllinateTheophyllineDyphyllineAminophyllineValproic AcidZidovudineAzficel-TSt. John's WortAlfuzosinAcemetacinApixabanEdoxabanRivaroxabanLovastatinUrokinaseVorapaxarMidazolamSimvastatinCabergolineBromocriptineDihydroergotamineErgotamineErgoloid mesylateErgonovineMethylergometrineTriazolamHemin Melting PointHydrophobicityIsoelectric PointMolecular WeightMolecular Formula 65 °C-0.7774.046963.425C287H440N80O110S6 Otto, A. & Seckler, R. Eur. J. Biochem. 202:67-73 (1991) B01AE02 Direct thrombin inhibitorsANTITHROMBOTIC AGENTSANTITHROMBOTIC AGENTSBLOOD AND BLOOD FORMING ORGANS B01AEB01AB01B Amino Acids, Peptides, and ProteinsAnti-coagulantAnticoagulantsAntithrombin ProteinsAntithrombinsBlood and Blood Forming OrgansCardiovascular AgentsChemical Actions and UsesEnzyme InhibitorsFibrin Modulating AgentsFibrinolytic AgentsHematologic AgentsMolecular Mechanisms of Pharmacological ActionPeptidesPharmacologic ActionsProtease InhibitorsProteinsSerine Proteinase InhibitorsSerpinsTherapeutic Uses D000602D000925D058833D000991D002317D020164D004791D050299D005343D006401D045504D010455D020228D011480D011506D015842D015843D045506 1191646507011D06880PA450195P01050DAP000541LepirudinCHEMBL1201666 Drugs Product Database (DPD)PubChem SubstanceKEGG DrugPharmGKBUniProtKBTherapeutic Targets DatabaseWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic/lepirudin.htmhttp://www.drugs.com/cdi/lepirudin.html //s3-us-west-2.amazonaws.com/drugbank/fda_labels/DB00001.pdf?1265924858 Smythe MA, Stephens JL, Koerber JM, Mattson JC: A comparison of lepirudin and argatroban outcomes. Clin Appl Thromb Hemost. 2005 Oct;11(4):371-4.Tardy B, Lecompte T, Boelhen F, Tardy-Poncet B, Elalamy I, Morange P, Gruel Y, Wolf M, Francois D, Racadot E, Camarasa P, Blouch MT, Nguyen F, Doubine S, Dutrillaux F, Alhenc-Gelas M, Martin-Toutain I, Bauters A, Ffrench P, de Maistre E, Grunebaum L, Mouton C, Huisse MG, Gouault-Heilmann M, Lucke V: Predictive factors for thrombosis and major bleeding in an observational study in 181 patients with heparin-induced thrombocytopenia treated with lepirudin. Blood. 2006 Sep 1;108(5):1492-6. Epub 2006 May 11.Lubenow N, Eichler P, Lietz T, Greinacher A: Lepirudin in patients with heparin-induced thrombocytopenia - results of the third prospective study (HAT-3) and a combined analysis of HAT-1, HAT-2, and HAT-3. J Thromb Haemost. 2005 Nov;3(11):2428-36. 162447621669096716241940 approved Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides 5180668 United States 1993-01-19 2010-01-19 false drug_action DB00001DB01022DB01373 LepirudinPhylloquinoneCalcium P00734P00748P02452P03952P03951P00740P00451P12259P00742P02671P02675P02679P00488P05160P00747P00750P08709P13726Q9BQB6P38435 Lepirudin Action Pathway SMP00278 Bayer healthcare pharmaceuticals inc false LepirudinLepirudinLepirudinLepirudinLepirudin RefludanRefludanRefludanRefludanRefludan Bayer HealthcareBerlex Labs http://www.bayerhealthcare.comhttp://www.berlex.com RefludanRefludanRefludanRefludanRefludan falsefalsefalsefalsefalse BayerCelgene Europe LimitedCelgene Europe LimitedCelgene Europe LimitedCelgene Europe Limited falsefalsefalsefalsefalse IntravenousIntravenousIntravenousIntravenousIntravenous Powder, for solutionInjection, solution, concentrateInjection, solution, concentrateInjection, solution, concentrateInjection, solution, concentrate DPDEMAEMAEMAEMA 50 mg50 mg50 mg20 mg20 mg truefalsefalsefalsefalse 02240996 CanadaEUEUEUEU 2000-01-311997-03-131997-03-131997-03-131997-03-13 2013-07-262012-07-272012-07-272012-07-272012-07-27 vial 273.19 USD Refludan 50 mg vial DB00002 205923-56-4 Cetuximab CetuximabCétuximabCetuximabumImmunoglobulin G 1 (human-mouse monoclonal C 225 gamma 1 - chain anti-human epidermal growt factor receptor), disulfide wit human-mouse monoclonal C 225 kappa - chain, dimer biotech PQX0D8J21J //s3-us-west-2.amazonaws.com/drugbank/msds/DB00002.pdf?1458412933 liquid Cetuximab is an epidermal growth factor receptor binding FAB. Cetuximab is composed of the Fv (variable; antigen-binding) regions of the 225 murine EGFr monoclonal antibody specific for the N-terminal portion of human EGFr with human IgG1 heavy and kappa light chain constant (framework) regions. Cetuximab is marketed under the brand Erbitux® by Eli Lilly and Company. In the United States, a regimen of cetuximab costs approximately $30,790 for an eight-week course. Humans and other mammals Injection, solutionSolutionSolution IntravenousIntravenousIntravenous 5 mg/ml2 mg2 mg/mL Cetuximab, used in combination with irinotecan, is indicated for the treatment of EGFR-expressing, metastatic colorectal carcinoma in patients who are refractory to irinotecan-based chemotherapy. Cetuximab administered as a single agent is indicated for the treatment of EGFR-expressing, metastatic colorectal carcinoma in patients who are intolerant to irinotecan-based chemotherapy. Cetuximab binds to the epidermal growth factor receptor (EGFr) on both normal and tumor cells. EGFr is over-expressed in many colorectal cancers. Cetuximab competitively inhibits the binding of epidermal growth factor (EGF) and TGF alpha, thereby reducing their effects on cell growth and metastatic spread. antagonist Epidermal growth factor receptorLow affinity immunoglobulin gamma Fc region receptor III-BComplement C1r subcomponentComplement C1q subcomponent subunit AComplement C1q subcomponent subunit BComplement C1q subcomponent subunit CLow affinity immunoglobulin gamma Fc region receptor III-AComplement C1s subcomponentHigh affinity immunoglobulin gamma Fc receptor ILow affinity immunoglobulin gamma Fc region receptor II-aLow affinity immunoglobulin gamma Fc region receptor II-bLow affinity immunoglobulin gamma Fc region receptor II-c BE0000767BE0000901BE0002093BE0002094BE0002095BE0002096BE0002097BE0001529BE0000710BE0002098BE0002099BE0002100 HumanHumanHumanHumanHumanHumanHumanHumanHumanHumanHumanHuman Hosokawa N, Yamamoto S, Uehara Y, Hori M, Tsuchiya KS: Effect of thiazinotrienomycin B, an ansamycin antibiotic, on the function of epidermal growth factor receptor in human stomach tumor cells. J Antibiot (Tokyo). 1999 May;52(5):485-90.Wakita H, Takigawa M: Activation of epidermal growth factor receptor promotes late terminal differentiation of cell-matrix interaction-disrupted keratinocytes. J Biol Chem. 1999 Dec 24;274(52):37285-91.Suwa T, Ueda M, Jinno H, Ozawa S, Kitagawa Y, Ando N, Kitajima M: Epidermal growth factor receptor-dependent cytotoxic effect of anti-EGFR antibody-ribonuclease conjugate on human cancer cells. Anticancer Res. 1999 Sep-Oct;19(5B):4161-5.Burke P, Schooler K, Wiley HS: Regulation of epidermal growth factor receptor signaling by endocytosis and intracellular trafficking. Mol Biol Cell. 2001 Jun;12(6):1897-910.Viloria-Petit A, Crombet T, Jothy S, Hicklin D, Bohlen P, Schlaeppi JM, Rak J, Kerbel RS: Acquired resistance to the antitumor effect of epidermal growth factor receptor-blocking antibodies in vivo: a role for altered tumor angiogenesis. Cancer Res. 2001 Jul 1;61(13):5090-101.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.Snyder LC, Astsaturov I, Weiner LM: Overview of monoclonal antibodies and small molecules targeting the epidermal growth factor receptor pathway in colorectal cancer. Clin Colorectal Cancer. 2005 Nov;5 Suppl 2:S71-80.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Zhang W, Gordon M, Schultheis AM, Yang DY, Nagashima F, Azuma M, Chang HM, Borucka E, Lurje G, Sherrod AE, Iqbal S, Groshen S, Lenz HJ: FCGR2A and FCGR3A polymorphisms associated with clinical outcome of epidermal growth factor receptor expressing metastatic colorectal cancer patients treated with single-agent cetuximab. J Clin Oncol. 2007 Aug 20;25(24):3712-8.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Negri DR, Tosi E, Valota O, Ferrini S, Cambiaggi A, Sforzini S, Silvani A, Ruffini PA, Colnaghi MI, Canevari S: In vitro and in vivo stability and anti-tumour efficacy of an anti-EGFR/anti-CD3 F(ab')2 bispecific monoclonal antibody. Br J Cancer. 1995 Oct;72(4):928-33.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Zhang W, Gordon M, Schultheis AM, Yang DY, Nagashima F, Azuma M, Chang HM, Borucka E, Lurje G, Sherrod AE, Iqbal S, Groshen S, Lenz HJ: FCGR2A and FCGR3A polymorphisms associated with clinical outcome of epidermal growth factor receptor expressing metastatic colorectal cancer patients treated with single-agent cetuximab. J Clin Oncol. 2007 Aug 20;25(24):3712-8.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. 1048057310601294106283691140859411431346117523521633675217139284170164231713928417016423171392841701642317139284170164231713928417016423177044201713928417016423754724217139284170164231770442017139284170164231713928417016423 P00533O75015P00736P02745P02746P02747P08637P09871P12314P12318P31994P31995 Epidermal growth factor receptorLow affinity immunoglobulin gamma Fc region receptor III-BComplement C1r subcomponentComplement C1q subcomponent subunit AComplement C1q subcomponent subunit BComplement C1q subcomponent subunit CLow affinity immunoglobulin gamma Fc region receptor III-AComplement C1s subcomponentHigh affinity immunoglobulin gamma Fc receptor ILow affinity immunoglobulin gamma Fc region receptor II-aLow affinity immunoglobulin gamma Fc region receptor II-bLow affinity immunoglobulin gamma Fc region receptor II-c 7p121q2312p131p36.121p36.121p36.111q2312p131q21.2-q21.31q231q231q23.3 HumanHumanHumanHumanHumanHumanHumanHumanHumanHumanHumanHuman cytoplasmfocal adhesionearly endosome membranebasolateral plasma membranemembranecell surfaceendosome membranemembrane raftnucleusendosomeplasma membraneendocytic vesicleintegral component of membranereceptor complexnuclear membraneextracellular spaceperinuclear region of cytoplasmmultivesicular body, internal vesicle lumenGolgi membraneShc-EGFR complexendoplasmic reticulum membraneepidermal growth factor-activated receptor activityATP bindingprotein heterodimerization activityenzyme bindingactin filament bindingtransmembrane receptor protein tyrosine kinase activityreceptor signaling protein tyrosine kinase activitytransmembrane signaling receptor activityidentical protein bindingprotein phosphatase bindingdouble-stranded DNA bindingubiquitin protein ligase bindingchromatin bindingprotein tyrosine kinase activityMAP kinase kinase kinase activityaxon guidancepositive regulation of fibroblast proliferationpositive regulation of MAP kinase activityactivation of MAPKK activitysmall GTPase mediated signal transductionepidermal growth factor receptor signaling pathwaypositive regulation of phosphorylationpositive regulation of epithelial cell proliferationphosphatidylinositol-mediated signalingfibroblast growth factor receptor signaling pathwayactivation of phospholipase A2 activity by calcium-mediated signalingcellular response to estradiol stimuluscell surface receptor signaling pathwayinnate immune responsepositive regulation of cyclin-dependent protein serine/threonine kinase activity involved in G1/S transition of mitotic cell cyclesignal transductionpositive regulation of ERK1 and ERK2 cascadeinsulin receptor signaling pathwaymorphogenesis of an epithelial foldresponse to stressnegative regulation of protein catabolic processpositive regulation of cell proliferationpeptidyl-tyrosine phosphorylationnegative regulation of epidermal growth factor receptor signaling pathwayprotein autophosphorylationMAPK cascaderesponse to UV-Apositive regulation of protein phosphorylationregulation of peptidyl-tyrosine phosphorylationnegative regulation of apoptotic processpositive regulation of nitric oxide biosynthetic processFc-epsilon receptor signaling pathwaypositive regulation of catenin import into nucleusneurotrophin TRK receptor signaling pathwaycell proliferationembryonic placenta developmentsalivary gland morphogenesisossificationpositive regulation of transcription from RNA polymerase II promotersingle organismal cell-cell adhesioncellular response to amino acid stimulusprotein insertion into membraneRas protein signal transductioncerebral cortex cell migrationpositive regulation of DNA replicationcellular response to epidermal growth factor stimulusdigestive tract morphogenesispositive regulation of protein kinase B signalingvascular endothelial growth factor receptor signaling pathwaypositive regulation of cell migrationregulation of nitric-oxide synthase activitypositive regulation of DNA repairactivation of phospholipase C activitylearning or memoryhair follicle developmentplasma membraneextracellular exosomeanchored component of membraneimmune responsepositive regulation of defense response to virus by hostxenophagymitophagy in response to mitochondrial depolarizationextracellular regionextracellular exosomeblood microparticlecalcium ion bindingserine-type endopeptidase activityserine-type peptidase activityproteolysisimmune responsecomplement activationinnate immune responsecomplement activation, classical pathwayextracellular regionextracellular exosomecollagen trimercomplement component C1 complexcomplement activationcell-cell signalinginnate immune responsecomplement activation, classical pathwayextracellular regionextracellular exosomeblood microparticlecollagen trimercomplement component C1 complexcomplement activationinnate immune responseinner ear developmentcomplement activation, classical pathwayextracellular regionextracellular spaceextracellular exosomeblood microparticlecollagen trimerimmune responsecomplement activationinnate immune responsecomplement activation, classical pathwaynegative regulation of granulocyte differentiationnegative regulation of macrophage differentiationplasma membraneintegral component of membraneextracellular exosomeexternal side of plasma membraneimmune responseFc-gamma receptor signaling pathway involved in phagocytosisinnate immune responseregulation of immune responseextracellular regionextracellular exosomeblood microparticlecalcium ion bindingserine-type endopeptidase activityidentical protein bindingproteolysiscomplement activationinnate immune responsecomplement activation, classical pathwayearly endosome membraneplasma membraneintegral component of membraneclathrin-coated endocytic vesicle membranereceptor signaling protein activitysignal transductioncytokine-mediated signaling pathwayimmune responseantigen processing and presentation of exogenous peptide antigen via MHC class I, TAP-dependentantigen processing and presentation of peptide antigen via MHC class Iinterferon-gamma-mediated signaling pathwayFc-gamma receptor signaling pathway involved in phagocytosisinnate immune responseregulation of immune responseantigen processing and presentation of exogenous peptide antigen via MHC class Iphagocytosis, engulfmentintracellular signal transductionplasma membraneintegral component of membraneextracellular exosomeFc-gamma receptor signaling pathway involved in phagocytosisinnate immune responseplasma membraneintegral component of membranesignal transductionimmune responseregulation of immune responseviral processcytoplasmplasma membraneintegral component of membranetransmembrane signaling receptor activitysignal transductionimmune response Ubiquitin protein ligase bindingSerine-type peptidase activitySerine-type endopeptidase activityReceptor signaling protein activityTransmembrane signaling receptor activity Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses. Known ligands include EGF, TGFA/TGF-alpha, amphiregulin, epigen/EPGN, BTC/betacellulin, epiregulin/EREG and HBEGF/heparin-binding EGF. Ligand binding triggers receptor homo- and/or heterodimerization and autophosphorylation on key cytoplasmic residues. The phosphorylated receptor recruits adapter proteins like GRB2 which in turn activates complex downstream signaling cascades. Activates at least 4 major downstream signaling cascades including the RAS-RAF-MEK-ERK, PI3 kinase-AKT, PLCgamma-PKC and STATs modules. May also activate the NF-kappa-B signaling cascade. Also directly phosphorylates other proteins like RGS16, activating its GTPase activity and probably coupling the EGF receptor signaling to the G protein-coupled receptor signaling. Also phosphorylates MUC1 and increases its interaction with SRC and CTNNB1/beta-catenin.Isoform 2 may act as an antagonist of EGF action.Receptor for the Fc region of immunoglobulins gamma. Low affinity receptor. Binds complexed or aggregated IgG and also monomeric IgG. Contrary to III-A, is not capable to mediate antibody-dependent cytotoxicity and phagocytosis. May serve as a trap for immune complexes in the peripheral circulation which does not activate neutrophils.C1r B chain is a serine protease that combines with C1q and C1s to form C1, the first component of the classical pathway of the complement system.C1q associates with the proenzymes C1r and C1s to yield C1, the first component of the serum complement system. The collagen-like regions of C1q interact with the Ca(2+)-dependent C1r(2)C1s(2) proenzyme complex, and efficient activation of C1 takes place on interaction of the globular heads of C1q with the Fc regions of IgG or IgM antibody present in immune complexes.C1q associates with the proenzymes C1r and C1s to yield C1, the first component of the serum complement system. The collagen-like regions of C1q interact with the Ca(2+)-dependent C1r(2)C1s(2) proenzyme complex, and efficient activation of C1 takes place on interaction of the globular heads of C1q with the Fc regions of IgG or IgM antibody present in immune complexes.C1q associates with the proenzymes C1r and C1s to yield C1, the first component of the serum complement system. The collagen-like regions of C1q interact with the Ca(2+)-dependent C1r(2)C1s(2) proenzyme complex, and efficient activation of C1 takes place on interaction of the globular heads of C1q with the Fc regions of IgG or IgM antibody present in immune complexes.Receptor for the Fc region of IgG. Binds complexed or aggregated IgG and also monomeric IgG. Mediates antibody-dependent cellular cytotoxicity (ADCC) and other antibody-dependent responses, such as phagocytosis.C1s B chain is a serine protease that combines with C1q and C1r to form C1, the first component of the classical pathway of the complement system. C1r activates C1s so that it can, in turn, activate C2 and C4.High affinity receptor for the Fc region of immunoglobulins gamma. Functions in both innate and adaptive immune responses.Binds to the Fc region of immunoglobulins gamma. Low affinity receptor. By binding to IgG it initiates cellular responses against pathogens and soluble antigens. Promotes phagocytosis of opsonized antigens.Receptor for the Fc region of complexed or aggregated immunoglobulins gamma. Low affinity receptor. Involved in a variety of effector and regulatory functions such as phagocytosis of immune complexes and modulation of antibody production by B-cells. Binding to this receptor results in down-modulation of previous state of cell activation triggered via antigen receptors on B-cells (BCR), T-cells (TCR) or via another Fc receptor. Isoform IIB1 fails to mediate endocytosis or phagocytosis. Isoform IIB2 does not trigger phagocytosis.Receptor for the Fc region of complexed immunoglobulins gamma. Low affinity receptor. Involved in a variety of effector and regulatory functions such as phagocytosis of immune complexes and modulation of antibody production by B-cells. Pulmonary ToxicityInterstitial lung disease (ILD) was reported in 3 of 633 (<0.5%) patients with advanced colorectal cancer receiving cetuximab. Interstitial pneumonitis with non-cardiogenic pulmonary edema resulting in death was reported in one case. Two patients had pre-existing fibrotic lung disease and experienced an acute exacerbation of their disease while receiving cetuximab in combination with irinotecan. In the clinical investigational program, an additional case of interstitial pneumonitis was reported in a patient with head and neck cancer treated with cetuximab and cisplatin. The onset of symptoms occurred between the fourth and eleventh doses of treatment in all reported cases. The mean half-life for Cetuximab is 114 hours (range 75-188 hours). Female patients had 25% lower intrinsic clearance than male patients. appeared to be independent of dose and approximated the vascular space of 2-3 L/m2. Used in the treatment of colorectal cancer, cetuximab binds specifically to the epidermal growth factor receptor (EGFr, HER1, c-ErbB-1) on both normal and tumor cells. EGFr is over-expressed in many colorectal cancers. Cetuximab competitively inhibits the binding of epidermal growth factor (EGF) and other ligands, such as transforming growth factor–alpha. Binding of cetuximab to the EGFr blocks phosphorylation and activation of receptor-associated kinases, resulting in inhibition of cell growth, induction of apoptosis, decreased matrix metalloproteinase secretion and reduced vascular endothelial growth factor production. Trastuzumab may increase the cardiotoxic activities of Cetuximab.The risk or severity of cytotoxicity can be increased when Ancestim is combined with Cetuximab.The therapeutic efficacy of Varicella Zoster Vaccine (Live/Attenuated) can be decreased when used in combination with Cetuximab.The therapeutic efficacy of Yellow Fever Vaccine can be decreased when used in combination with Cetuximab.The therapeutic efficacy of Clostridium tetani toxoid antigen (formaldehyde inactivated) can be decreased when used in combination with Cetuximab.The therapeutic efficacy of Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated) can be decreased when used in combination with Cetuximab.The therapeutic efficacy of Rotavirus Vaccine can be decreased when used in combination with Cetuximab.The therapeutic efficacy of G17DT can be decreased when used in combination with Cetuximab.The therapeutic efficacy of INGN 201 can be decreased when used in combination with Cetuximab.The therapeutic efficacy of INGN 225 can be decreased when used in combination with Cetuximab.The therapeutic efficacy of Rindopepimut can be decreased when used in combination with Cetuximab.The therapeutic efficacy of SRP 299 can be decreased when used in combination with Cetuximab.The therapeutic efficacy of GI-5005 can be decreased when used in combination with Cetuximab.The therapeutic efficacy of TG4010 can be decreased when used in combination with Cetuximab.The therapeutic efficacy of Rabies virus inactivated antigen, A can be decreased when used in combination with Cetuximab.The therapeutic efficacy of Tecemotide can be decreased when used in combination with Cetuximab.The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Cetuximab.The therapeutic efficacy of Rubella virus vaccine can be decreased when used in combination with Cetuximab.The therapeutic efficacy of Anthrax immune globulin human can be decreased when used in combination with Cetuximab.The therapeutic efficacy of Bacillus calmette-guerin substrain tice live antigen can be decreased when used in combination with Cetuximab.The therapeutic efficacy of Japanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated) can be decreased when used in combination with Cetuximab.The therapeutic efficacy of Salmonella typhi ty2 vi polysaccharide antigen can be decreased when used in combination with Cetuximab.The therapeutic efficacy of Bacillus calmette-guerin substrain connaught live antigen can be decreased when used in combination with Cetuximab.The therapeutic efficacy of Hepatitis A Vaccine can be decreased when used in combination with Cetuximab.The therapeutic efficacy of Salmonella typhi ty21a live antigen can be decreased when used in combination with Cetuximab.The therapeutic efficacy of Human rabies virus immune globulin can be decreased when used in combination with Cetuximab.The therapeutic efficacy of Hepatitis B Vaccine (Recombinant) can be decreased when used in combination with Cetuximab.The risk or severity of adverse effects can be increased when Paclitaxel is combined with Cetuximab.The risk or severity of adverse effects can be increased when Docetaxel is combined with Cetuximab.The risk or severity of adverse effects can be increased when Cabazitaxel is combined with Cetuximab.Digoxin may decrease the cardiotoxic activities of Cetuximab.Acetyldigitoxin may decrease the cardiotoxic activities of Cetuximab.Deslanoside may decrease the cardiotoxic activities of Cetuximab.Ouabain may decrease the cardiotoxic activities of Cetuximab.Digitoxin may decrease the cardiotoxic activities of Cetuximab.Cymarin may decrease the cardiotoxic activities of Cetuximab.Proscillaridin may decrease the cardiotoxic activities of Cetuximab.Metildigoxin may decrease the cardiotoxic activities of Cetuximab.Peruvoside may decrease the cardiotoxic activities of Cetuximab.Lanatoside C may decrease the cardiotoxic activities of Cetuximab.Gitoformate may decrease the cardiotoxic activities of Cetuximab.Acetyldigoxin may decrease the cardiotoxic activities of Cetuximab.Oleandrin may decrease the cardiotoxic activities of Cetuximab.Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Cetuximab.Bevacizumab may increase the cardiotoxic activities of Cetuximab.Cyclophosphamide may increase the cardiotoxic activities of Cetuximab.The risk or severity of adverse effects can be increased when Cetuximab is combined with Belimumab. DB00072DB09103DB10318DB10805DB10583DB10584DB10276DB04914DB05322DB05325DB05374DB05440DB05942DB06584DB10283DB12568DB12768DB10317DB09057DB10343DB10769DB10803DB10804DB10989DB11050DB11603DB11627DB01229DB01248DB06772DB00390DB00511DB01078DB01092DB01396DB13240DB13307DB13401DB13756DB13467DB13537DB13691DB12843DB00076DB00112DB00531DB08879 TrastuzumabAncestimVaricella Zoster Vaccine (Live/Attenuated)Yellow Fever VaccineClostridium tetani toxoid antigen (formaldehyde inactivated)Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated)Rotavirus VaccineG17DTINGN 201INGN 225RindopepimutSRP 299GI-5005TG4010Rabies virus inactivated antigen, ATecemotideBCG vaccineRubella virus vaccineAnthrax immune globulin humanBacillus calmette-guerin substrain tice live antigenJapanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated)Salmonella typhi ty2 vi polysaccharide antigenBacillus calmette-guerin substrain connaught live antigenHepatitis A VaccineSalmonella typhi ty21a live antigenHuman rabies virus immune globulinHepatitis B Vaccine (Recombinant)PaclitaxelDocetaxelCabazitaxelDigoxinAcetyldigitoxinDeslanosideOuabainDigitoxinCymarinProscillaridinMetildigoxinPeruvosideLanatoside CGitoformateAcetyldigoxinOleandrinDigoxin Immune Fab (Ovine)BevacizumabCyclophosphamideBelimumab Melting PointHydrophobicityIsoelectric PointMolecular WeightMolecular Formula 61 °C (FAB fragment), 71 °C (whole mAb)-0.4138.48145781.6C6484H10042N1732O2023S36 Vermeer, A.W.P. & Norde, W., Biophys. J. 78:394-404 (2000) L01XC06 Monoclonal antibodiesOTHER ANTINEOPLASTIC AGENTSANTINEOPLASTIC AGENTSANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L01XCL01XL01L Amino Acids, Peptides, and ProteinsAntibodiesAntibodies, MonoclonalAntibodies, Monoclonal, HumanizedAntineoplastic AgentsAntineoplastic and Immunomodulating AgentsBlood ProteinsChemical Actions and UsesEpidermal Growth Factor Receptor AntagonistGlobulinsImmunoglobulinsImmunoproteinsPharmacologic ActionsProteinsSerum GlobulinsTherapeutic Uses D000602D000906D000911D061067D000970D001798D020164D005916D007136D007162D020228D011506D012712D045506 1317546507042D03455J00228PA10040DNC000788CetuximabCHEMBL1201577 Drugs Product Database (DPD)PubChem SubstanceKEGG DrugGenBankPharmGKBTherapeutic Targets DatabaseWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic3/erbitux.htmhttp://www.drugs.com/cdi/cetuximab.html //s3-us-west-2.amazonaws.com/drugbank/fda_labels/DB00002.pdf?1265922813 Hosokawa N, Yamamoto S, Uehara Y, Hori M, Tsuchiya KS: Effect of thiazinotrienomycin B, an ansamycin antibiotic, on the function of epidermal growth factor receptor in human stomach tumor cells. J Antibiot (Tokyo). 1999 May;52(5):485-90.Wakita H, Takigawa M: Activation of epidermal growth factor receptor promotes late terminal differentiation of cell-matrix interaction-disrupted keratinocytes. J Biol Chem. 1999 Dec 24;274(52):37285-91.Suwa T, Ueda M, Jinno H, Ozawa S, Kitagawa Y, Ando N, Kitajima M: Epidermal growth factor receptor-dependent cytotoxic effect of anti-EGFR antibody-ribonuclease conjugate on human cancer cells. Anticancer Res. 1999 Sep-Oct;19(5B):4161-5.Burke P, Schooler K, Wiley HS: Regulation of epidermal growth factor receptor signaling by endocytosis and intracellular trafficking. Mol Biol Cell. 2001 Jun;12(6):1897-910.Viloria-Petit A, Crombet T, Jothy S, Hicklin D, Bohlen P, Schlaeppi JM, Rak J, Kerbel RS: Acquired resistance to the antitumor effect of epidermal growth factor receptor-blocking antibodies in vivo: a role for altered tumor angiogenesis. Cancer Res. 2001 Jul 1;61(13):5090-101.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.Schrag D: The price tag on progress--chemotherapy for colorectal cancer. N Engl J Med. 2004 Jul 22;351(4):317-9.Snyder LC, Astsaturov I, Weiner LM: Overview of monoclonal antibodies and small molecules targeting the epidermal growth factor receptor pathway in colorectal cancer. Clin Colorectal Cancer. 2005 Nov;5 Suppl 2:S71-80. 1048057310601294106283691140859411431346117523521526930816336752 approved Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides 1340417 Canada 1999-03-02 2016-03-02 false drug_action DB00002 Cetuximab P00533 Cetuximab Action Pathway SMP00474 CetuximabCetuximabCetuximabCetuximabCetuximab ErbituxErbituxErbituxErbituxErbitux Cardinal HealthCatalent Pharma SolutionsImClone Systems Inc.Oso Biopharmaceuticals Manufacturing LLC http://www.cardinal.comhttp://www.catalent.comhttp://www.imclone.com ErbituxErbituxErbituxErbituxErbitux falsefalsefalsefalsefalse Im Clone LlcMerck K Ga AMerck K Ga AIm Clone LlcIm Clone Llc falsefalsefalsefalsefalse IntravenousIntravenousIntravenousIntravenousIntravenous SolutionInjection, solutionInjection, solutionSolutionSolution DPDEMAEMAFDA NDCFDA NDC 2 mg5 mg/ml5 mg/ml2 mg/mL2 mg/mL 66733-94866733-958 BLA125084BLA125084 truetruetruetruetrue 02271249 CanadaEUEUUSUS 2008-10-282004-06-292004-06-292004-02-122007-10-02 DB00003 143831-71-4 Dornase alfa Deoxyribonuclease (human clone 18-1 protein moiety)Dornase alfa, recombinantDornase alphaRecombinant deoxyribonuclease (DNAse) biotech 953A26OA1Y //s3-us-west-2.amazonaws.com/drugbank/msds/DB00003.pdf?1410714694 liquid Dornase alfa is a biosynthetic form of human deoxyribunuclease I (DNase I) enzyme. It is produced in genetically modified Chinese hamster ovary (CHO) cells using recombinant DNA technology. The 260-amino acid sequence of dornase alfa is identical to the endogenous human enzyme. Dornase alfa cleaves extracellular DNA to 5´-phosphodinucleotide and 5´-phosphooligonucleotide end products without affecting intracellular DNA. In individuals with cystic fibrosis, extracellular DNA, which is an extremely viscous anion, is released by degenerating leukocytes that accumulate during inflammatory responses to infections. Enzymatic breakdown of this extracellular DNA appears to reduce sputum viscosity and viscoelasticity. Humans and other mammals SolutionSolution Respiratory (inhalation)Respiratory (inhalation) 1 mg/mL1 mg Used as adjunct therapy in the treatment of cystic fibrosis. Dornase alfa is a biosynthetic form of human DNase I. The enzyme is involved in endonucleolytic cleavage of extracellular DNA to 5´-phosphodinucleotide and 5´-phosphooligonucleotide end products. It has no effect on intracellular DNA. Optimal activity is dependent on the presence of divalent cations such as calcium and magnesium. Extracellular DNA is a viscous anionic polymer and its breakdown appears to improve the viscosity and viscoelasticity of purulent sputum of individuals with CF, thus reducing airflow obstruction. Dornase alfa does not seem to have any effect on non-purulent sputum. DNA BE0004796 Human Cramer GW, Bosso JA: The role of dornase alfa in the treatment of cystic fibrosis. Ann Pharmacother. 1996 Jun;30(6):656-61. 8792953 Adverse reactions occur at a frequency of < 1/1000 and are usually mild and transient in nature. Reported adverse effects include chest pain (pleuritic/non-cardiac), fever, dyspepsia, voice alteration (hoarseness), pharyngitis, dyspnea, laryngitis, rhinitis, decreased lung function, rash, urticaria, and conjunctivitis. There is no evidence of carcinogenic or mutagenic properties. The safety of dornase alfa has not been studied in pregnant women, nursing women and children under the age of 5 years old. Studies in rats and monkeys after inhalation of dornase alfa shows very little systemic absorption (less than 15% for rats and less than 2% for monkeys). The results were also witnessed in patients. Dornase alfa is also associated with very low accumulation with no serum concentration greater than 10ng/mL observed no matter the dose administered. Bioavailability: mean sputum concentrations of dornase alfa can be measured after 15 minutes. Onset is achieved within 3 to 7 days. Peak concentrations are achieved after 9 days. While no conclusive studies have yet been published, dornase alfa is expected to be metabolized by proteases in biofluids. Studies in rats indicate that, following aerosol administration, the disappearance half-life of dornase alfa from the lungs is 11 hours. In humans, sputum DNase levels declined below half of those detected immediately post-administration within 2 hours but effects on sputum rheology persisted beyond 12 hours. In studies in rats and monkeys, the initial volume of distribution is similar to the serum volume. Concentrations in sputum decline rapidly after inhalation. Cystic fibrosis (CF) is a disease characterized by the retention of viscous purulent secretions in the airways. These thick secretions contribute both to reduced pulmonary function and to frequent pulmonary infection. Purulent pulmonary secretions of individuals with cystic fibrosis contain very high concentrations of extracellular DNA released by degenerating leukocytes that accumulate in response to these infections. Dornase alfa hydrolyzes the DNA in sputum of CF patients and reduces sputum viscosity and viscoelasticity. The enzyme does not appear to affect sputum in the absence of an inflammatory response to infection, nor does it affect the sputum of healthy individuals. Melting PointHydrophobicityIsoelectric PointMolecular WeightMolecular Formula 67 °C-0.0834.5829253.9C1321H1999N339O396S9 Chan, H.K. et al., Pharm Res. 13:756-761 (1996) R05CB13 MucolyticsEXPECTORANTS, EXCL. COMBINATIONS WITH COUGH SUPPRESSANTSCOUGH AND COLD PREPARATIONSRESPIRATORY SYSTEM R05CBR05CR05R Amino Acids, Peptides, and ProteinsCough and Cold PreparationsDeoxyribonucleasesEndodeoxyribonucleasesEndonucleasesEnzymesEnzymes and CoenzymesEsterasesExpectorantsHydrolasesProteinsRecombinant Human Deoxyribonuclease 1Respiratory System D000602D003851D004706D004720D004798D045762D004950D005100D006867D011506D012137 65046507792M55983PA10318P24855DAP000981Dornase_alfaCHEMBL1201431 Drugs Product Database (DPD)PubChem SubstanceGenBankPharmGKBUniProtKBTherapeutic Targets DatabaseWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic/pulmozyme.htmhttp://www.drugs.com/cdi/dornase-alfa.html //s3-us-west-2.amazonaws.com/drugbank/fda_labels/DB00003.pdf?1410715221 Cramer GW, Bosso JA: The role of dornase alfa in the treatment of cystic fibrosis. Ann Pharmacother. 1996 Jun;30(6):656-61.Jones AP, Wallis C: Dornase alfa for cystic fibrosis. Cochrane Database Syst Rev. 2010 Mar 17;(3):CD001127. doi: 10.1002/14651858.CD001127.pub2.Riethmueller J, Kumpf M, Borth-Bruhns T, Brehm W, Wiskirchen J, Sieverding L, Ankele C, Hofbeck M, Baden W: Clinical and in vitro effect of dornase alfa in mechanically ventilated pediatric non-cystic fibrosis patients with atelectases. Cell Physiol Biochem. 2009;23(1-3):205-10. doi: 10.1159/000204109. Epub 2009 Feb 18. 87929532023831419255515 approved Roche (Chile) Viscozyme Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides 21845812137237 CanadaCanada 2005-02-222004-10-26 2015-02-282013-05-28 falsefalse Genentech, Inc false Dornase alfaDornase alfa Pulmozyme 1mg/mlPulmozyme Cardinal HealthCatalent Pharma SolutionsF Hoffmann-La Roche Ltd.Genentech Inc.Meda ABMedpointe Pharmaceuticals http://www.cardinal.comhttp://www.catalent.comhttp://www.roche.comhttp://www.gene.comhttp://www.meda.se PulmozymePulmozyme 1mg/ml falsefalse Genentech, Inc.Hoffmann La Roche falsefalse Respiratory (inhalation)Respiratory (inhalation) SolutionSolution FDA NDCDPD 1 mg/mL1 mg 50242-100 BLA103532 truetrue 02046733 USCanada 1993-12-301994-12-31 tablettablettablettablettabletmlplasticml 3.213.843.994.624.8137.0577.060.6 USDUSDUSDUSDUSDUSDUSDUSD Lufyllin 200 mg tabletLufyllin-gg tabletLufyllin-GG 200-200 mg tabletLufyllin-400 tabletLufyllin 400 mg tabletPulmozyme 1 mg/ml ampulPulmozyme 1 mg/ml Solution 2.5ml Plastic ContainerLufyllin-GG 100-100 mg/15ml Elixir DB00004 173146-27-5 Denileukin diftitox Diphtheria toxin precursorDTNAD(+--diphthamide ADP- ribosyltransferase) biotech 25E79B5CTM liquid A recombinant DNA-derived cytotoxic protein composed of the amino acid sequences for diphtheria toxin fragments A and B (Met 1-Thr 387)-His followed by the sequences for interleukin-2 (IL-2; Ala 1-Thr 133). It is produced in an E. coli expression system. Humans and other mammals Injection, solution Intravenous 150 ug/mL For treatment of cutaneous T-cell lymphoma Denileukin diftitox binds to the high-affinity IL-2 receptor complex. The IL-2 receptor (Tac) subunit is expressed on activated but not resting lymphocytes. The diphtheria toxin associated with Ontak then selectively kills the IL-2 bearing cells. binderagonist Interleukin-2 receptor subunit alphaInterleukin-2 receptor subunit betaCytokine receptor common subunit gamma BE0000658BE0000651BE0002102 HumanHumanHuman Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Kiyokawa T, Shirono K, Hattori T, Nishimura H, Yamaguchi K, Nichols JC, Strom TB, Murphy JR, Takatsuki K: Cytotoxicity of interleukin 2-toxin toward lymphocytes from patients with adult T-cell leukemia. Cancer Res. 1989 Jul 15;49(14):4042-6.Murphy JR, Kelley VE, Strom TB: Interleukin 2 toxin: a step toward selective immunomodulation. Am J Kidney Dis. 1988 Feb;11(2):159-62.Duvic M, Talpur R: Optimizing denileukin diftitox (Ontak) therapy. Future Oncol. 2008 Aug;4(4):457-69. doi: 10.2217/14796694.4.4.457.Turturro F: Denileukin diftitox: a biotherapeutic paradigm shift in the treatment of lymphoid-derived disorders. Expert Rev Anticancer Ther. 2007 Jan;7(1):11-7.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.Foss F, Demierre MF, DiVenuti G: A phase-1 trial of bexarotene and denileukin diftitox in patients with relapsed or refractory cutaneous T-cell lymphoma. Blood. 2005 Jul 15;106(2):454-7. Epub 2005 Apr 5.Foss F: Clinical experience with denileukin diftitox (ONTAK). Semin Oncol. 2006 Feb;33(1 Suppl 3):S11-6.Duvic M, Talpur R: Optimizing denileukin diftitox (Ontak) therapy. Future Oncol. 2008 Aug;4(4):457-69. doi: 10.2217/14796694.4.4.457.Turturro F: Denileukin diftitox: a biotherapeutic paradigm shift in the treatment of lymphoid-derived disorders. Expert Rev Anticancer Ther. 2007 Jan;7(1):11-7.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.Foss F, Demierre MF, DiVenuti G: A phase-1 trial of bexarotene and denileukin diftitox in patients with relapsed or refractory cutaneous T-cell lymphoma. Blood. 2005 Jul 15;106(2):454-7. Epub 2005 Apr 5.Foss F: Clinical experience with denileukin diftitox (ONTAK). Semin Oncol. 2006 Feb;33(1 Suppl 3):S11-6.Foss FM: DAB(389)IL-2 (denileukin diftitox, ONTAK): a new fusion protein technology. Clin Lymphoma. 2000 Nov;1 Suppl 1:S27-31. 1713928417016423278674931246101868405717187516117523521581195916516670186840571718751611752352158119591651667011707860 P01589P14784P31785 Interleukin-2 receptor subunit alphaInterleukin-2 receptor subunit betaCytokine receptor common subunit gamma 10p15-p1422q13|22q13.1Xq13.1 HumanHumanHuman external side of plasma membraneintracellularplasma membraneintegral component of membranedrug bindinginterleukin-2 bindinginterleukin-2 receptor activitycell surface receptor signaling pathwayregulation of T cell homeostatic proliferationnegative regulation of inflammatory responseinflammatory response to antigenic stimulusFc-epsilon receptor signaling pathwaynegative regulation of T cell proliferationimmune responseregulation of T cell tolerance inductionactivation of MAPKK activityNotch signaling pathwayapoptotic processnegative regulation of immune responseinflammatory responsefibroblast growth factor receptor signaling pathwaypositive regulation of T cell differentiationsmall GTPase mediated signal transductioninsulin receptor signaling pathwayactivation-induced cell death of T cellscell proliferationMAPK cascadenegative regulation of defense response to virusneurotrophin TRK receptor signaling pathwayaxon guidanceRas protein signal transductionepidermal growth factor receptor signaling pathwayvascular endothelial growth factor receptor signaling pathwaypositive regulation of activated T cell proliferationinnate immune responseintracellularmembraneplasma membraneexternal side of plasma membraneintegral component of plasma membraneinterleukin-2 bindinginterleukin-2 receptor activityviral processFc-epsilon receptor signaling pathwayactivation of MAPKK activitysignal transductionfibroblast growth factor receptor signaling pathwayinterleukin-2-mediated signaling pathwayinsulin receptor signaling pathwaysmall GTPase mediated signal transductionMAPK cascadeprotein complex assemblynegative regulation of apoptotic processaxon guidanceneurotrophin TRK receptor signaling pathwayepidermal growth factor receptor signaling pathwayRas protein signal transductioninnate immune responsevascular endothelial growth factor receptor signaling pathwaycytokine-mediated signaling pathwayintracellularmembraneplasma membraneexternal side of plasma membraneintegral component of plasma membraneinterleukin-2 bindingcytokine receptor activityFc-epsilon receptor signaling pathwayinterleukin-2-mediated signaling pathwayactivation of MAPKK activityinterleukin-4-mediated signaling pathwaysignal transductionfibroblast growth factor receptor signaling pathwayinterleukin-7-mediated signaling pathwayimmune responseinsulin receptor signaling pathwayMAPK cascadesmall GTPase mediated signal transductionneurotrophin TRK receptor signaling pathwayaxon guidanceRas protein signal transductionepidermal growth factor receptor signaling pathwayvascular endothelial growth factor receptor signaling pathwayinnate immune responseviral process Interleukin-2 receptor activityInterleukin-2 receptor activityInterleukin-2 binding Receptor for interleukin-2. The receptor is involved in the regulation of immune tolerance by controlling regulatory T cells (TREGs) activity. TREGs suppress the activation and expansion of autoreactive T cells.Receptor for interleukin-2. This beta subunit is involved in receptor mediated endocytosis and transduces the mitogenic signals of IL2.Common subunit for the receptors for a variety of interleukins. 70-80 min * 0.6 - 2.0 mL/min/kg [Lymphoma] * 0.06 to 0.09 L/kg Denileukin diftitox (Ontak) directs the cytocidal action of diphtheria toxin to cells which express the IL-2 receptor. The human IL-2 receptor exists in three forms, low (CD25), intermediate (CD122/CD132) and high (CD25/CD122/CD132) affinity. Malignant cells expressing one or more of the subunits of the IL-2 receptor are found in certain leukemias and lymphomas including cutaneous T-cell lymphoma (CTCL). Ontak interacts with the high affinity IL-2 receptor on the cell surface and inhibits cellular protein synthesis, resulting in cell death within hours. Trastuzumab may increase the cardiotoxic activities of Denileukin diftitox.The risk or severity of cytotoxicity can be increased when Ancestim is combined with Denileukin diftitox.The risk or severity of adverse effects can be increased when Paclitaxel is combined with Denileukin diftitox.The risk or severity of adverse effects can be increased when Docetaxel is combined with Denileukin diftitox.The risk or severity of adverse effects can be increased when Cabazitaxel is combined with Denileukin diftitox.Digoxin may decrease the cardiotoxic activities of Denileukin diftitox.Acetyldigitoxin may decrease the cardiotoxic activities of Denileukin diftitox.Deslanoside may decrease the cardiotoxic activities of Denileukin diftitox.Ouabain may decrease the cardiotoxic activities of Denileukin diftitox.Digitoxin may decrease the cardiotoxic activities of Denileukin diftitox.Cymarin may decrease the cardiotoxic activities of Denileukin diftitox.Proscillaridin may decrease the cardiotoxic activities of Denileukin diftitox.Metildigoxin may decrease the cardiotoxic activities of Denileukin diftitox.Peruvoside may decrease the cardiotoxic activities of Denileukin diftitox.Lanatoside C may decrease the cardiotoxic activities of Denileukin diftitox.Gitoformate may decrease the cardiotoxic activities of Denileukin diftitox.Acetyldigoxin may decrease the cardiotoxic activities of Denileukin diftitox.Oleandrin may decrease the cardiotoxic activities of Denileukin diftitox.Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Denileukin diftitox.Bevacizumab may increase the cardiotoxic activities of Denileukin diftitox.Cyclophosphamide may increase the cardiotoxic activities of Denileukin diftitox. DB00072DB09103DB01229DB01248DB06772DB00390DB00511DB01078DB01092DB01396DB13240DB13307DB13401DB13756DB13467DB13537DB13691DB12843DB00076DB00112DB00531 TrastuzumabAncestimPaclitaxelDocetaxelCabazitaxelDigoxinAcetyldigitoxinDeslanosideOuabainDigitoxinCymarinProscillaridinMetildigoxinPeruvosideLanatoside CGitoformateAcetyldigoxinOleandrinDigoxin Immune Fab (Ovine)BevacizumabCyclophosphamide HydrophobicityIsoelectric PointMolecular WeightMolecular Formula -0.3015.4557647.3C2560H4042N678O799S17 L01XX29 Other antineoplastic agentsOTHER ANTINEOPLASTIC AGENTSANTINEOPLASTIC AGENTSANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L01XXL01XL01L ADP Ribose TransferasesAmino Acids, Peptides, and ProteinsAntineoplastic AgentsAntineoplastic and Immunomodulating AgentsBacterial ToxinsBiological FactorsChemical Actions and UsesCytokinesEnzymesEnzymes and CoenzymesGlycosyltransferasesIntercellular Signaling Peptides and ProteinsInterleukinsLymphokinesPentosyltransferasesPeptidesPharmacologic ActionsProteinsRecombinant ProteinsTherapeutic UsesToxins, BiologicalTransferases D036002D000602D000970D001427D001685D020164D016207D004798D045762D016695D036341D007378D008222D010430D010455D020228D011506D011994D045506D014118D014166 46506950V01536PA164750594P00587DAP001098Denileukin_diftitoxCHEMBL1201550 PubChem SubstanceGenBankPharmGKBUniProtKBTherapeutic Targets DatabaseWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic2/denileukin.htmhttp://www.drugs.com/cdi/denileukin-diftitox.html //s3-us-west-2.amazonaws.com/drugbank/fda_labels/DB00004.pdf?1265922800 Turturro F: Denileukin diftitox: a biotherapeutic paradigm shift in the treatment of lymphoid-derived disorders. Expert Rev Anticancer Ther. 2007 Jan;7(1):11-7.Park M, Liu GT, Piltz-Seymour J, Wisda CL, Rook AH, Junkins-Hopkins JM, Nasta SD, Kim EJ: Vision loss following denileukin diftitox treatment: a case report of possible posterior ischemic optic neuropathy. Leuk Lymphoma. 2007 Apr;48(4):808-11. 1718751617454642 approvedinvestigational Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides Denileukin diftitox Ontak Eisai Inc.Hollister-Stier Laboratories LLCLigand Pharmaceuticals Inc. http://www.eisai.comhttp://www.hollisterstier.comhttp://www.ligand.com Ontak false Eisai Limited false Intravenous Injection, solution FDA NDC 150 ug/mL 62856-603 BLA103767 true US 2008-10-15 2017-01-31 ml 878.4 USD Ontak 150 mcg/ml vial DB00005 185243-69-0 Etanercept Etanercept-szzsRHU TNFR:FCRHU-TNFR:FCTNFR-Immunoadhesin biotech OP401G7OJC Timothy D. Osslund, Christi L. Clogston, Shon Lee Crampton, Randal B. Bass, "Crystals of etanercept and methods of making thereof." U.S. Patent US07276477, issued October 02, 2007. liquid Dimeric fusion protein consisting of the extracellular ligand-binding portion of the human 75 kilodalton (p75) tumor necrosis factor receptor (TNFR) linked to the Fc portion of human IgG1. The Fc component of etanercept contains the CH2 domain, the CH3 domain and hinge region, but not the CH1 domain of IgG1. Etanercept is produced by recombinant DNA technology in a Chinese hamster ovary (CHO) mammalian cell expression system. It consists of 934 amino acids. Humans and other mammals Injection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, solutionInjection, solutionKitKit; liquid; powder, for solutionSolutionSolutionSolutionSolution SubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneous 10 mg25 mg50 mg25 mg50 mg25 mg/.5mL50 mg50 mg/mL25 mg Etanercept is indicated for the treatment of moderately to severely active rheumatoid arthritis in adults and chronic moderate to severe plaque psoriasis in adults. It is also used to manage signs and symptoms of polyarticular idiopathic arthritis in those aged 4 to 17 after insufficient response to one or more disease-modifying anti-rheumatic drugs. Etanercept is also used to improve psoriatic arthritis and ankylosing spondylitis. There are two distinct receptors for TNF (TNFRs), a 55 kilodalton protein (p55) and a 75 kilodalton protein (p75). The biological activity of TNF is dependent upon binding to either cell surface receptor (p75 or p55). Etanercept is a dimeric soluble form of the p75 TNF receptor that can bind to two TNF molecules, thereby effectively removing them from circulation.TNF is a naturally occurring cytokine that is involved in normal inflammatory and immune responses. Increased levels of TNF are found in tissues and fluids of those with rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis (AS), and plaque psoriasis. antibody Tumor necrosis factorTumor necrosis factor receptor superfamily member 1BHigh affinity immunoglobulin gamma Fc receptor ILow affinity immunoglobulin gamma Fc region receptor III-ALow affinity immunoglobulin gamma Fc region receptor II-aLow affinity immunoglobulin gamma Fc region receptor II-bLow affinity immunoglobulin gamma Fc region receptor II-cLymphotoxin-alphaLow affinity immunoglobulin gamma Fc region receptor III-BComplement C1s subcomponentComplement C1r subcomponentComplement C1q subcomponent subunit AComplement C1q subcomponent subunit BComplement C1q subcomponent subunit C BE0000704BE0000949BE0000710BE0002097BE0002098BE0002099BE0002100BE0001087BE0000901BE0001529BE0002093BE0002094BE0002095BE0002096 HumanHumanHumanHumanHumanHumanHumanHumanHumanHumanHumanHumanHumanHuman Park YC, Burkitt V, Villa AR, Tong L, Wu H: Structural basis for self-association and receptor recognition of human TRAF2. Nature. 1999 Apr 8;398(6727):533-8.Sandborn WJ, Hanauer SB: Antitumor necrosis factor therapy for inflammatory bowel disease: a review of agents, pharmacology, clinical results, and safety. Inflamm Bowel Dis. 1999 May;5(2):119-33.Grell M, Zimmermann G, Gottfried E, Chen CM, Grunwald U, Huang DC, Wu Lee YH, Durkop H, Engelmann H, Scheurich P, Wajant H, Strasser A: Induction of cell death by tumour necrosis factor (TNF) receptor 2, CD40 and CD30: a role for TNF-R1 activation by endogenous membrane-anchored TNF. EMBO J. 1999 Jun 1;18(11):3034-43.Moreland LW: Inhibitors of tumor necrosis factor: new treatment options for rheumatoid arthritis. Cleve Clin J Med. 1999 Jun;66(6):367-74.Calabrese LH: Rheumatoid arthritis and primary care: the case for early diagnosis and treatment. J Am Osteopath Assoc. 1999 Jun;99(6):313-21.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Criswell LA, Lum RF, Turner KN, Woehl B, Zhu Y, Wang J, Tiwari HK, Edberg JC, Kimberly RP, Moreland LW, Seldin MF, Bridges SL Jr: The influence of genetic variation in the HLA-DRB1 and LTA-TNF regions on the response to treatment of early rheumatoid arthritis with methotrexate or etanercept. Arthritis Rheum. 2004 Sep;50(9):2750-6.Hughes LB, Criswell LA, Beasley TM, Edberg JC, Kimberly RP, Moreland LW, Seldin MF, Bridges SL: Genetic risk factors for infection in patients with early rheumatoid arthritis. Genes Immun. 2004 Dec;5(8):641-7.Criswell LA, Lum RF, Turner KN, Woehl B, Zhu Y, Wang J, Tiwari HK, Edberg JC, Kimberly RP, Moreland LW, Seldin MF, Bridges SL Jr: The influence of genetic variation in the HLA-DRB1 and LTA-TNF regions on the response to treatment of early rheumatoid arthritis with methotrexate or etanercept. Arthritis Rheum. 2004 Sep;50(9):2750-6.Hughes LB, Criswell LA, Beasley TM, Edberg JC, Kimberly RP, Moreland LW, Seldin MF, Bridges SL: Genetic risk factors for infection in patients with early rheumatoid arthritis. Genes Immun. 2004 Dec;5(8):641-7.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Hart SP, Ross JA, Ross K, Haslett C, Dransfield I: Molecular characterization of the surface of apoptotic neutrophils: implications for functional downregulation and recognition by phagocytes. Cell Death Differ. 2000 May;7(5):493-503.Ranheim EA, Kipps TJ: Tumor necrosis factor-alpha facilitates induction of CD80 (B7-1) and CD54 on human B cells by activated T cells: complex regulation by IL-4, IL-10, and CD40L. Cell Immunol. 1995 Apr 1;161(2):226-35.Johnson CJ, Reilly KM, Murray KM: Etanercept in juvenile rheumatoid arthritis. Ann Pharmacother. 2001 Apr;35(4):464-71.Pennica D, Lam VT, Mize NK, Weber RF, Lewis M, Fendly BM, Lipari MT, Goeddel DV: Biochemical properties of the 75-kDa tumor necrosis factor receptor. Characterization of ligand binding, internalization, and receptor phosphorylation. J Biol Chem. 1992 Oct 15;267(29):21172-8.Gudbrandsdottir S, Larsen R, Sorensen LK, Nielsen S, Hansen MB, Svenson M, Bendtzen K, Muller K: TNF and LT binding capacities in the plasma of arthritis patients: effect of etanercept treatment in juvenile idiopathic arthritis. Clin Exp Rheumatol. 2004 Jan-Feb;22(1):118-24.Buch MH, Conaghan PG, Quinn MA, Bingham SJ, Veale D, Emery P: True infliximab resistance in rheumatoid arthritis: a role for lymphotoxin alpha? Ann Rheum Dis. 2004 Oct;63(10):1344-6. Epub 2004 Mar 19.Kang CP, Lee KW, Yoo DH, Kang C, Bae SC: The influence of a polymorphism at position -857 of the tumour necrosis factor alpha gene on clinical response to etanercept therapy in rheumatoid arthritis. Rheumatology (Oxford). 2005 Apr;44(4):547-52. Epub 2005 Feb 3.Hart SP, Ross JA, Ross K, Haslett C, Dransfield I: Molecular characterization of the surface of apoptotic neutrophils: implications for functional downregulation and recognition by phagocytes. Cell Death Differ. 2000 May;7(5):493-503.Ozgocmen S, Godekmerdan A, Ozkurt-Zengin F: Acute-phase response, clinical measures and disease activity in ankylosing spondylitis. Joint Bone Spine. 2007 May;74(3):249-53. Epub 2007 Mar 5.Criswell LA, Lum RF, Turner KN, Woehl B, Zhu Y, Wang J, Tiwari HK, Edberg JC, Kimberly RP, Moreland LW, Seldin MF, Bridges SL Jr: The influence of genetic variation in the HLA-DRB1 and LTA-TNF regions on the response to treatment of early rheumatoid arthritis with methotrexate or etanercept. Arthritis Rheum. 2004 Sep;50(9):2750-6.Hughes LB, Criswell LA, Beasley TM, Edberg JC, Kimberly RP, Moreland LW, Seldin MF, Bridges SL: Genetic risk factors for infection in patients with early rheumatoid arthritis. Genes Immun. 2004 Dec;5(8):641-7.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. 1020664910338381103578161037584610405518117523521175235217139284170164231545744215526004154574421552600417139284170164231080008375351961130241113282241500501515033655156952961080008317387033154574421552600417139284170164231713928417016423171392841701642317139284170164231713928417016423 P01375P20333P12314P08637P12318P31994P31995P01374O75015P09871P00736P02745P02746P02747 Tumor necrosis factorTumor necrosis factor receptor superfamily member 1BHigh affinity immunoglobulin gamma Fc receptor ILow affinity immunoglobulin gamma Fc region receptor III-ALow affinity immunoglobulin gamma Fc region receptor II-aLow affinity immunoglobulin gamma Fc region receptor II-bLow affinity immunoglobulin gamma Fc region receptor II-cLymphotoxin-alphaLow affinity immunoglobulin gamma Fc region receptor III-BComplement C1s subcomponentComplement C1r subcomponentComplement C1q subcomponent subunit AComplement C1q subcomponent subunit BComplement C1q subcomponent subunit C 6p21.31p36.3-p36.21q21.2-q21.31q231q231q231q23.36p21.31q2312p1312p131p36.121p36.121p36.11 HumanHumanHumanHumanHumanHumanHumanHumanHumanHumanHumanHumanHumanHuman extracellular regionexternal side of plasma membranephagocytic cupplasma membraneintegral component of plasma membraneextracellular spacemembrane raftcell surfacerecycling endosomecytokine activityidentical protein bindingprotease bindingtumor necrosis factor receptor bindingtranscription regulatory region DNA bindingextrinsic apoptotic signaling pathwaynegative regulation of lipid storagepositive regulation of transcription from RNA polymerase II promoternegative regulation of growth of symbiont in hostpositive regulation of translational initiation by ironregulation of establishment of endothelial barrierpositive regulation of NIK/NF-kappaB signalinglipopolysaccharide-mediated signaling pathwaypositive regulation of protein phosphorylationpositive regulation of protein localization to cell surfacepositive regulation of interferon-gamma productionepithelial cell proliferation involved in salivary gland morphogenesisregulation of tumor necrosis factor-mediated signaling pathwaypositive regulation of calcidiol 1-monooxygenase activitynegative regulation of fat cell differentiationregulation of insulin secretionpositive regulation of interleukin-8 biosynthetic processprotein import into nucleus, translocationregulation of I-kappaB kinase/NF-kappaB signalingnegative regulation of glucose importpositive regulation of ERK1 and ERK2 cascadenegative regulation of branching involved in lung morphogenesisI-kappaB kinase/NF-kappaB signalingpositive regulation of NF-kappaB transcription factor activitypositive regulation of cytokine secretionpositive regulation of chemokine biosynthetic processcell surface receptor signaling pathwaysequestering of triglyceridenecroptotic signaling pathwaypositive regulation of smooth muscle cell proliferationnegative regulation of protein complex disassemblypositive regulation of heterotypic cell-cell adhesionnegative regulation of extrinsic apoptotic signaling pathway in absence of ligandactivation of MAPKKK activitypositive regulation of membrane protein ectodomain proteolysispositive regulation of interleukin-6 productiontumor necrosis factor-mediated signaling pathwaypositive regulation of hair follicle developmentpositive regulation of protein complex assemblyembryonic digestive tract developmentpositive regulation of ceramide biosynthetic processregulation of branching involved in salivary gland morphogenesisactivation of cysteine-type endopeptidase activity involved in apoptotic processosteoclast differentiationpositive regulation of vitamin D biosynthetic processpositive regulation of phagocytosispositive regulation of cell adhesionpositive regulation of chronic inflammatory response to antigenic stimuluspositive regulation of mononuclear cell migrationpositive regulation of podosome assemblycellular response to amino acid stimuluspositive regulation of NFAT protein import into nucleuspositive regulation of osteoclast differentiationreceptor biosynthetic processpositive regulation of interleukin-8 productionpositive regulation of cysteine-type endopeptidase activity involved in apoptotic processpositive regulation of humoral immune response mediated by circulating immunoglobulinhumoral immune responsenegative regulation of myoblast differentiationpositive regulation of chemokine (C-X-C motif) ligand 2 productionextracellular matrix organizationresponse to viruspositive regulation of JUN kinase activityresponse to glucocorticoidregulation of immunoglobulin secretionactivation of MAPK activityleukocyte tethering or rollingpositive regulation of cytokine productioninflammatory responseextrinsic apoptotic signaling pathway via death domain receptorspositive regulation of transcription, DNA-templatednegative regulation of lipid catabolic processpositive regulation of protein kinase activitypositive regulation of sequence-specific DNA binding transcription factor activitynegative regulation of transcription from RNA polymerase II promoternegative regulation of alkaline phosphatase activityJNK cascadepositive regulation of nitric oxide biosynthetic processcortical actin cytoskeleton organizationdefense response to Gram-positive bacteriumnegative regulation of osteoblast differentiationdeath-inducing signaling complex assemblypositive regulation of fever generationpositive regulation of programmed cell deathprotein kinase B signalingglucose metabolic processnegative regulation of cytokine secretion involved in immune responsepositive regulation of chemokine productioncellular response to organic cyclic compoundestablishment of protein localization to plasma membranenegative regulation of interleukin-6 productionresponse to salt stressMAPK cascadenegative regulation of transcription, DNA-templatedchronic inflammatory response to antigenic stimulusintrinsic apoptotic signaling pathway in response to DNA damagepositive regulation of protein transportpositive regulation of gene expressionpositive regulation of I-kappaB kinase/NF-kappaB signalingnegative regulation of bicellular tight junction assemblynegative regulation of viral genome replicationtransformed cell apoptotic processpositive regulation of peptidyl-serine phosphorylationpositive regulation of protein kinase B signalingpositive regulation of NF-kappaB import into nucleuspositive regulation of MAP kinase activitypositive regulation of apoptotic processpositive regulation of protein complex disassemblynegative regulation of gene expressioncellular response to nicotinenegative regulation of myosin-light-chain-phosphatase activityextracellular regionmembrane raftnucleusvaricosityplasma membraneneuronal cell bodyperinuclear region of cytoplasmintegral component of plasma membranetumor necrosis factor-activated receptor activityubiquitin protein ligase bindingextrinsic apoptotic signaling pathwaypositive regulation of membrane protein ectodomain proteolysisnegative regulation of inflammatory responseimmune responsecellular response to lipopolysaccharideRNA destabilizationinflammatory responseregulation of apoptotic processapoptotic signaling pathwayagingintrinsic apoptotic signaling pathway in response to DNA damagepositive regulation of MAPK cascaderegulation of cell proliferationcellular response to growth factor stimulustumor necrosis factor-mediated signaling pathwaymulticellular organismal developmentearly endosome membraneplasma membraneintegral component of membraneclathrin-coated endocytic vesicle membranereceptor signaling protein activitysignal transductioncytokine-mediated signaling pathwayimmune responseantigen processing and presentation of exogenous peptide antigen via MHC class I, TAP-dependentantigen processing and presentation of peptide antigen via MHC class Iinterferon-gamma-mediated signaling pathwayFc-gamma receptor signaling pathway involved in phagocytosisinnate immune responseregulation of immune responseantigen processing and presentation of exogenous peptide antigen via MHC class Iphagocytosis, engulfmentintracellular signal transductionplasma membraneintegral component of membraneextracellular exosomeexternal side of plasma membraneimmune responseFc-gamma receptor signaling pathway involved in phagocytosisinnate immune responseregulation of immune responseplasma membraneintegral component of membraneextracellular exosomeFc-gamma receptor signaling pathway involved in phagocytosisinnate immune responseplasma membraneintegral component of membranesignal transductionimmune responseregulation of immune responseviral processcytoplasmplasma membraneintegral component of membranetransmembrane signaling receptor activitysignal transductionimmune responseplasma membraneextracellular spacereceptor bindingsignal transductionresponse to nutrientresponse to drugpositive regulation of interferon-gamma productionnegative regulation of growth of symbiont in hosttumor necrosis factor-mediated signaling pathwaynegative regulation of fibroblast proliferationhumoral immune responsedefense response to Gram-positive bacteriumcell-cell signalinglymph node developmentpositive regulation of apoptotic processpositive regulation of chronic inflammatory response to antigenic stimulusapoptotic processpositive regulation of glial cell proliferationresponse to hypoxiapositive regulation of humoral immune response mediated by circulating immunoglobulinresponse to lipopolysaccharideplasma membraneextracellular exosomeanchored component of membraneimmune responsepositive regulation of defense response to virus by hostxenophagymitophagy in response to mitochondrial depolarizationextracellular regionextracellular exosomeblood microparticlecalcium ion bindingserine-type endopeptidase activityidentical protein bindingproteolysiscomplement activationinnate immune responsecomplement activation, classical pathwayextracellular regionextracellular exosomeblood microparticlecalcium ion bindingserine-type endopeptidase activityserine-type peptidase activityproteolysisimmune responsecomplement activationinnate immune responsecomplement activation, classical pathwayextracellular regionextracellular exosomecollagen trimercomplement component C1 complexcomplement activationcell-cell signalinginnate immune responsecomplement activation, classical pathwayextracellular regionextracellular exosomeblood microparticlecollagen trimercomplement component C1 complexcomplement activationinnate immune responseinner ear developmentcomplement activation, classical pathwayextracellular regionextracellular spaceextracellular exosomeblood microparticlecollagen trimerimmune responsecomplement activationinnate immune responsecomplement activation, classical pathwaynegative regulation of granulocyte differentiationnegative regulation of macrophage differentiation Tumor necrosis factor receptor bindingUbiquitin protein ligase bindingReceptor signaling protein activityTransmembrane signaling receptor activityReceptor bindingSerine-type endopeptidase activitySerine-type peptidase activity Cytokine that binds to TNFRSF1A/TNFR1 and TNFRSF1B/TNFBR. It is mainly secreted by macrophages and can induce cell death of certain tumor cell lines. It is potent pyrogen causing fever by direct action or by stimulation of interleukin-1 secretion and is implicated in the induction of cachexia, Under certain conditions it can stimulate cell proliferation and induce cell differentiation. Impairs regulatory T-cells (Treg) function in individuals with rheumatoid arthritis via FOXP3 dephosphorylation. Upregulates the expression of protein phosphatase 1 (PP1), which dephosphorylates the key 'Ser-418' residue of FOXP3, thereby inactivating FOXP3 and rendering Treg cells functionally defective (PubMed:23396208). Key mediator of cell death in the anticancer action of BCG-stimulated neutrophils in combination with DIABLO/SMAC mimetic in the RT4v6 bladder cancer cell line (PubMed:22517918).The TNF intracellular domain (ICD) form induces IL12 production in dendritic cells.Receptor with high affinity for TNFSF2/TNF-alpha and approximately 5-fold lower affinity for homotrimeric TNFSF1/lymphotoxin-alpha. The TRAF1/TRAF2 complex recruits the apoptotic suppressors BIRC2 and BIRC3 to TNFRSF1B/TNFR2. This receptor mediates most of the metabolic effects of TNF-alpha. Isoform 2 blocks TNF-alpha-induced apoptosis, which suggests that it regulates TNF-alpha function by antagonizing its biological activity.High affinity receptor for the Fc region of immunoglobulins gamma. Functions in both innate and adaptive immune responses.Receptor for the Fc region of IgG. Binds complexed or aggregated IgG and also monomeric IgG. Mediates antibody-dependent cellular cytotoxicity (ADCC) and other antibody-dependent responses, such as phagocytosis.Binds to the Fc region of immunoglobulins gamma. Low affinity receptor. By binding to IgG it initiates cellular responses against pathogens and soluble antigens. Promotes phagocytosis of opsonized antigens.Receptor for the Fc region of complexed or aggregated immunoglobulins gamma. Low affinity receptor. Involved in a variety of effector and regulatory functions such as phagocytosis of immune complexes and modulation of antibody production by B-cells. Binding to this receptor results in down-modulation of previous state of cell activation triggered via antigen receptors on B-cells (BCR), T-cells (TCR) or via another Fc receptor. Isoform IIB1 fails to mediate endocytosis or phagocytosis. Isoform IIB2 does not trigger phagocytosis.Receptor for the Fc region of complexed immunoglobulins gamma. Low affinity receptor. Involved in a variety of effector and regulatory functions such as phagocytosis of immune complexes and modulation of antibody production by B-cells.Cytokine that in its homotrimeric form binds to TNFRSF1A/TNFR1, TNFRSF1B/TNFBR and TNFRSF14/HVEM. In its heterotrimeric form with LTB binds to TNFRSF3/LTBR. Lymphotoxin is produced by lymphocytes and cytotoxic for a wide range of tumor cells in vitro and in vivo.Receptor for the Fc region of immunoglobulins gamma. Low affinity receptor. Binds complexed or aggregated IgG and also monomeric IgG. Contrary to III-A, is not capable to mediate antibody-dependent cytotoxicity and phagocytosis. May serve as a trap for immune complexes in the peripheral circulation which does not activate neutrophils.C1s B chain is a serine protease that combines with C1q and C1r to form C1, the first component of the classical pathway of the complement system. C1r activates C1s so that it can, in turn, activate C2 and C4.C1r B chain is a serine protease that combines with C1q and C1s to form C1, the first component of the classical pathway of the complement system.C1q associates with the proenzymes C1r and C1s to yield C1, the first component of the serum complement system. The collagen-like regions of C1q interact with the Ca(2+)-dependent C1r(2)C1s(2) proenzyme complex, and efficient activation of C1 takes place on interaction of the globular heads of C1q with the Fc regions of IgG or IgM antibody present in immune complexes.C1q associates with the proenzymes C1r and C1s to yield C1, the first component of the serum complement system. The collagen-like regions of C1q interact with the Ca(2+)-dependent C1r(2)C1s(2) proenzyme complex, and efficient activation of C1 takes place on interaction of the globular heads of C1q with the Fc regions of IgG or IgM antibody present in immune complexes.C1q associates with the proenzymes C1r and C1s to yield C1, the first component of the serum complement system. The collagen-like regions of C1q interact with the Ca(2+)-dependent C1r(2)C1s(2) proenzyme complex, and efficient activation of C1 takes place on interaction of the globular heads of C1q with the Fc regions of IgG or IgM antibody present in immune complexes. 102 +/- 30 hrs in individuals with rheumatoid arthritis and 68 hours in healthy adults. Bioavailability following sub-Q administration is approximately 60%. Peak plasma concentrations achieved within 69 hours. * 160 +/- 80 mL/hr [RA patients] Etanercept binds specifically to tumor necrosis factor (TNF) and thereby modulates biological processes that are induced or regulated by TNF. Such processes or molecules affected include the level of adhesion molecules expressed, as well as serum levels of cytokines and matrix metalloproteinase-3, also known as stromelysin. In animal models, etanarcept has been demonstrated to affect inflammation, such as in murine collagen-induced arthritis. Sarilumab may increase the immunosuppressive activities of Etanercept.The therapeutic efficacy of Torasemide can be decreased when used in combination with Etanercept.The therapeutic efficacy of Furosemide can be decreased when used in combination with Etanercept.The therapeutic efficacy of Bumetanide can be decreased when used in combination with Etanercept.The therapeutic efficacy of Etacrynic acid can be decreased when used in combination with Etanercept.The therapeutic efficacy of Azosemide can be decreased when used in combination with Etanercept.The therapeutic efficacy of Piretanide can be decreased when used in combination with Etanercept.The serum concentration of Lithium can be increased when it is combined with Etanercept.The serum concentration of Methotrexate can be increased when it is combined with Etanercept.The risk or severity of adverse effects can be increased when Etanercept is combined with Tenofovir disoproxil.Sodium phosphate may increase the nephrotoxic activities of Etanercept.The risk or severity of bleeding can be increased when Betrixaban is combined with Etanercept.The risk or severity of adverse effects can be increased when Etanercept is combined with Leflunomide.Etanercept may increase the immunosuppressive activities of Fingolimod.Roflumilast may increase the immunosuppressive activities of Etanercept.Etanercept may increase the nephrotoxic activities of Cyclosporine.The therapeutic efficacy of Varicella Zoster Vaccine (Live/Attenuated) can be decreased when used in combination with Etanercept.The therapeutic efficacy of Yellow Fever Vaccine can be decreased when used in combination with Etanercept.The therapeutic efficacy of Clostridium tetani toxoid antigen (formaldehyde inactivated) can be decreased when used in combination with Etanercept.The therapeutic efficacy of Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated) can be decreased when used in combination with Etanercept.The therapeutic efficacy of Rotavirus Vaccine can be decreased when used in combination with Etanercept.The therapeutic efficacy of G17DT can be decreased when used in combination with Etanercept.The therapeutic efficacy of INGN 201 can be decreased when used in combination with Etanercept.The therapeutic efficacy of INGN 225 can be decreased when used in combination with Etanercept.The therapeutic efficacy of Rindopepimut can be decreased when used in combination with Etanercept.The therapeutic efficacy of SRP 299 can be decreased when used in combination with Etanercept.The therapeutic efficacy of GI-5005 can be decreased when used in combination with Etanercept.The therapeutic efficacy of TG4010 can be decreased when used in combination with Etanercept.The therapeutic efficacy of Rabies virus inactivated antigen, A can be decreased when used in combination with Etanercept.The therapeutic efficacy of Tecemotide can be decreased when used in combination with Etanercept.The therapeutic efficacy of Rubella virus vaccine can be decreased when used in combination with Etanercept.The therapeutic efficacy of Anthrax immune globulin human can be decreased when used in combination with Etanercept.The therapeutic efficacy of Bacillus calmette-guerin substrain tice live antigen can be decreased when used in combination with Etanercept.The therapeutic efficacy of Japanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated) can be decreased when used in combination with Etanercept.The therapeutic efficacy of Salmonella typhi ty2 vi polysaccharide antigen can be decreased when used in combination with Etanercept.The therapeutic efficacy of Bacillus calmette-guerin substrain connaught live antigen can be decreased when used in combination with Etanercept.The therapeutic efficacy of Hepatitis A Vaccine can be decreased when used in combination with Etanercept.The therapeutic efficacy of Salmonella typhi ty21a live antigen can be decreased when used in combination with Etanercept.The therapeutic efficacy of Human rabies virus immune globulin can be decreased when used in combination with Etanercept.The therapeutic efficacy of Hepatitis B Vaccine (Recombinant) can be decreased when used in combination with Etanercept.The risk or severity of adverse effects can be increased when Diclofenac is combined with Etanercept.Ocrelizumab may increase the immunosuppressive activities of Etanercept.Colestipol can cause a decrease in the absorption of Etanercept resulting in a reduced serum concentration and potentially a decrease in efficacy.Colesevelam can cause a decrease in the absorption of Etanercept resulting in a reduced serum concentration and potentially a decrease in efficacy.Cholestyramine can cause a decrease in the absorption of Etanercept resulting in a reduced serum concentration and potentially a decrease in efficacy.Etanercept may decrease the excretion rate of Amikacin which could result in a higher serum level.Etanercept may decrease the excretion rate of Tobramycin which could result in a higher serum level.Etanercept may decrease the excretion rate of Gentamicin which could result in a higher serum level.Etanercept may decrease the excretion rate of Neomycin which could result in a higher serum level.Etanercept may decrease the excretion rate of Streptomycin which could result in a higher serum level.Etanercept may decrease the excretion rate of Valrubicin which could result in a higher serum level.Etanercept may decrease the excretion rate of Streptozocin which could result in a higher serum level.Etanercept may decrease the excretion rate of Epirubicin which could result in a higher serum level.Etanercept may decrease the excretion rate of Framycetin which could result in a higher serum level.Etanercept may decrease the excretion rate of Daunorubicin which could result in a higher serum level.Etanercept may decrease the excretion rate of Spectinomycin which could result in a higher serum level.Etanercept may decrease the excretion rate of Netilmicin which could result in a higher serum level.Etanercept may decrease the excretion rate of Doxorubicin which could result in a higher serum level.Etanercept may decrease the excretion rate of Kanamycin which could result in a higher serum level.Etanercept may decrease the excretion rate of Idarubicin which could result in a higher serum level.Etanercept may decrease the excretion rate of Paromomycin which could result in a higher serum level.Etanercept may decrease the excretion rate of Metrizamide which could result in a higher serum level.Etanercept may decrease the excretion rate of Ribostamycin which could result in a higher serum level.Etanercept may decrease the excretion rate of Geneticin which could result in a higher serum level.Etanercept may decrease the excretion rate of Apramycin which could result in a higher serum level.Etanercept may decrease the excretion rate of GENTAMICIN C1A which could result in a higher serum level.Etanercept may decrease the excretion rate of Neamine which could result in a higher serum level.Etanercept may decrease the excretion rate of SP1049C which could result in a higher serum level.Etanercept may decrease the excretion rate of Aldoxorubicin which could result in a higher serum level.Etanercept may decrease the excretion rate of Amrubicin which could result in a higher serum level.Etanercept may decrease the excretion rate of Annamycin which could result in a higher serum level.Etanercept may decrease the excretion rate of Arbekacin which could result in a higher serum level.Etanercept may decrease the excretion rate of Plicamycin which could result in a higher serum level.Etanercept may decrease the excretion rate of Puromycin which could result in a higher serum level.Etanercept may decrease the excretion rate of Dihydrostreptomycin which could result in a higher serum level.Etanercept may decrease the excretion rate of Hygromycin B which could result in a higher serum level.Etanercept may decrease the excretion rate of Pirarubicin which could result in a higher serum level.Etanercept may decrease the excretion rate of Aclarubicin which could result in a higher serum level.Etanercept may decrease the excretion rate of Zorubicin which could result in a higher serum level.Etanercept may decrease the excretion rate of Sabarubicin which could result in a higher serum level.Etanercept may decrease the excretion rate of Sisomicin which could result in a higher serum level.Etanercept may decrease the excretion rate of Plazomicin which could result in a higher serum level.Etanercept may decrease the excretion rate of Zoptarelin doxorubicin which could result in a higher serum level.Etanercept may decrease the excretion rate of GPX-150 which could result in a higher serum level.Etanercept may decrease the excretion rate of Dibekacin which could result in a higher serum level.Etanercept may decrease the excretion rate of Micronomicin which could result in a higher serum level.Etanercept may decrease the excretion rate of Isepamicin which could result in a higher serum level.Etanercept may decrease the excretion rate of Bekanamycin which could result in a higher serum level.Etanercept may decrease the antihypertensive activities of Aliskiren.The risk or severity of adverse effects can be increased when Etanercept is combined with Deferasirox.The risk or severity of adverse effects can be increased when Etanercept is combined with Desmopressin.Etanercept may increase the neuroexcitatory activities of Grepafloxacin.Etanercept may increase the neuroexcitatory activities of Enoxacin.Etanercept may increase the neuroexcitatory activities of Pefloxacin.Etanercept may increase the neuroexcitatory activities of Trovafloxacin.Etanercept may increase the neuroexcitatory activities of Nalidixic Acid.Etanercept may increase the neuroexcitatory activities of Rosoxacin.Etanercept may increase the neuroexcitatory activities of Cinoxacin.Etanercept may increase the neuroexcitatory activities of Gatifloxacin.Etanercept may increase the neuroexcitatory activities of Norfloxacin.Etanercept may increase the neuroexcitatory activities of Levofloxacin.Etanercept may increase the neuroexcitatory activities of Gemifloxacin.Etanercept may increase the neuroexcitatory activities of Sparfloxacin.Etanercept may increase the neuroexcitatory activities of Temafloxacin.Etanercept may increase the neuroexcitatory activities of Fleroxacin.Etanercept may increase the neuroexcitatory activities of Garenoxacin.Etanercept may increase the neuroexcitatory activities of Nemonoxacin.Etanercept may increase the neuroexcitatory activities of Flumequine.Etanercept may increase the neuroexcitatory activities of Pazufloxacin.Etanercept may increase the neuroexcitatory activities of Prulifloxacin.Etanercept may increase the neuroexcitatory activities of Sitafloxacin.Etanercept may increase the neuroexcitatory activities of Oxolinic acid.Etanercept may increase the neuroexcitatory activities of Piromidic acid.Etanercept may increase the neuroexcitatory activities of Rufloxacin.Etanercept may increase the neuroexcitatory activities of Pipemidic acid.The serum concentration of Digoxin can be increased when it is combined with Etanercept.Etanercept may increase the hyperkalemic activities of Drospirenone.Etanercept may decrease the antihypertensive activities of Eplerenone.The risk or severity of adverse effects can be increased when Etanercept is combined with Haloperidol.Etanercept may decrease the antihypertensive activities of Hydralazine.The serum concentration of Pralatrexate can be increased when it is combined with Etanercept.The serum concentration of Etanercept can be increased when it is combined with Probenecid.The risk or severity of adverse effects can be increased when Treprostinil is combined with Etanercept.The serum concentration of Vancomycin can be increased when it is combined with Etanercept.The therapeutic efficacy of Methyclothiazide can be decreased when used in combination with Etanercept.The therapeutic efficacy of Chlorothiazide can be decreased when used in combination with Etanercept.The therapeutic efficacy of Hydrochlorothiazide can be decreased when used in combination with Etanercept.The therapeutic efficacy of Epitizide can be decreased when used in combination with Etanercept.The therapeutic efficacy of Chlorthalidone can be decreased when used in combination with Etanercept.The therapeutic efficacy of Bendroflumethiazide can be decreased when used in combination with Etanercept.The therapeutic efficacy of Metolazone can be decreased when used in combination with Etanercept.The therapeutic efficacy of Hydroflumethiazide can be decreased when used in combination with Etanercept.The therapeutic efficacy of Indapamide can be decreased when used in combination with Etanercept.The therapeutic efficacy of Trichlormethiazide can be decreased when used in combination with Etanercept.The therapeutic efficacy of Polythiazide can be decreased when used in combination with Etanercept.The therapeutic efficacy of Quinethazone can be decreased when used in combination with Etanercept.The therapeutic efficacy of Cyclopenthiazide can be decreased when used in combination with Etanercept.Etanercept may increase the nephrotoxic activities of Mesalazine.Etanercept may increase the nephrotoxic activities of Balsalazide.Etanercept may increase the nephrotoxic activities of Olsalazine.The risk or severity of adverse effects can be increased when Denosumab is combined with Etanercept.The therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Etanercept.Trastuzumab may increase the neutropenic activities of Etanercept.The risk or severity of adverse effects can be increased when Etanercept is combined with Risedronate.The risk or severity of adverse effects can be increased when Etanercept is combined with Etidronic acid.The risk or severity of adverse effects can be increased when Etanercept is combined with Clodronic Acid.The risk or severity of adverse effects can be increased when Etanercept is combined with Pamidronate.The risk or severity of adverse effects can be increased when Etanercept is combined with Zoledronic acid.The risk or severity of adverse effects can be increased when Etanercept is combined with Ibandronate.The risk or severity of adverse effects can be increased when Etanercept is combined with Alendronic acid.The risk or severity of adverse effects can be increased when Etanercept is combined with Technetium Tc-99m medronate.The risk or severity of adverse effects can be increased when Etanercept is combined with Technetium Tc-99m etidronate.The risk or severity of adverse effects can be increased when Etanercept is combined with Tiludronic acid.The therapeutic efficacy of Carboprost Tromethamine can be decreased when used in combination with Etanercept.The therapeutic efficacy of Dinoprostone can be decreased when used in combination with Etanercept.The therapeutic efficacy of Misoprostol can be decreased when used in combination with Etanercept.The therapeutic efficacy of Gemeprost can be decreased when used in combination with Etanercept.The therapeutic efficacy of Dinoprost can be decreased when used in combination with Etanercept.The therapeutic efficacy of Sulprostone can be decreased when used in combination with Etanercept.The therapeutic efficacy of Enprostil can be decreased when used in combination with Etanercept.The therapeutic efficacy of Folic Acid can be decreased when used in combination with Etanercept.The therapeutic efficacy of Travoprost can be decreased when used in combination with Etanercept.The therapeutic efficacy of Latanoprost can be decreased when used in combination with Etanercept.The therapeutic efficacy of Alprostadil can be decreased when used in combination with Etanercept.The therapeutic efficacy of Bimatoprost can be decreased when used in combination with Etanercept.The therapeutic efficacy of Lubiprostone can be decreased when used in combination with Etanercept.The therapeutic efficacy of Iloprost can be decreased when used in combination with Etanercept.The therapeutic efficacy of Dinoprost Tromethamine can be decreased when used in combination with Etanercept.The therapeutic efficacy of Epoprostenol can be decreased when used in combination with Etanercept.The therapeutic efficacy of Prostaglandin B2 can be decreased when used in combination with Etanercept.The therapeutic efficacy of Prostaglandin G2 can be decreased when used in combination with Etanercept.The therapeutic efficacy of Beraprost can be decreased when used in combination with Etanercept.The therapeutic efficacy of Unoprostone can be decreased when used in combination with Etanercept.The therapeutic efficacy of Tafluprost can be decreased when used in combination with Etanercept.The therapeutic efficacy of Limaprost can be decreased when used in combination with Etanercept.The therapeutic efficacy of Fenprostalene can be decreased when used in combination with Etanercept.The therapeutic efficacy of Luprostiol can be decreased when used in combination with Etanercept.The therapeutic efficacy of Prostalene can be decreased when used in combination with Etanercept.The therapeutic efficacy of Cloprostenol can be decreased when used in combination with Etanercept.The therapeutic efficacy of Fluprostenol can be decreased when used in combination with Etanercept.The therapeutic efficacy of Latanoprostene Bunod can be decreased when used in combination with Etanercept.Etanercept may increase the anticoagulant activities of Lepirudin.Etanercept may increase the anticoagulant activities of Bivalirudin.Etanercept may increase the anticoagulant activities of Abciximab.Etanercept may increase the anticoagulant activities of Becaplermin.Etanercept may increase the anticoagulant activities of Dicoumarol.Etanercept may increase the anticoagulant activities of Argatroban.Etanercept may increase the anticoagulant activities of Ardeparin.Etanercept may increase the anticoagulant activities of Phenindione.Etanercept may increase the anticoagulant activities of Fondaparinux sodium.Etanercept may increase the anticoagulant activities of Warfarin.Etanercept may increase the anticoagulant activities of Pentosan Polysulfate.Etanercept may increase the anticoagulant activities of Phenprocoumon.Etanercept may increase the anticoagulant activities of Edetic Acid.Etanercept may increase the anticoagulant activities of Heparin.Etanercept may increase the anticoagulant activities of Enoxaparin.Etanercept may increase the anticoagulant activities of Acenocoumarol.Etanercept may increase the anticoagulant activities of Citric Acid.Etanercept may increase the anticoagulant activities of Ximelagatran.Etanercept may increase the anticoagulant activities of Ancrod.Etanercept may increase the anticoagulant activities of Pentaerythritol Tetranitrate.Etanercept may increase the anticoagulant activities of Rivaroxaban.Etanercept may increase the anticoagulant activities of Sulodexide.Etanercept may increase the anticoagulant activities of Idraparinux.Etanercept may increase the anticoagulant activities of Apixaban.Etanercept may increase the anticoagulant activities of Otamixaban.Etanercept may increase the anticoagulant activities of Dabigatran etexilate.Etanercept may increase the anticoagulant activities of Danaparoid.Etanercept may increase the anticoagulant activities of Dalteparin.Etanercept may increase the anticoagulant activities of Ferulic acid.Etanercept may increase the anticoagulant activities of Ethyl biscoumacetate.Etanercept may increase the anticoagulant activities of Nadroparin.Etanercept may increase the anticoagulant activities of Edoxaban.Etanercept may increase the anticoagulant activities of Dextran.Etanercept may increase the anticoagulant activities of Reviparin.Etanercept may increase the anticoagulant activities of Certoparin.Etanercept may increase the anticoagulant activities of Dextran 70.Etanercept may increase the anticoagulant activities of Desirudin.Etanercept may increase the anticoagulant activities of Dextran 40.Etanercept may increase the anticoagulant activities of Dextran 75.Etanercept may increase the anticoagulant activities of Protocatechualdehyde.Etanercept may increase the anticoagulant activities of Protein C.Etanercept may increase the anticoagulant activities of Antithrombin III human.Etanercept may increase the anticoagulant activities of Fondaparinux.Etanercept may increase the anticoagulant activities of Letaxaban.Etanercept may increase the anticoagulant activities of Darexaban.Etanercept may increase the anticoagulant activities of Nafamostat.Etanercept may increase the anticoagulant activities of Gabexate.Etanercept may increase the anticoagulant activities of Troxerutin.Etanercept may increase the anticoagulant activities of Fluindione.Etanercept may increase the anticoagulant activities of Protein S human.Etanercept may increase the anticoagulant activities of Melagatran.The risk or severity of adverse effects can be increased when Etanercept is combined with Fluorometholone.The risk or severity of adverse effects can be increased when Etanercept is combined with Beclomethasone dipropionate.The risk or severity of adverse effects can be increased when Etanercept is combined with Betamethasone.The risk or severity of adverse effects can be increased when Etanercept is combined with Triamcinolone.The risk or severity of adverse effects can be increased when Etanercept is combined with Hydrocortisone.The risk or severity of adverse effects can be increased when Etanercept is combined with Prednisolone.The risk or severity of adverse effects can be increased when Etanercept is combined with Fluocinonide.The risk or severity of adverse effects can be increased when Etanercept is combined with Budesonide.The risk or severity of adverse effects can be increased when Etanercept is combined with Dexamethasone.The risk or severity of adverse effects can be increased when Etanercept is combined with Ciclesonide.The risk or severity of adverse effects can be increased when Etanercept is combined with Tixocortol.The risk or severity of adverse effects can be increased when Etanercept is combined with Fluocinolone Acetonide.The risk or severity of adverse effects can be increased when Etanercept is combined with Diflorasone.The risk or severity of adverse effects can be increased when Etanercept is combined with Alclometasone.The risk or severity of adverse effects can be increased when Etanercept is combined with Amcinonide.The risk or severity of adverse effects can be increased when Etanercept is combined with Desoximetasone.The risk or severity of adverse effects can be increased when Etanercept is combined with Clocortolone.The risk or severity of adverse effects can be increased when Etanercept is combined with Flurandrenolide.The risk or severity of adverse effects can be increased when Etanercept is combined with Rimexolone.The risk or severity of adverse effects can be increased when Etanercept is combined with Methylprednisolone.The risk or severity of adverse effects can be increased when Etanercept is combined with Clobetasol propionate.The risk or severity of adverse effects can be increased when Etanercept is combined with Prednicarbate.The risk or severity of adverse effects can be increased when Etanercept is combined with Cortisone acetate.The risk or severity of adverse effects can be increased when Etanercept is combined with Flunisolide.The risk or severity of adverse effects can be increased when Etanercept is combined with Fluticasone propionate.The risk or severity of adverse effects can be increased when Etanercept is combined with Mometasone.The risk or severity of adverse effects can be increased when Etanercept is combined with Loteprednol.The risk or severity of adverse effects can be increased when Etanercept is combined with Fluticasone furoate.The risk or severity of adverse effects can be increased when Etanercept is combined with Difluprednate.The risk or severity of adverse effects can be increased when Etanercept is combined with Medrysone.The risk or severity of adverse effects can be increased when Etanercept is combined with Prednisone.The risk or severity of adverse effects can be increased when Etanercept is combined with Estrone.The risk or severity of adverse effects can be increased when Etanercept is combined with Flumethasone.The risk or severity of adverse effects can be increased when Etanercept is combined with Fludrocortisone.The risk or severity of adverse effects can be increased when Etanercept is combined with Desoxycorticosterone Pivalate.The risk or severity of adverse effects can be increased when Etanercept is combined with Paramethasone.The risk or severity of adverse effects can be increased when Etanercept is combined with 19-norandrostenedione.The risk or severity of adverse effects can be increased when Etanercept is combined with 5-androstenedione.The risk or severity of adverse effects can be increased when Etanercept is combined with Androstenedione.The risk or severity of adverse effects can be increased when Etanercept is combined with Prasterone.The risk or severity of adverse effects can be increased when Etanercept is combined with Equilin.The risk or severity of adverse effects can be increased when Etanercept is combined with Pregnenolone.The risk or severity of adverse effects can be increased when Etanercept is combined with Equilenin.The risk or severity of adverse effects can be increased when Etanercept is combined with Estrone sulfate.The risk or severity of adverse effects can be increased when Etanercept is combined with Aldosterone.The risk or severity of adverse effects can be increased when Etanercept is combined with Corticosterone.The risk or severity of adverse effects can be increased when Etanercept is combined with Oleoyl-estrone.The risk or severity of adverse effects can be increased when Etanercept is combined with 16-Bromoepiandrosterone.The risk or severity of adverse effects can be increased when Etanercept is combined with HE3286.The risk or severity of adverse effects can be increased when Etanercept is combined with anecortave acetate.The risk or severity of adverse effects can be increased when Etanercept is combined with ME-609.The risk or severity of adverse effects can be increased when Etanercept is combined with NCX 1022.The risk or severity of adverse effects can be increased when Etanercept is combined with Prasterone sulfate.The risk or severity of adverse effects can be increased when Etanercept is combined with Istaroxime.The risk or severity of adverse effects can be increased when Etanercept is combined with Fluasterone.The risk or severity of adverse effects can be increased when Etanercept is combined with Desoxycorticosterone acetate.The risk or severity of adverse effects can be increased when Etanercept is combined with Formestane.The risk or severity of adverse effects can be increased when Etanercept is combined with Fluprednidene.The risk or severity of adverse effects can be increased when Etanercept is combined with Fluocortolone.The risk or severity of adverse effects can be increased when Etanercept is combined with Difluocortolone.The risk or severity of adverse effects can be increased when Etanercept is combined with Fluprednisolone.The risk or severity of adverse effects can be increased when Etanercept is combined with Dexamethasone isonicotinate.The risk or severity of adverse effects can be increased when Etanercept is combined with Melengestrol.The risk or severity of adverse effects can be increased when Etanercept is combined with Clobetasol.The risk or severity of adverse effects can be increased when Etanercept is combined with Anecortave.The risk or severity of adverse effects can be increased when Etanercept is combined with Atamestane.The risk or severity of adverse effects can be increased when Etanercept is combined with Cortexolone 17α-propionate.The risk or severity of adverse effects can be increased when Etanercept is combined with Clobetasone.The risk or severity of adverse effects can be increased when Etanercept is combined with Ulobetasol.The risk or severity of adverse effects can be increased when Etanercept is combined with Desonide.The risk or severity of adverse effects can be increased when Etanercept is combined with Halcinonide.The risk or severity of adverse effects can be increased when Etanercept is combined with Deflazacort.The risk or severity of adverse effects can be increased when Flurbiprofen is combined with Etanercept.The risk or severity of adverse effects can be increased when Bromfenac is combined with Etanercept.The risk or severity of adverse effects can be increased when Nepafenac is combined with Etanercept.The risk or severity of adverse effects can be increased when Etanercept is combined with Masoprocol.The risk or severity of adverse effects can be increased when Etanercept is combined with Adapalene.The risk or severity of adverse effects can be increased when Etanercept is combined with Indomethacin.The risk or severity of adverse effects can be increased when Etanercept is combined with Nabumetone.The risk or severity of adverse effects can be increased when Etanercept is combined with Tenoxicam.The risk or severity of adverse effects can be increased when Etanercept is combined with Celecoxib.The risk or severity of adverse effects can be increased when Etanercept is combined with Tolmetin.The risk or severity of adverse effects can be increased when Etanercept is combined with Rofecoxib.The risk or severity of adverse effects can be increased when Etanercept is combined with Piroxicam.The risk or severity of adverse effects can be increased when Etanercept is combined with Fenoprofen.The risk or severity of adverse effects can be increased when Etanercept is combined with Valdecoxib.The risk or severity of adverse effects can be increased when Etanercept is combined with Sulindac.The risk or severity of adverse effects can be increased when Etanercept is combined with Chloroquine.The risk or severity of adverse effects can be increased when Etanercept is combined with Mycophenolate mofetil.The risk or severity of adverse effects can be increased when Etanercept is combined with Naftifine.The risk or severity of adverse effects can be increased when Etanercept is combined with Zileuton.The risk or severity of adverse effects can be increased when Etanercept is combined with Etodolac.The risk or severity of adverse effects can be increased when Etanercept is combined with Olopatadine.The risk or severity of adverse effects can be increased when Etanercept is combined with Mefenamic acid.The risk or severity of adverse effects can be increased when Etanercept is combined with Naproxen.The risk or severity of adverse effects can be increased when Etanercept is combined with Sulfasalazine.The risk or severity of adverse effects can be increased when Etanercept is combined with Phenylbutazone.The risk or severity of adverse effects can be increased when Etanercept is combined with Meloxicam.The risk or severity of adverse effects can be increased when Etanercept is combined with Carprofen.The risk or severity of adverse effects can be increased when Etanercept is combined with Diflunisal.The risk or severity of adverse effects can be increased when Etanercept is combined with Suprofen.The risk or severity of adverse effects can be increased when Etanercept is combined with Salicylic acid.The risk or severity of adverse effects can be increased when Etanercept is combined with Meclofenamic acid.The risk or severity of adverse effects can be increased when Etanercept is combined with Acetylsalicylic acid.The risk or severity of adverse effects can be increased when Etanercept is combined with Azelastine.The risk or severity of adverse effects can be increased when Etanercept is combined with Oxaprozin.The risk or severity of adverse effects can be increased when Etanercept is combined with Ketoprofen.The risk or severity of adverse effects can be increased when Etanercept is combined with Mycophenolic acid.The risk or severity of adverse effects can be increased when Etanercept is combined with Ibuprofen.The risk or severity of adverse effects can be increased when Etanercept is combined with Lumiracoxib.The risk or severity of adverse effects can be increased when Etanercept is combined with Magnesium salicylate.The risk or severity of adverse effects can be increased when Etanercept is combined with Salsalate.The risk or severity of adverse effects can be increased when Etanercept is combined with Choline magnesium trisalicylate.The risk or severity of adverse effects can be increased when Etanercept is combined with Antipyrine.The risk or severity of adverse effects can be increased when Etanercept is combined with Tiaprofenic acid.The risk or severity of adverse effects can be increased when Etanercept is combined with Etoricoxib.The risk or severity of adverse effects can be increased when Etanercept is combined with Castanospermine.The risk or severity of adverse effects can be increased when Etanercept is combined with Resveratrol.The risk or severity of adverse effects can be increased when Etanercept is combined with Oxyphenbutazone.The risk or severity of adverse effects can be increased when Etanercept is combined with Niflumic Acid.The risk or severity of adverse effects can be increased when Etanercept is combined with Nimesulide.The risk or severity of adverse effects can be increased when Etanercept is combined with Benoxaprofen.The risk or severity of adverse effects can be increased when Etanercept is combined with Metamizole.The risk or severity of adverse effects can be increased when Etanercept is combined with Zomepirac.The risk or severity of adverse effects can be increased when Etanercept is combined with Pirfenidone.The risk or severity of adverse effects can be increased when Etanercept is combined with SRT501.The risk or severity of adverse effects can be increased when Etanercept is combined with PTC299.The risk or severity of adverse effects can be increased when Etanercept is combined with Tarenflurbil.The risk or severity of adverse effects can be increased when Etanercept is combined with Apremilast.The risk or severity of adverse effects can be increased when Etanercept is combined with Andrographolide.The risk or severity of adverse effects can be increased when Etanercept is combined with Icatibant.The risk or severity of adverse effects can be increased when Etanercept is combined with Exisulind.The risk or severity of adverse effects can be increased when Etanercept is combined with Lornoxicam.The risk or severity of adverse effects can be increased when Etanercept is combined with Aceclofenac.The risk or severity of adverse effects can be increased when Etanercept is combined with Zaltoprofen.The risk or severity of adverse effects can be increased when Etanercept is combined with Seratrodast.The risk or severity of adverse effects can be increased when Etanercept is combined with Azapropazone.The risk or severity of adverse effects can be increased when Etanercept is combined with Felbinac.The risk or severity of adverse effects can be increased when Etanercept is combined with Tranilast.The risk or severity of adverse effects can be increased when Etanercept is combined with Parecoxib.The risk or severity of adverse effects can be increased when Etanercept is combined with Salicylamide.The risk or severity of adverse effects can be increased when Etanercept is combined with Teriflunomide.The risk or severity of adverse effects can be increased when Etanercept is combined with (4R)-limonene.The risk or severity of adverse effects can be increased when Etanercept is combined with Kebuzone.The risk or severity of adverse effects can be increased when Etanercept is combined with Isoxicam.The risk or severity of adverse effects can be increased when Etanercept is combined with Indoprofen.The risk or severity of adverse effects can be increased when Etanercept is combined with Ibuproxam.The risk or severity of adverse effects can be increased when Etanercept is combined with Fenbufen.The risk or severity of adverse effects can be increased when Etanercept is combined with Etofenamate.The risk or severity of adverse effects can be increased when Etanercept is combined with Epirizole.The risk or severity of adverse effects can be increased when Etanercept is combined with Loxoprofen.The risk or severity of adverse effects can be increased when Etanercept is combined with Droxicam.The risk or severity of adverse effects can be increased when Etanercept is combined with Tolfenamic Acid.The risk or severity of adverse effects can be increased when Etanercept is combined with Clonixin.The risk or severity of adverse effects can be increased when Etanercept is combined with Propacetamol.The risk or severity of adverse effects can be increased when Etanercept is combined with Evening primrose oil.The risk or severity of adverse effects can be increased when Etanercept is combined with Orgotein.The risk or severity of adverse effects can be increased when Etanercept is combined with Tepoxalin.The risk or severity of adverse effects can be increased when Etanercept is combined with Flunixin.The risk or severity of adverse effects can be increased when Etanercept is combined with Curcumin.The risk or severity of adverse effects can be increased when Etanercept is combined with E-6201.The risk or severity of adverse effects can be increased when Etanercept is combined with Anisodamine.The risk or severity of adverse effects can be increased when Etanercept is combined with Duvelisib.The risk or severity of adverse effects can be increased when Etanercept is combined with Triptolide.The risk or severity of adverse effects can be increased when Etanercept is combined with Semapimod.The risk or severity of adverse effects can be increased when Etanercept is combined with Bucillamine.The risk or severity of adverse effects can be increased when Etanercept is combined with Lisofylline.The risk or severity of adverse effects can be increased when Etanercept is combined with Nitroaspirin.The risk or severity of adverse effects can be increased when Etanercept is combined with Indobufen.The risk or severity of adverse effects can be increased when Etanercept is combined with Mizoribine.The risk or severity of adverse effects can be increased when Etanercept is combined with Apocynin.The risk or severity of adverse effects can be increased when Etanercept is combined with Higenamine.The risk or severity of adverse effects can be increased when Etanercept is combined with Tinoridine.The risk or severity of adverse effects can be increased when Etanercept is combined with Parthenolide.The risk or severity of adverse effects can be increased when Etanercept is combined with Serrapeptase.The risk or severity of adverse effects can be increased when Etanercept is combined with Alclofenac.The risk or severity of adverse effects can be increased when Etanercept is combined with Fentiazac.The risk or severity of adverse effects can be increased when Etanercept is combined with Tribenoside.The risk or severity of adverse effects can be increased when Etanercept is combined with Suxibuzone.The risk or severity of adverse effects can be increased when Etanercept is combined with Bumadizone.The risk or severity of adverse effects can be increased when Etanercept is combined with Alminoprofen.The risk or severity of adverse effects can be increased when Etanercept is combined with Flunoxaprofen.The risk or severity of adverse effects can be increased when Etanercept is combined with Bufexamac.The risk or severity of adverse effects can be increased when Etanercept is combined with Feprazone.The risk or severity of adverse effects can be increased when Etanercept is combined with Difenpiramide.The risk or severity of adverse effects can be increased when Etanercept is combined with Nifenazone.The risk or severity of adverse effects can be increased when Etanercept is combined with Lonazolac.The risk or severity of adverse effects can be increased when Etanercept is combined with Tenidap.The risk or severity of adverse effects can be increased when Etanercept is combined with Bendazac.The risk or severity of adverse effects can be increased when Etanercept is combined with Pranoprofen.The risk or severity of adverse effects can be increased when Etanercept is combined with Propyphenazone.The risk or severity of adverse effects can be increased when Etanercept is combined with Proglumetacin.The risk or severity of adverse effects can be increased when Etanercept is combined with Guacetisal.The risk or severity of adverse effects can be increased when Etanercept is combined with Bevonium.The risk or severity of adverse effects can be increased when Etanercept is combined with Ethenzamide.The risk or severity of adverse effects can be increased when Etanercept is combined with Carbaspirin calcium.The risk or severity of adverse effects can be increased when Etanercept is combined with Mofebutazone.The risk or severity of adverse effects can be increased when Etanercept is combined with Proquazone.The risk or severity of adverse effects can be increased when Etanercept is combined with Benorilate.The risk or severity of adverse effects can be increased when Etanercept is combined with Pirprofen.The risk or severity of adverse effects can be increased when Etanercept is combined with Imidazole salicylate.The risk or severity of adverse effects can be increased when Etanercept is combined with Benzydamine.Etanercept may increase the nephrotoxic activities of Tacrolimus.The risk or severity of adverse effects can be increased when Valsartan is combined with Etanercept.The risk or severity of adverse effects can be increased when Olmesartan is combined with Etanercept.The risk or severity of adverse effects can be increased when Losartan is combined with Etanercept.The risk or severity of adverse effects can be increased when Candesartan cilexetil is combined with Etanercept.The risk or severity of adverse effects can be increased when Eprosartan is combined with Etanercept.The risk or severity of adverse effects can be increased when Telmisartan is combined with Etanercept.The risk or severity of adverse effects can be increased when Irbesartan is combined with Etanercept.The risk or severity of adverse effects can be increased when Saprisartan is combined with Etanercept.The risk or severity of adverse effects can be increased when Tasosartan is combined with Etanercept.The risk or severity of adverse effects can be increased when Azilsartan medoxomil is combined with Etanercept.The risk or severity of adverse effects can be increased when Candesartan is combined with Etanercept.The risk or severity of adverse effects can be increased when Saralasin is combined with Etanercept.The risk or severity of adverse effects can be increased when Sacubitril is combined with Etanercept.The risk or severity of adverse effects can be increased when Forasartan is combined with Etanercept.The risk or severity of adverse effects can be increased when Fimasartan is combined with Etanercept.The risk or severity of adverse effects can be increased when Etanercept is combined with Ramipril.The risk or severity of adverse effects can be increased when Etanercept is combined with Fosinopril.The risk or severity of adverse effects can be increased when Etanercept is combined with Trandolapril.The risk or severity of adverse effects can be increased when Etanercept is combined with Benazepril.The risk or severity of adverse effects can be increased when Etanercept is combined with Enalapril.The risk or severity of adverse effects can be increased when Etanercept is combined with Moexipril.The risk or severity of adverse effects can be increased when Etanercept is combined with Lisinopril.The risk or severity of adverse effects can be increased when Etanercept is combined with Perindopril.The risk or severity of adverse effects can be increased when Etanercept is combined with Quinapril.The risk or severity of adverse effects can be increased when Etanercept is combined with Captopril.The risk or severity of adverse effects can be increased when Etanercept is combined with Cilazapril.The risk or severity of adverse effects can be increased when Etanercept is combined with Spirapril.The risk or severity of adverse effects can be increased when Etanercept is combined with Enalaprilat.The risk or severity of adverse effects can be increased when Etanercept is combined with Temocapril.The risk or severity of adverse effects can be increased when Etanercept is combined with Zofenopril.The risk or severity of adverse effects can be increased when Etanercept is combined with Omapatrilat.The risk or severity of adverse effects can be increased when Etanercept is combined with Imidapril.The risk or severity of adverse effects can be increased when Etanercept is combined with Delapril.The risk or severity of adverse effects can be increased when Etanercept is combined with Rescinnamine.The risk or severity of adverse effects can be increased when Etanercept is combined with Candoxatril.The risk or severity of adverse effects can be increased when Etanercept is combined with Azficel-T.Etanercept may decrease the antihypertensive activities of Triamterene.Etanercept may decrease the antihypertensive activities of Amiloride.Etanercept may decrease the antihypertensive activities of Spironolactone.Etanercept may decrease the antihypertensive activities of Esmolol.Etanercept may decrease the antihypertensive activities of Betaxolol.Etanercept may decrease the antihypertensive activities of Metoprolol.Etanercept may decrease the antihypertensive activities of Atenolol.Etanercept may decrease the antihypertensive activities of Timolol.Etanercept may decrease the antihypertensive activities of Carteolol.Etanercept may decrease the antihypertensive activities of Propranolol.Etanercept may decrease the antihypertensive activities of Labetalol.Etanercept may decrease the antihypertensive activities of Bisoprolol.Etanercept may decrease the antihypertensive activities of Pindolol.Etanercept may decrease the antihypertensive activities of Carvedilol.Etanercept may decrease the antihypertensive activities of Acebutolol.Etanercept may decrease the antihypertensive activities of Nadolol.Etanercept may decrease the antihypertensive activities of Levobunolol.Etanercept may decrease the antihypertensive activities of Metipranolol.Etanercept may decrease the antihypertensive activities of Sotalol.Etanercept may decrease the antihypertensive activities of Nebivolol.Etanercept may decrease the antihypertensive activities of Alprenolol.Etanercept may decrease the antihypertensive activities of Bevantolol.Etanercept may decrease the antihypertensive activities of Practolol.Etanercept may decrease the antihypertensive activities of Penbutolol.Etanercept may decrease the antihypertensive activities of Oxprenolol.Etanercept may decrease the antihypertensive activities of Platelet Activating Factor.Etanercept may decrease the antihypertensive activities of Celiprolol.Etanercept may decrease the antihypertensive activities of Bufuralol.Etanercept may decrease the antihypertensive activities of Bopindolol.Etanercept may decrease the antihypertensive activities of Bupranolol.Etanercept may decrease the antihypertensive activities of Indenolol.Etanercept may decrease the antihypertensive activities of Befunolol.Etanercept may decrease the antihypertensive activities of Arotinolol.Etanercept may decrease the antihypertensive activities of Talinolol.Etanercept may decrease the antihypertensive activities of Landiolol.Etanercept may decrease the antihypertensive activities of Bucindolol.Etanercept may decrease the antihypertensive activities of Cloranolol.Etanercept may decrease the antihypertensive activities of Mepindolol.Etanercept may decrease the antihypertensive activities of Epanolol.Etanercept may decrease the antihypertensive activities of Tertatolol.The risk or severity of adverse effects can be increased when Etanercept is combined with Dibotermin alfa.The risk or severity of adverse effects can be increased when Etanercept is combined with Pitolisant.The risk or severity of adverse effects can be increased when Floctafenine is combined with Etanercept.The risk or severity of adverse effects can be increased when Etanercept is combined with Acemetacin.The risk or severity of infection can be increased when Etanercept is combined with Abatacept.The risk or severity of adverse effects can be increased when Etanercept is combined with Anakinra.The risk or severity of adverse effects can be increased when Etanercept is combined with Belimumab.The risk or severity of infection and neutropenia can be increased when Etanercept is combined with Canakinumab.The risk or severity of infection can be increased when Etanercept is combined with Certolizumab pegol.The risk or severity of adverse effects can be increased when Etanercept is combined with Cyclophosphamide.Etanercept may increase the immunosuppressive activities of Infliximab.The risk or severity of adverse effects can be increased when Etanercept is combined with Natalizumab.The risk or severity of adverse effects can be increased when Pimecrolimus is combined with Etanercept.The risk or severity of adverse effects can be increased when Etanercept is combined with Rilonacept.Tocilizumab may increase the immunosuppressive activities of Etanercept.The risk or severity of adverse effects can be increased when Etanercept is combined with Tofacitinib.The risk or severity of infection can be increased when Etanercept is combined with Vedolizumab.The risk or severity of adverse effects can be increased when Dexketoprofen is combined with Etanercept.The risk or severity of adverse effects can be increased when Ketorolac is combined with Etanercept.The risk or severity of adverse effects can be increased when Morniflumate is combined with Etanercept.The risk or severity of bleeding can be increased when Etanercept is combined with Omacetaxine mepesuccinate.The risk or severity of adverse effects can be increased when Talniflumate is combined with Etanercept.The therapeutic efficacy of Mifamurtide can be decreased when used in combination with Etanercept.The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Etanercept.The risk or severity of adverse effects can be increased when Adalimumab is combined with Etanercept.The risk or severity of adverse effects can be increased when Etanercept is combined with Golimumab.The risk or severity of adverse effects can be increased when Etanercept is combined with Rituximab. 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SarilumabTorasemideFurosemideBumetanideEtacrynic acidAzosemidePiretanideLithiumMethotrexateTenofovir disoproxilSodium phosphateBetrixabanLeflunomideFingolimodRoflumilastCyclosporineVaricella Zoster Vaccine (Live/Attenuated)Yellow Fever VaccineClostridium tetani toxoid antigen (formaldehyde inactivated)Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated)Rotavirus VaccineG17DTINGN 201INGN 225RindopepimutSRP 299GI-5005TG4010Rabies virus inactivated antigen, ATecemotideRubella virus vaccineAnthrax immune globulin humanBacillus calmette-guerin substrain tice live antigenJapanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated)Salmonella typhi ty2 vi polysaccharide antigenBacillus calmette-guerin substrain connaught live antigenHepatitis A VaccineSalmonella typhi ty21a live antigenHuman rabies virus immune globulinHepatitis B Vaccine (Recombinant)DiclofenacOcrelizumabColestipolColesevelamCholestyramineAmikacinTobramycinGentamicinNeomycinStreptomycinValrubicinStreptozocinEpirubicinFramycetinDaunorubicinSpectinomycinNetilmicinDoxorubicinKanamycinIdarubicinParomomycinMetrizamideRibostamycinGeneticinApramycinGENTAMICIN C1ANeamineSP1049CAldoxorubicinAmrubicinAnnamycinArbekacinPlicamycinPuromycinDihydrostreptomycinHygromycin BPirarubicinAclarubicinZorubicinSabarubicinSisomicinPlazomicinZoptarelin doxorubicinGPX-150DibekacinMicronomicinIsepamicinBekanamycinAliskirenDeferasiroxDesmopressinGrepafloxacinEnoxacinPefloxacinTrovafloxacinNalidixic AcidRosoxacinCinoxacinGatifloxacinNorfloxacinLevofloxacinGemifloxacinSparfloxacinTemafloxacinFleroxacinGarenoxacinNemonoxacinFlumequinePazufloxacinPrulifloxacinSitafloxacinOxolinic acidPiromidic acidRufloxacinPipemidic acidDigoxinDrospirenoneEplerenoneHaloperidolHydralazinePralatrexateProbenecidTreprostinilVancomycinMethyclothiazideChlorothiazideHydrochlorothiazideEpitizideChlorthalidoneBendroflumethiazideMetolazoneHydroflumethiazideIndapamideTrichlormethiazidePolythiazideQuinethazoneCyclopenthiazideMesalazineBalsalazideOlsalazineDenosumabSipuleucel-TTrastuzumabRisedronateEtidronic acidClodronic AcidPamidronateZoledronic acidIbandronateAlendronic acidTechnetium Tc-99m medronateTechnetium Tc-99m etidronateTiludronic acidCarboprost TromethamineDinoprostoneMisoprostolGemeprostDinoprostSulprostoneEnprostilFolic AcidTravoprostLatanoprostAlprostadilBimatoprostLubiprostoneIloprostDinoprost TromethamineEpoprostenolProstaglandin B2Prostaglandin G2BeraprostUnoprostoneTafluprostLimaprostFenprostaleneLuprostiolProstaleneCloprostenolFluprostenolLatanoprostene BunodLepirudinBivalirudinAbciximabBecaplerminDicoumarolArgatrobanArdeparinPhenindioneFondaparinux sodiumWarfarinPentosan PolysulfatePhenprocoumonEdetic 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acidEtoricoxibCastanospermineResveratrolOxyphenbutazoneNiflumic AcidNimesulideBenoxaprofenMetamizoleZomepiracPirfenidoneSRT501PTC299TarenflurbilApremilastAndrographolideIcatibantExisulindLornoxicamAceclofenacZaltoprofenSeratrodastAzapropazoneFelbinacTranilastParecoxibSalicylamideTeriflunomide(4R)-limoneneKebuzoneIsoxicamIndoprofenIbuproxamFenbufenEtofenamateEpirizoleLoxoprofenDroxicamTolfenamic AcidClonixinPropacetamolEvening primrose oilOrgoteinTepoxalinFlunixinCurcuminE-6201AnisodamineDuvelisibTriptolideSemapimodBucillamineLisofyllineNitroaspirinIndobufenMizoribineApocyninHigenamineTinoridineParthenolideSerrapeptaseAlclofenacFentiazacTribenosideSuxibuzoneBumadizoneAlminoprofenFlunoxaprofenBufexamacFeprazoneDifenpiramideNifenazoneLonazolacTenidapBendazacPranoprofenPropyphenazoneProglumetacinGuacetisalBevoniumEthenzamideCarbaspirin calciumMofebutazoneProquazoneBenorilatePirprofenImidazole salicylateBenzydamineTacrolimusValsartanOlmesartanLosartanCandesartan cilexetilEprosartanTelmisartanIrbesartanSaprisartanTasosartanAzilsartan medoxomilCandesartanSaralasinSacubitrilForasartanFimasartanRamiprilFosinoprilTrandolaprilBenazeprilEnalaprilMoexiprilLisinoprilPerindoprilQuinaprilCaptoprilCilazaprilSpiraprilEnalaprilatTemocaprilZofenoprilOmapatrilatImidaprilDelaprilRescinnamineCandoxatrilAzficel-TTriamtereneAmilorideSpironolactoneEsmololBetaxololMetoprololAtenololTimololCarteololPropranololLabetalolBisoprololPindololCarvedilolAcebutololNadololLevobunololMetipranololSotalolNebivololAlprenololBevantololPractololPenbutololOxprenololPlatelet Activating FactorCeliprololBufuralolBopindololBupranololIndenololBefunololArotinololTalinololLandiololBucindololCloranololMepindololEpanololTertatololDibotermin alfaPitolisantFloctafenineAcemetacinAbataceptAnakinraBelimumabCanakinumabCertolizumab pegolCyclophosphamideInfliximabNatalizumabPimecrolimusRilonaceptTocilizumabTofacitinibVedolizumabDexketoprofenKetorolacMorniflumateOmacetaxine mepesuccinateTalniflumateMifamurtideBCG vaccineAdalimumabGolimumabRituximab Melting PointHydrophobicityIsoelectric PointMolecular WeightMolecular Formula 71 °C (whole mAb)-0.5297.8951234.9C2224H3475N621O698S36 Vermeer, A.W.P. & Norde, W., Biophys. J. 78:394-404 (2000) L04AB01 Tumor necrosis factor alpha (TNF-α) inhibitorsIMMUNOSUPPRESSANTSIMMUNOSUPPRESSANTSANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L04ABL04AL04L Amino Acids, Peptides, and ProteinsAnalgesicsAnalgesics, Non-NarcoticAnti-Inflammatory AgentsAnti-Inflammatory Agents, Non-SteroidalAntibodiesAntineoplastic and Immunomodulating AgentsAntirheumatic AgentsBiologics for Rheumatoid Arthritis TreatmentBlood ProteinsCentral Nervous System AgentsChemical Actions and UsesDisease-modifying Antirheumatic AgentsGastrointestinal AgentsGlobulinsImmunoglobulin GImmunoglobulin IsotypesImmunoglobulinsImmunologic FactorsImmunoproteinsImmunosuppressive AgentsMembrane ProteinsPeripheral Nervous System AgentsPharmacologic ActionsPhysiological Effects of DrugsProteinsReceptors, Cell SurfaceReceptors, CytokineReceptors, ImmunologicReceptors, Tumor Necrosis FactorSensory System AgentsSerum GlobulinsTherapeutic UsesTumor Necrosis Factor Alpha (TNF-α) InhibitorsTumor Necrosis Factor Blocker D000602D000700D018712D000893D000894D000906D018501D001798D002491D020164D005765D005916D007074D007132D007136D007155D007162D007166D008565D018373D020228D045505D011506D011956D018121D011971D018124D018689D012712D045506 1203246506732C07897D00742M32315PA449515P20333DNC000605EtanerceptCHEMBL1201572 Drugs Product Database (DPD)PubChem SubstanceKEGG CompoundKEGG DrugGenBankPharmGKBUniProtKBTherapeutic Targets DatabaseWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic/etanercept.htmhttp://www.drugs.com/cdi/etanercept.html approvedinvestigational DavictrelEnbrel SureclickTunex Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides 24769342123593727647736755 CanadaCanadaUnited StatesUnited States 2009-06-162000-03-142007-10-022000-06-27 2023-02-272013-09-142024-07-292012-10-23 falsefalsefalsefalse Amgen Inc. + Wyeth + Takeda false EtanerceptEtanercept + WaterEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanerceptEtanercept EnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelBrenzysBrenzysErelziErelziEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelErelzi Amgen Inc.Boehringer Ingelheim Ltd.DSM Corp.Immunex Corp.Physicians Total Care Inc.Vetter Pharma Fertigung GmbH and Co. KG http://www.amgen.comhttp://www.boehringer-ingelheim.comhttp://www.dsm.comhttp://www.physicianstotalcare.comhttp://www.vetter-pharma.com BrenzysBrenzysEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelEnbrelErelziErelziErelzi falsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalse Samsung Bioepis Co., Ltd.Samsung Bioepis Co., Ltd.Immunex CorporationImmunex CorporationImmunex CorporationPfizerPfizerPfizerPfizerPfizerPfizerPfizerPfizerPfizerPfizerPfizerPfizerPfizerPfizerPfizerPfizerPfizerPfizerPfizerPfizerPfizerImmunex CorporationImmunex CorporationImmunex CorporationImmunex CorporationImmunex CorporationSandoz Canada IncorporatedSandoz Canada IncorporatedSandoz Canada Incorporated falsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalse SubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneous SolutionSolutionSolutionSolutionKit; Liquid; Powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, powder, for solutionSolutionSolutionSolutionKitSolutionSolutionSolutionSolution DPDDPDFDA NDCFDA NDCDPDEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAFDA NDCFDA NDCDPDFDA NDCFDA NDCDPDDPDDPD 50 mg50 mg50 mg/mL25 mg/.5mL25 mg25 mg25 mg25 mg25 mg50 mg50 mg50 mg50 mg50 mg50 mg25 mg25 mg25 mg50 mg50 mg50 mg50 mg50 mg50 mg10 mg50 mg/mL50 mg/mL50 mg50 mg/mL25 mg50 mg50 mg 58406-44558406-45558406-44658406-45658406-42558406-435 BLA103795BLA103795BLA103795BLA103795 truetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetrue 02455323024553310224290302274728024628770246285002462869 CanadaCanadaUSUSCanadaEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUUSUSCanadaUSUSCanadaCanadaCanada 2016-09-232016-09-132005-11-102005-11-102001-03-142000-02-032000-02-032000-02-032000-02-032000-02-032000-02-032000-02-032000-02-032000-02-032000-02-032000-02-032000-02-032000-02-032000-02-032000-02-032000-02-032000-02-032000-02-032000-02-032000-02-032000-02-032017-10-202017-09-292005-12-212003-01-022005-10-062017-12-082017-08-042017-08-04 eachsyringeboxboxbox 250.37488.741016.572033.142033.14 USDUSDUSDUSDUSD Enbrel 25 mg kitEnbrel 50 mg/ml sureclick syrEnbrel 4 25 mg Kit (1 Box = 1 Kit = Four 25 mg Vials)Enbrel (1 Box = 1 Kit = Four 50 mg Syringes) 3.92ml BoxEnbrel SureClick (1 Box Contains Four 50 mg Prefilled Autoinjectors) !BmhCGCI@JkwTFHBcCqprIopnx@Nzx]KZ@kwVo]S|iraAWwGe_b[|KnDAVxPBGBwakwWJDHbjIrIotAVB{ca@MaskwWJDLhPc~HKnND@ezNOxi^c{g~Oxi^cc~Ka@I^cc~JWh~yc~JWhxb{ga@I^cezNOxhb{g~Wh~yc~JWhxb{ga@I^cezNOxhb{ga@I^cjIrOxnyezNWh{Cmc~Kn_~y{ga@I^cezNp{Xb{g~Wh~D@ezLbC~yc~JOxi^cxPBOxnyc~JhgND@ezNp{Y^c[|ha_~yaZAsqy~EWpYdIHV`YBQ_AbAyaZBEhFPdWpZEhBAyFunEhE|FYBQdIHV`HGedIE|FYBRzgrAyaZBEhFPdYBQ_AbAyaZBEhHV`ni}dIFPdWpX`^XV`aZ@ ]U:vzxvzbxuzfvCzQjzqwxUz_h@PbMbN7zqdLTUqRLCnded6zBrq0Di14@kJ0J13zKs@m2d8Wq0v0 DB00006DB02351 128270-60-0 Bivalirudin BivalirudinaBivalirudinumHirulog small molecule TN9BEX005G 2180.2853 Avi Tovi, Chaim Eidelman, Shimon Shushan, Alon Hagi, Alexander Ivchenko, Gabriel-Marcus Butilca, Leah Bar-Oz, Tehila Gadi, Gil Zaovi, "Process for production of Bivalirudin." U.S. Patent US20070093423, issued April 26, 2007. solid Bivalirudin is a synthetic 20 residue peptide (thrombin inhibitor) which reversibly inhibits thrombin. Once bound to the active site, thrombin cannot activate fibrinogen into fibrin, the crucial step in the formation of thrombus. It is administered intravenously. Because it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure. Humans and other mammals Injection, powder, lyophilized, for solutionInjectionPowder, for solutionInjectionInjection IntravenousIntracavernousIntravenousIntravenousIntravenous 250 mg/1250 mg/1250 mg250 mg/50mL500 mg/100mL For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned. Inhibits the action of thrombin by binding both to its catalytic site and to its anion-binding exosite. Thrombin is a serine proteinase that plays a central role in the thrombotic process, acting to cleave fibrinogen into fibrin monomers and to activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release. inhibitor Prothrombin BE0000048 Human Scatena R: Bivalirudin: a new generation antithrombotic drug. Expert Opin Investig Drugs. 2000 May;9(5):1119-27.Bates ER: Bivalirudin for percutaneous coronary intervention and in acute coronary syndromes. Curr Cardiol Rep. 2001 Sep;3(5):348-54.Gladwell TD: Bivalirudin: a direct thrombin inhibitor. Clin Ther. 2002 Jan;24(1):38-58.Kleiman NS, Klem J, Fernandes LS, Rubin H, Challa S, Solomon S, Maresh K, Arora U, Klem E, Buergler J, Mathew S, Browning A, DeLao T: Pharmacodynamic profile of the direct thrombin antagonist bivalirudin given in combination with the glycoprotein IIb/IIIa antagonist eptifibatide. Am Heart J. 2002 Apr;143(4):585-93.Carswell CI, Plosker GL: Bivalirudin: a review of its potential place in the management of acute coronary syndromes. Drugs. 2002;62(5):841-70.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. 110607321150457011833835119237941192933411752352 P00734 Prothrombin 11p11-q12 Human blood microparticleextracellular matrixGolgi lumencytosolextracellular exosomeextracellular regionendoplasmic reticulum lumenplasma membraneextracellular spacethrombospondin receptor activitycalcium ion bindingserine-type endopeptidase activitygrowth factor activityreceptor bindingnegative regulation of platelet activationregulation of cell shaperegulation of gene expressionblood coagulationnegative regulation of proteolysisplatelet activationresponse to inactivitypositive regulation of blood coagulationresponse to woundingacute-phase responsepositive regulation of cell growthblood coagulation, intrinsic pathwayproteolysispositive regulation of cell proliferationpositive regulation of protein phosphorylationcell surface receptor signaling pathwaypositive regulation of collagen biosynthetic processcytosolic calcium ion homeostasispositive regulation of phosphatidylinositol 3-kinase signalingcellular response to mechanical stimulusfibrinolysispositive regulation of phospholipase C-activating G-protein coupled receptor signaling pathwayleukocyte migrationmulticellular organismal developmentpositive regulation of reactive oxygen species metabolic processcellular protein metabolic processnegative regulation of astrocyte differentiationpeptidyl-glutamic acid carboxylationpositive regulation of release of sequestered calcium ion into cytosolpost-translational protein modificationnegative regulation of fibrinolysisregulation of blood coagulation Thrombospondin receptor activity Thrombin, which cleaves bonds after Arg and Lys, converts fibrinogen to fibrin and activates factors V, VII, VIII, XIII, and, in complex with thrombomodulin, protein C. Functions in blood homeostasis, inflammation and wound healing. Other than thrombin and red blood cells, bivalirudin does not bind to plasma proteins. Based on a study by Gleason et al., the no-observed-adverse-effect level (NOAEL) for bivalirudin, administered to rats via intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h. * Normal renal function: 25 min (in normal conditions)* Creatinine clearance 10-29mL/min: 57min* Dialysis-dependant patients: 3.5h Following intravenous administration, bivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 +/- 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr intravenous infusion given over 4 hours. 80% proteolytic cleavage * 3.4 mL/min/kg [Normal renal function]* 3.4 mL/min/kg [mild renal function]* 2.7 mL/min/kg [moderate renal function]* 2.8 mL/min/kg [severe renal function]* 1 mL/min/kg [Dialysis-dependent patients] 0.2L/kg Bivalirudin is cleared from plasma by a combination of renal mechanisms (20%) and proteolytic cleavage. Bivalirudin directly and reversibly inhibits thrombin by specifically binding both to the catalytic site and to the anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible because thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin. The serum concentration of Ethinyl Estradiol can be decreased when it is combined with Bivalirudin.The serum concentration of Mestranol can be decreased when it is combined with Bivalirudin.The serum concentration of Estradiol can be decreased when it is combined with Bivalirudin.The serum concentration of Estrone sulfate can be decreased when it is combined with Bivalirudin.The serum concentration of Synthetic Conjugated Estrogens, A can be decreased when it is combined with Bivalirudin.The serum concentration of Estrogens, esterified can be decreased when it is combined with Bivalirudin.The serum concentration of Chlorotrianisene can be decreased when it is combined with Bivalirudin.The serum concentration of Conjugated estrogens can be decreased when it is combined with Bivalirudin.The serum concentration of Estramustine can be decreased when it is combined with Bivalirudin.The serum concentration of Dienestrol can be decreased when it is combined with Bivalirudin.The serum concentration of Diethylstilbestrol can be decreased when it is combined with Bivalirudin.The serum concentration of Hexestrol can be decreased when it is combined with Bivalirudin.The serum concentration of Methallenestril can be decreased when it is combined with Bivalirudin.The serum concentration of Cyclosporine can be increased when it is combined with Bivalirudin.The serum concentration of Bivalirudin can be decreased when it is combined with Garlic.The metabolism of Tacrolimus can be decreased when combined with Bivalirudin.The risk or severity of adverse effects can be increased when Bivalirudin is combined with Pethidine.The serum concentration of Alprazolam can be increased when it is combined with Bivalirudin.The serum concentration of Bivalirudin can be decreased when it is combined with Boceprevir.The metabolism of Bivalirudin can be increased when combined with Carbamazepine.The therapeutic efficacy of Clarithromycin can be decreased when used in combination with Bivalirudin.The serum concentration of Delavirdine can be decreased when it is combined with Bivalirudin.Estrone may decrease the anticoagulant activities of Bivalirudin.Polyestradiol phosphate may decrease the anticoagulant activities of Bivalirudin.Genistein may decrease the anticoagulant activities of Bivalirudin.Quinestrol may decrease the anticoagulant activities of Bivalirudin.Synthetic Conjugated Estrogens, B may decrease the anticoagulant activities of Bivalirudin.Zeranol may decrease the anticoagulant activities of Bivalirudin.Equol may decrease the anticoagulant activities of Bivalirudin.Secoisolariciresinol may decrease the anticoagulant activities of Bivalirudin.Daidzein may decrease the anticoagulant activities of Bivalirudin.Epimestrol may decrease the anticoagulant activities of Bivalirudin.Estriol may decrease the anticoagulant activities of Bivalirudin.Promestriene may decrease the anticoagulant activities of Bivalirudin.Moxestrol may decrease the anticoagulant activities of Bivalirudin.Estradiol acetate may decrease the anticoagulant activities of Bivalirudin.Estradiol cypionate may decrease the anticoagulant activities of Bivalirudin.Estradiol valerate may decrease the anticoagulant activities of Bivalirudin.The risk or severity of bleeding can be increased when Bivalirudin is combined with Omacetaxine mepesuccinate.The serum concentration of Nefazodone can be increased when it is combined with Bivalirudin.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Aprotinin.The therapeutic efficacy of Bivalirudin can be increased when used in combination with Testosterone cypionate.The therapeutic efficacy of Bivalirudin can be increased when used in combination with Testosterone enanthate.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Allylestrenol.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Etonogestrel.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Medroxyprogesterone acetate.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Progesterone.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Norethisterone.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Hydroxyprogesterone caproate.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Desogestrel.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Dydrogesterone.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Gestodene.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Altrenogest.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Gestrinone.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Medrogestone.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Nomegestrol.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Gestonorone.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Methylestrenolone.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Norgestrienone.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Promegestone.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Demegestone.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Megestrol acetate.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Levonorgestrel.The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Dienogest.The therapeutic efficacy of Bivalirudin can be increased when used in combination with Testosterone undecanoate.The serum concentration of Riociguat can be increased when it is combined with Bivalirudin.The serum concentration of Sildenafil can be increased when it is combined with Bivalirudin.The risk or severity of adverse effects can be increased when Bivalirudin is combined with Temsirolimus.The metabolism of Diltiazem can be decreased when combined with Bivalirudin.The metabolism of Verapamil can be decreased when combined with Bivalirudin.Pentosan Polysulfate may increase the anticoagulant activities of Bivalirudin.The serum concentration of Amitriptyline can be increased when it is combined with Bivalirudin.The serum concentration of Protriptyline can be increased when it is combined with Bivalirudin.The serum concentration of Imipramine can be increased when it is combined with Bivalirudin.The serum concentration of Nortriptyline can be increased when it is combined with Bivalirudin.The serum concentration of Trimipramine can be increased when it is combined with Bivalirudin.The serum concentration of Doxepin can be increased when it is combined with Bivalirudin.The serum concentration of Desipramine can be increased when it is combined with Bivalirudin.The serum concentration of Clomipramine can be increased when it is combined with Bivalirudin.The serum concentration of Mirtazapine can be increased when it is combined with Bivalirudin.The serum concentration of Cyclobenzaprine can be increased when it is combined with Bivalirudin.The serum concentration of Amineptine can be increased when it is combined with Bivalirudin.The serum concentration of Esmirtazapine can be increased when it is combined with Bivalirudin.The serum concentration of Dosulepin can be increased when it is combined with Bivalirudin.The serum concentration of Tianeptine can be increased when it is combined with Bivalirudin.The serum concentration of Opipramol can be increased when it is combined with Bivalirudin.The serum concentration of Dibenzepin can be increased when it is combined with Bivalirudin.The serum concentration of Lofepramine can be increased when it is combined with Bivalirudin.The serum concentration of Iprindole can be increased when it is combined with Bivalirudin.The serum concentration of Amoxapine can be increased when it is combined with Bivalirudin.The serum concentration of Abacavir can be decreased when it is combined with Bivalirudin.The risk or severity of adverse effects can be increased when Bivalirudin is combined with Cyclophosphamide.The serum concentration of Digoxin can be increased when it is combined with Bivalirudin.The serum concentration of Enfuvirtide can be increased when it is combined with Bivalirudin.The serum concentration of Etravirine can be decreased when it is combined with Bivalirudin.Dasatinib may increase the anticoagulant activities of Bivalirudin.The risk or severity of adverse effects can be increased when Bivalirudin is combined with Deferasirox.The risk or severity of adverse effects can be increased when Bivalirudin is combined with Deoxycholic Acid.The risk or severity of adverse effects can be increased when Bivalirudin is combined with Ibritumomab tiuxetan.The risk or severity of adverse effects can be increased when Ibrutinib is combined with Bivalirudin.The risk or severity of adverse effects can be increased when Bivalirudin is combined with Nintedanib.The risk or severity of adverse effects can be increased when Bivalirudin is combined with Obinutuzumab.The risk or severity of adverse effects can be increased when Bivalirudin is combined with Collagenase clostridium histolyticum.Sugammadex may increase the anticoagulant activities of Bivalirudin.The risk or severity of adverse effects can be increased when Limaprost is combined with Bivalirudin.Tibolone may increase the anticoagulant activities of Bivalirudin.Ketorolac may increase the anticoagulant activities of Bivalirudin.Diclofenac may increase the anticoagulant activities of Bivalirudin.Flurbiprofen may increase the anticoagulant activities of Bivalirudin.Bromfenac may increase the anticoagulant activities of Bivalirudin.Nepafenac may increase the anticoagulant activities of Bivalirudin.Etanercept may increase the anticoagulant activities of Bivalirudin.Masoprocol may increase the anticoagulant activities of Bivalirudin.Adapalene may increase the anticoagulant activities of Bivalirudin.Mesalazine may increase the anticoagulant activities of Bivalirudin.Indomethacin may increase the anticoagulant activities of Bivalirudin.Pimecrolimus may increase the anticoagulant activities of Bivalirudin.Nabumetone may increase the anticoagulant activities of Bivalirudin.Tenoxicam may increase the anticoagulant activities of Bivalirudin.Celecoxib may increase the anticoagulant activities of Bivalirudin.Tolmetin may increase the anticoagulant activities of Bivalirudin.Rofecoxib may increase the anticoagulant activities of Bivalirudin.Piroxicam may increase the anticoagulant activities of Bivalirudin.Fenoprofen may increase the anticoagulant activities of Bivalirudin.Valdecoxib may increase the anticoagulant activities of Bivalirudin.Sulindac may increase the anticoagulant activities of Bivalirudin.Chloroquine may increase the anticoagulant activities of Bivalirudin.Mycophenolate mofetil may increase the anticoagulant activities of Bivalirudin.Naftifine may increase the anticoagulant activities of Bivalirudin.Zileuton may increase the anticoagulant activities of Bivalirudin.Etodolac may increase the anticoagulant activities of Bivalirudin.Olopatadine may increase the anticoagulant activities of Bivalirudin.Mefenamic acid may increase the anticoagulant activities of Bivalirudin.Naproxen may increase the anticoagulant activities of Bivalirudin.Sulfasalazine may increase the anticoagulant activities of Bivalirudin.Phenylbutazone may increase the anticoagulant activities of Bivalirudin.Meloxicam may increase the anticoagulant activities of Bivalirudin.Carprofen may increase the anticoagulant activities of Bivalirudin.Diflunisal may increase the anticoagulant activities of Bivalirudin.Suprofen may increase the anticoagulant activities of Bivalirudin.Salicylic acid may increase the anticoagulant activities of Bivalirudin.Meclofenamic acid may increase the anticoagulant activities of Bivalirudin.Acetylsalicylic acid may increase the anticoagulant activities of Bivalirudin.Azelastine may increase the anticoagulant activities of Bivalirudin.Oxaprozin may increase the anticoagulant activities of Bivalirudin.Ketoprofen may increase the anticoagulant activities of Bivalirudin.Balsalazide may increase the anticoagulant activities of Bivalirudin.Mycophenolic acid may increase the anticoagulant activities of Bivalirudin.Ibuprofen may increase the anticoagulant activities of Bivalirudin.Leflunomide may increase the anticoagulant activities of Bivalirudin.Olsalazine may increase the anticoagulant activities of Bivalirudin.Lumiracoxib may increase the anticoagulant activities of Bivalirudin.Magnesium salicylate may increase the anticoagulant activities of Bivalirudin.Salsalate may increase the anticoagulant activities of Bivalirudin.Choline magnesium trisalicylate may increase the anticoagulant activities of Bivalirudin.Antipyrine may increase the anticoagulant activities of Bivalirudin.Tiaprofenic acid may increase the anticoagulant activities of Bivalirudin.Etoricoxib may increase the anticoagulant activities of Bivalirudin.Castanospermine may increase the anticoagulant activities of Bivalirudin.Resveratrol may increase the anticoagulant activities of Bivalirudin.Oxyphenbutazone may increase the anticoagulant activities of Bivalirudin.Niflumic Acid may increase the anticoagulant activities of Bivalirudin.Nimesulide may increase the anticoagulant activities of Bivalirudin.Benoxaprofen may increase the anticoagulant activities of Bivalirudin.Metamizole may increase the anticoagulant activities of Bivalirudin.Zomepirac may increase the anticoagulant activities of Bivalirudin.Pirfenidone may increase the anticoagulant activities of Bivalirudin.SRT501 may increase the anticoagulant activities of Bivalirudin.PTC299 may increase the anticoagulant activities of Bivalirudin.Tarenflurbil may increase the anticoagulant activities of Bivalirudin.Apremilast may increase the anticoagulant activities of Bivalirudin.Andrographolide may increase the anticoagulant activities of Bivalirudin.Icatibant may increase the anticoagulant activities of Bivalirudin.Exisulind may increase the anticoagulant activities of Bivalirudin.Lornoxicam may increase the anticoagulant activities of Bivalirudin.Aceclofenac may increase the anticoagulant activities of Bivalirudin.Zaltoprofen may increase the anticoagulant activities of Bivalirudin.Seratrodast may increase the anticoagulant activities of Bivalirudin.Azapropazone may increase the anticoagulant activities of Bivalirudin.Felbinac may increase the anticoagulant activities of Bivalirudin.Tranilast may increase the anticoagulant activities of Bivalirudin.Ferulic acid may increase the anticoagulant activities of Bivalirudin.Parecoxib may increase the anticoagulant activities of Bivalirudin.Salicylamide may increase the anticoagulant activities of Bivalirudin.Teriflunomide may increase the anticoagulant activities of Bivalirudin.(4R)-limonene may increase the anticoagulant activities of Bivalirudin.Kebuzone may increase the anticoagulant activities of Bivalirudin.Isoxicam may increase the anticoagulant activities of Bivalirudin.Indoprofen may increase the anticoagulant activities of Bivalirudin.Ibuproxam may increase the anticoagulant activities of Bivalirudin.Floctafenine may increase the anticoagulant activities of Bivalirudin.Fenbufen may increase the anticoagulant activities of Bivalirudin.Etofenamate may increase the anticoagulant activities of Bivalirudin.Epirizole may increase the anticoagulant activities of Bivalirudin.Loxoprofen may increase the anticoagulant activities of Bivalirudin.Droxicam may increase the anticoagulant activities of Bivalirudin.Tolfenamic Acid may increase the anticoagulant activities of Bivalirudin.Clonixin may increase the anticoagulant activities of Bivalirudin.Propacetamol may increase the anticoagulant activities of Bivalirudin.Evening primrose oil may increase the anticoagulant activities of Bivalirudin.Orgotein may increase the anticoagulant activities of Bivalirudin.Tepoxalin may increase the anticoagulant activities of Bivalirudin.Flunixin may increase the anticoagulant activities of Bivalirudin.Curcumin may increase the anticoagulant activities of Bivalirudin.E-6201 may increase the anticoagulant activities of Bivalirudin.Anisodamine may increase the anticoagulant activities of Bivalirudin.Duvelisib may increase the anticoagulant activities of Bivalirudin.Triptolide may increase the anticoagulant activities of Bivalirudin.Semapimod may increase the anticoagulant activities of Bivalirudin.Bucillamine may increase the anticoagulant activities of Bivalirudin.Lisofylline may increase the anticoagulant activities of Bivalirudin.Nitroaspirin may increase the anticoagulant activities of Bivalirudin.Nafamostat may increase the anticoagulant activities of Bivalirudin.Mizoribine may increase the anticoagulant activities of Bivalirudin.Apocynin may increase the anticoagulant activities of Bivalirudin.Higenamine may increase the anticoagulant activities of Bivalirudin.Tinoridine may increase the anticoagulant activities of Bivalirudin.Parthenolide may increase the anticoagulant activities of Bivalirudin.Serrapeptase may increase the anticoagulant activities of Bivalirudin.Alclofenac may increase the anticoagulant activities of Bivalirudin.Fentiazac may increase the anticoagulant activities of Bivalirudin.Tribenoside may increase the anticoagulant activities of Bivalirudin.Suxibuzone may increase the anticoagulant activities of Bivalirudin.Bumadizone may increase the anticoagulant activities of Bivalirudin.Alminoprofen may increase the anticoagulant activities of Bivalirudin.Flunoxaprofen may increase the anticoagulant activities of Bivalirudin.Bufexamac may increase the anticoagulant activities of Bivalirudin.Feprazone may increase the anticoagulant activities of Bivalirudin.Difenpiramide may increase the anticoagulant activities of Bivalirudin.Nifenazone may increase the anticoagulant activities of Bivalirudin.Lonazolac may increase the anticoagulant activities of Bivalirudin.Tenidap may increase the anticoagulant activities of Bivalirudin.Bendazac may increase the anticoagulant activities of Bivalirudin.Pranoprofen may increase the anticoagulant activities of Bivalirudin.Propyphenazone may increase the anticoagulant activities of Bivalirudin.Proglumetacin may increase the anticoagulant activities of Bivalirudin.Guacetisal may increase the anticoagulant activities of Bivalirudin.Bevonium may increase the anticoagulant activities of Bivalirudin.Ethenzamide may increase the anticoagulant activities of Bivalirudin.Carbaspirin calcium may increase the anticoagulant activities of Bivalirudin.Mofebutazone may increase the anticoagulant activities of Bivalirudin.Proquazone may increase the anticoagulant activities of Bivalirudin.Benorilate may increase the anticoagulant activities of Bivalirudin.Pirprofen may increase the anticoagulant activities of Bivalirudin.Imidazole salicylate may increase the anticoagulant activities of Bivalirudin.Benzydamine may increase the anticoagulant activities of Bivalirudin.Tipranavir may increase the anticoagulant activities of Bivalirudin.Omega-3 fatty acids may increase the anticoagulant activities of Bivalirudin.Vitamin E may increase the anticoagulant activities of Bivalirudin.The risk or severity of adverse effects can be increased when Bivalirudin is combined with Tositumomab.Bivalirudin may increase the anticoagulant activities of Dabigatran etexilate.Lepirudin may increase the anticoagulant activities of Bivalirudin.Bivalirudin may increase the anticoagulant activities of Abciximab.Bivalirudin may increase the anticoagulant activities of Becaplermin.Bivalirudin may increase the anticoagulant activities of Dicoumarol.Bivalirudin may increase the anticoagulant activities of Argatroban.Bivalirudin may increase the anticoagulant activities of Ardeparin.Bivalirudin may increase the anticoagulant activities of Phenindione.Bivalirudin may increase the anticoagulant activities of Fondaparinux sodium.Bivalirudin may increase the anticoagulant activities of Warfarin.Bivalirudin may increase the anticoagulant activities of Phenprocoumon.Bivalirudin may increase the anticoagulant activities of Edetic Acid.Bivalirudin may increase the anticoagulant activities of Heparin.Bivalirudin may increase the anticoagulant activities of Enoxaparin.Bivalirudin may increase the anticoagulant activities of Acenocoumarol.Bivalirudin may increase the anticoagulant activities of Citric Acid.Bivalirudin may increase the anticoagulant activities of Ximelagatran.Bivalirudin may increase the anticoagulant activities of Ancrod.Bivalirudin may increase the anticoagulant activities of Pentaerythritol Tetranitrate.Bivalirudin may increase the anticoagulant activities of Sulodexide.Bivalirudin may increase the anticoagulant activities of Idraparinux.Bivalirudin may increase the anticoagulant activities of Otamixaban.Bivalirudin may increase the anticoagulant activities of Danaparoid.Bivalirudin may increase the anticoagulant activities of Dalteparin.Bivalirudin may increase the anticoagulant activities of Ethyl biscoumacetate.Bivalirudin may increase the anticoagulant activities of Nadroparin.Bivalirudin may increase the anticoagulant activities of Dextran.Bivalirudin may increase the anticoagulant activities of Reviparin.Bivalirudin may increase the anticoagulant activities of Certoparin.Bivalirudin may increase the anticoagulant activities of Dextran 70.Bivalirudin may increase the anticoagulant activities of Desirudin.Bivalirudin may increase the anticoagulant activities of Dextran 40.Bivalirudin may increase the anticoagulant activities of Dextran 75.Bivalirudin may increase the anticoagulant activities of Protocatechualdehyde.Bivalirudin may increase the anticoagulant activities of Protein C.Bivalirudin may increase the anticoagulant activities of Antithrombin III human.Bivalirudin may increase the anticoagulant activities of Fondaparinux.Bivalirudin may increase the anticoagulant activities of Letaxaban.Bivalirudin may increase the anticoagulant activities of Darexaban.Bivalirudin may increase the anticoagulant activities of Gabexate.Bivalirudin may increase the anticoagulant activities of Troxerutin.Bivalirudin may increase the anticoagulant activities of Fluindione.Bivalirudin may increase the anticoagulant activities of Protein S human.Bivalirudin may increase the anticoagulant activities of Melagatran.Aminosalicylic Acid may increase the anticoagulant activities of Bivalirudin.Dersalazine may increase the anticoagulant activities of Bivalirudin.Aloxiprin may increase the anticoagulant activities of Bivalirudin.Hemoglobin crosfumaril may increase the anticoagulant activities of Bivalirudin.Methyl salicylate may increase the anticoagulant activities of Bivalirudin.Trolamine salicylate may increase the anticoagulant activities of Bivalirudin.Alteplase may increase the anticoagulant activities of Bivalirudin.Reteplase may increase the anticoagulant activities of Bivalirudin.Anistreplase may increase the anticoagulant activities of Bivalirudin.Tenecteplase may increase the anticoagulant activities of Bivalirudin.Drotrecogin alfa may increase the anticoagulant activities of Bivalirudin.Ticlopidine may increase the anticoagulant activities of Bivalirudin.Tirofiban may increase the anticoagulant activities of Bivalirudin.Cilostazol may increase the anticoagulant activities of Bivalirudin.Defibrotide may increase the anticoagulant activities of Bivalirudin.Tinzaparin may increase the anticoagulant activities of Bivalirudin.Brinase may increase the anticoagulant activities of Bivalirudin.Saruplase may increase the anticoagulant activities of Bivalirudin.Streptokinase may increase the anticoagulant activities of Bivalirudin.Anagrelide may increase the anticoagulant activities of Bivalirudin.Rosiglitazone may increase the anticoagulant activities of Bivalirudin.Desmoteplase may increase the anticoagulant activities of Bivalirudin.Fibrinolysin may increase the anticoagulant activities of Bivalirudin.Caplacizumab may increase the anticoagulant activities of Bivalirudin.eplivanserine may increase the anticoagulant activities of Bivalirudin.Astaxanthin may increase the anticoagulant activities of Bivalirudin.Batroxobin may increase the anticoagulant activities of Bivalirudin.Ozagrel may increase the anticoagulant activities of Bivalirudin.Sarpogrelate may increase the anticoagulant activities of Bivalirudin.Eplivanserin may increase the anticoagulant activities of Bivalirudin.Eptifibatide may increase the anticoagulant activities of Bivalirudin.Treprostinil may increase the anticoagulant activities of Bivalirudin.Clopidogrel may increase the anticoagulant activities of Bivalirudin.Dipyridamole may increase the anticoagulant activities of Bivalirudin.Iloprost may increase the anticoagulant activities of Bivalirudin.Epoprostenol may increase the anticoagulant activities of Bivalirudin.Beraprost may increase the anticoagulant activities of Bivalirudin.Prasugrel may increase the anticoagulant activities of Bivalirudin.Cangrelor may increase the anticoagulant activities of Bivalirudin.Triflusal may increase the anticoagulant activities of Bivalirudin.Ticagrelor may increase the anticoagulant activities of Bivalirudin.Ditazole may increase the anticoagulant activities of Bivalirudin.Bemiparin may increase the anticoagulant activities of Bivalirudin.Parnaparin may increase the anticoagulant activities of Bivalirudin.Selexipag may increase the anticoagulant activities of Bivalirudin.Indobufen may increase the anticoagulant activities of Bivalirudin.Clorindione may increase the anticoagulant activities of Bivalirudin.Picotamide may increase the anticoagulant activities of Bivalirudin.Diphenadione may increase the anticoagulant activities of Bivalirudin.Cloricromen may increase the anticoagulant activities of Bivalirudin.Tioclomarol may increase the anticoagulant activities of Bivalirudin.Milrinone may increase the anticoagulant activities of Bivalirudin.Epinastine may increase the anticoagulant activities of Bivalirudin.Alprostadil may increase the anticoagulant activities of Bivalirudin.Pentoxifylline may increase the anticoagulant activities of Bivalirudin.Ridogrel may increase the anticoagulant activities of Bivalirudin.Sevoflurane may increase the anticoagulant activities of Bivalirudin.Tesmilifene may increase the anticoagulant activities of Bivalirudin.Ibudilast may increase the anticoagulant activities of Bivalirudin.Icosapent ethyl may increase the anticoagulant activities of Bivalirudin.Ifenprodil may increase the anticoagulant activities of Bivalirudin.Trapidil may increase the anticoagulant activities of Bivalirudin.Naftopidil may increase the anticoagulant activities of Bivalirudin.Ifetroban may increase the anticoagulant activities of Bivalirudin.Ketanserin may increase the anticoagulant activities of Bivalirudin.Butylphthalide may increase the anticoagulant activities of Bivalirudin.Hydroxytyrosol may increase the anticoagulant activities of Bivalirudin.Ramatroban may increase the anticoagulant activities of Bivalirudin.Linsidomine may increase the anticoagulant activities of Bivalirudin.Buflomedil may increase the anticoagulant activities of Bivalirudin.Relcovaptan may increase the anticoagulant activities of Bivalirudin.The serum concentration of Ambroxol acefyllinate can be decreased when it is combined with Bivalirudin.The serum concentration of Theophylline can be decreased when it is combined with Bivalirudin.The serum concentration of Dyphylline can be decreased when it is combined with Bivalirudin.The serum concentration of Aminophylline can be decreased when it is combined with Bivalirudin.The serum concentration of Valproic Acid can be decreased when it is combined with Bivalirudin.The serum concentration of Zidovudine can be decreased when it is combined with Bivalirudin.The risk or severity of adverse effects can be increased when Bivalirudin is combined with Azficel-T.The metabolism of Bivalirudin can be increased when combined with St. John's Wort.The serum concentration of Alfuzosin can be increased when it is combined with Bivalirudin.The risk or severity of bleeding can be increased when Bivalirudin is combined with Acemetacin.Apixaban may increase the anticoagulant activities of Bivalirudin.Edoxaban may increase the anticoagulant activities of Bivalirudin.Bivalirudin may increase the anticoagulant activities of Rivaroxaban.The serum concentration of Lovastatin can be increased when it is combined with Bivalirudin.Urokinase may increase the anticoagulant activities of Bivalirudin.The risk or severity of adverse effects can be increased when Vorapaxar is combined with Bivalirudin.The serum concentration of Midazolam can be increased when it is combined with Bivalirudin.The serum concentration of Simvastatin can be increased when it is combined with Bivalirudin.The serum concentration of Cabergoline can be increased when it is combined with Bivalirudin.The serum concentration of Bromocriptine can be increased when it is combined with Bivalirudin.The serum concentration of Dihydroergotamine can be increased when it is combined with Bivalirudin.The serum concentration of Ergotamine can be increased when it is combined with Bivalirudin.The serum concentration of Ergoloid mesylate can be increased when it is combined with Bivalirudin.The serum concentration of Ergonovine can be increased when it is combined with Bivalirudin.The serum concentration of Methylergometrine can be increased when it is combined with Bivalirudin.The serum concentration of Triazolam can be increased when it is combined with Bivalirudin.Hemin may increase the anticoagulant activities of Bivalirudin. 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Ethinyl EstradiolMestranolEstradiolEstrone sulfateSynthetic Conjugated Estrogens, AEstrogens, esterifiedChlorotrianiseneConjugated estrogensEstramustineDienestrolDiethylstilbestrolHexestrolMethallenestrilCyclosporineGarlicTacrolimusPethidineAlprazolamBoceprevirCarbamazepineClarithromycinDelavirdineEstronePolyestradiol phosphateGenisteinQuinestrolSynthetic Conjugated Estrogens, BZeranolEquolSecoisolariciresinolDaidzeinEpimestrolEstriolPromestrieneMoxestrolEstradiol acetateEstradiol cypionateEstradiol valerateOmacetaxine mepesuccinateNefazodoneAprotininTestosterone cypionateTestosterone enanthateAllylestrenolEtonogestrelMedroxyprogesterone acetateProgesteroneNorethisteroneHydroxyprogesterone caproateDesogestrelDydrogesteroneGestodeneAltrenogestGestrinoneMedrogestoneNomegestrolGestonoroneMethylestrenoloneNorgestrienonePromegestoneDemegestoneMegestrol acetateLevonorgestrelDienogestTestosterone undecanoateRiociguatSildenafilTemsirolimusDiltiazemVerapamilPentosan PolysulfateAmitriptylineProtriptylineImipramineNortriptylineTrimipramineDoxepinDesipramineClomipramineMirtazapineCyclobenzaprineAmineptineEsmirtazapineDosulepinTianeptineOpipramolDibenzepinLofepramineIprindoleAmoxapineAbacavirCyclophosphamideDigoxinEnfuvirtideEtravirineDasatinibDeferasiroxDeoxycholic AcidIbritumomab tiuxetanIbrutinibNintedanibObinutuzumabCollagenase clostridium histolyticumSugammadexLimaprostTiboloneKetorolacDiclofenacFlurbiprofenBromfenacNepafenacEtanerceptMasoprocolAdapaleneMesalazineIndomethacinPimecrolimusNabumetoneTenoxicamCelecoxibTolmetinRofecoxibPiroxicamFenoprofenValdecoxibSulindacChloroquineMycophenolate mofetilNaftifineZileutonEtodolacOlopatadineMefenamic acidNaproxenSulfasalazinePhenylbutazoneMeloxicamCarprofenDiflunisalSuprofenSalicylic acidMeclofenamic acidAcetylsalicylic acidAzelastineOxaprozinKetoprofenBalsalazideMycophenolic acidIbuprofenLeflunomideOlsalazineLumiracoxibMagnesium salicylateSalsalateCholine magnesium trisalicylateAntipyrineTiaprofenic acidEtoricoxibCastanospermineResveratrolOxyphenbutazoneNiflumic AcidNimesulideBenoxaprofenMetamizoleZomepiracPirfenidoneSRT501PTC299TarenflurbilApremilastAndrographolideIcatibantExisulindLornoxicamAceclofenacZaltoprofenSeratrodastAzapropazoneFelbinacTranilastFerulic acidParecoxibSalicylamideTeriflunomide(4R)-limoneneKebuzoneIsoxicamIndoprofenIbuproxamFloctafenineFenbufenEtofenamateEpirizoleLoxoprofenDroxicamTolfenamic AcidClonixinPropacetamolEvening primrose oilOrgoteinTepoxalinFlunixinCurcuminE-6201AnisodamineDuvelisibTriptolideSemapimodBucillamineLisofyllineNitroaspirinNafamostatMizoribineApocyninHigenamineTinoridineParthenolideSerrapeptaseAlclofenacFentiazacTribenosideSuxibuzoneBumadizoneAlminoprofenFlunoxaprofenBufexamacFeprazoneDifenpiramideNifenazoneLonazolacTenidapBendazacPranoprofenPropyphenazoneProglumetacinGuacetisalBevoniumEthenzamideCarbaspirin calciumMofebutazoneProquazoneBenorilatePirprofenImidazole salicylateBenzydamineTipranavirOmega-3 fatty acidsVitamin ETositumomabDabigatran etexilateLepirudinAbciximabBecaplerminDicoumarolArgatrobanArdeparinPhenindioneFondaparinux sodiumWarfarinPhenprocoumonEdetic AcidHeparinEnoxaparinAcenocoumarolCitric AcidXimelagatranAncrodPentaerythritol TetranitrateSulodexideIdraparinuxOtamixabanDanaparoidDalteparinEthyl biscoumacetateNadroparinDextranReviparinCertoparinDextran 70DesirudinDextran 40Dextran 75ProtocatechualdehydeProtein CAntithrombin III humanFondaparinuxLetaxabanDarexabanGabexateTroxerutinFluindioneProtein S humanMelagatranAminosalicylic AcidDersalazineAloxiprinHemoglobin crosfumarilMethyl salicylateTrolamine salicylateAlteplaseReteplaseAnistreplaseTenecteplaseDrotrecogin alfaTiclopidineTirofibanCilostazolDefibrotideTinzaparinBrinaseSaruplaseStreptokinaseAnagrelideRosiglitazoneDesmoteplaseFibrinolysinCaplacizumabeplivanserineAstaxanthinBatroxobinOzagrelSarpogrelateEplivanserinEptifibatideTreprostinilClopidogrelDipyridamoleIloprostEpoprostenolBeraprostPrasugrelCangrelorTriflusalTicagrelorDitazoleBemiparinParnaparinSelexipagIndobufenClorindionePicotamideDiphenadioneCloricromenTioclomarolMilrinoneEpinastineAlprostadilPentoxifyllineRidogrelSevofluraneTesmilifeneIbudilastIcosapent ethylIfenprodilTrapidilNaftopidilIfetrobanKetanserinButylphthalideHydroxytyrosolRamatrobanLinsidomineBuflomedilRelcovaptanAmbroxol acefyllinateTheophyllineDyphyllineAminophyllineValproic AcidZidovudineAzficel-TSt. John's WortAlfuzosinAcemetacinApixabanEdoxabanRivaroxabanLovastatinUrokinaseVorapaxarMidazolamSimvastatinCabergolineBromocriptineDihydroergotamineErgotamineErgoloid mesylateErgonovineMethylergometrineTriazolamHemin Dan shen, dong quai, evening primrose oil, gingko, policosanol, willow barkEchinacea B01AE06 Direct thrombin inhibitorsANTITHROMBOTIC AGENTSANTITHROMBOTIC AGENTSBLOOD AND BLOOD FORMING ORGANS B01AEB01AB01B Amino Acids, Peptides, and ProteinsAnti-coagulantAnticoagulantsAntithrombin ProteinsAntithrombinsBlood and Blood Forming OrgansChemical Actions and UsesEnzyme InhibitorsFibrinolytic AgentsHematologic AgentsMolecular Mechanisms of Pharmacological ActionPeptidesPharmacologic ActionsProtease InhibitorsProteinsSerine Proteinase InhibitorsSerpinsTherapeutic Uses D000602D000925D058833D000991D020164D004791D005343D006401D045504D010455D020228D011480D011506D015842D015843D045506 12945591731612970446507415D0313610482069PA10032DAP000542BivalirudinCHEMBL2103749 Drugs Product Database (DPD)ChEBIPubChem CompoundPubChem SubstanceKEGG DrugChemSpiderPharmGKBTherapeutic Targets DatabaseWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic/angiomax.htmhttp://www.drugs.com/cdi/bivalirudin.html //s3-us-west-2.amazonaws.com/drugbank/fda_labels/DB00006.pdf?1265922803 Seybert AL, Coons JC, Zerumsky K: Treatment of heparin-induced thrombocytopenia: is there a role for bivalirudin? Pharmacotherapy. 2006 Feb;26(2):229-41.Dager WE, Dougherty JA, Nguyen PH, Militello MA, Smythe MA: Heparin-induced thrombocytopenia: treatment options and special considerations. Pharmacotherapy. 2007 Apr;27(4):564-87.Dang CH, Durkalski VL, Nappi JM: Evaluation of treatment with direct thrombin inhibitors in patients with heparin-induced thrombocytopenia. Pharmacotherapy. 2006 Apr;26(4):461-8.Robson R: The use of bivalirudin in patients with renal impairment. J Invasive Cardiol. 2000 Dec;12 Suppl F:33F-6.Van De Car DA, Rao SV, Ohman EM: Bivalirudin: a review of the pharmacology and clinical application. Expert Rev Cardiovasc Ther. 2010 Dec;8(12):1673-81. doi: 10.1586/erc.10.158.Shammas NW: Bivalirudin: pharmacology and clinical applications. Cardiovasc Drug Rev. 2005 Winter;23(4):345-60.Gleason TG, Chengelis CP, Jackson CB, Lindstrom P: A 24-hour continuous infusion study of bivalirudin in the rat. Int J Toxicol. 2003 May-Jun;22(3):195-206. 16466327173813841655350311156732211085491661473312851152 approvedinvestigational Angiox Organic compounds Organic Polymers Polypeptides This compound belongs to the class of organic compounds known as polypeptides. These are peptides containing ten or more amino acid residues. Polypeptides 1-hydroxy-2-unsubstituted benzenoidsAlpha amino acid amidesAmino acidsAmphetamines and derivativesAralkylaminesAsparagine and derivativesAspartic acid and derivativesAzacyclic compoundsCarbonyl compoundsCarboximidamidesCarboxylic acidsGlutamic acid and derivativesGuanidinesHexacarboxylic acids and derivativesHydrocarbon derivativesIminesIsoleucine and derivativesLeucine and derivativesMonoalkylaminesN-acyl aminesN-acyl-L-alpha-amino acidsN-acylpyrrolidinesOrganic oxidesOrganopnictogen compoundsPeptidesPhenylalanine and derivativesPrimary carboxylic acid amidesProline and derivativesPyrrolidinecarboxamidesSecondary carboxylic acid amidesTertiary carboxylic acid amidesTyrosine and derivatives 1-hydroxy-2-unsubstituted benzenoidAlpha peptideAlpha-amino acid amideAlpha-amino acid or derivativesAmineAmino acidAmino acid or derivativesAmphetamine or derivativesAralkylamineAromatic heteromonocyclic compoundAsparagine or derivativesAspartic acid or derivativesAzacycleBenzenoidCarbonyl groupCarboxamide groupCarboximidamideCarboxylic acidCarboxylic acid derivativeFatty acylFatty amideGlutamic acid or derivativesGuanidineHexacarboxylic acid or derivativesHydrocarbon derivativeImineIsoleucine or derivativesLeucine or derivativesMonocyclic benzene moietyN-acyl-alpha amino acid or derivativesN-acyl-alpha-amino acidN-acyl-amineN-acyl-l-alpha-amino acidN-acylpyrrolidineN-substituted-alpha-amino acidOrganic nitrogen compoundOrganic oxideOrganic oxygen compoundOrganoheterocyclic compoundOrganonitrogen compoundOrganooxygen compoundOrganopnictogen compoundPhenolPhenylalanine or derivativesPolypeptidePrimary aliphatic aminePrimary aminePrimary carboxylic acid amideProline or derivativesPyrrolidinePyrrolidine carboxylic acid or derivativesPyrrolidine-2-carboxamideSecondary carboxylic acid amideTertiary carboxylic acid amideTyrosine or derivatives 5196404206515075983437582727 United StatesCanadaUnited StatesUnited States 1993-05-231999-12-142009-01-272009-01-27 2010-05-232010-08-172029-01-272029-01-27 falsefalsetruetrue drug_action DB00006DB01022DB01373 BivalirudinPhylloquinoneCalcium P00734P00748P02452P03952P03951P00740P00451P12259P00742P02671P02675P02679P00488P05160P00747P00750P08709P13726Q9BQB6P38435 Bivalirudin Action Pathway SMP00277 The medicines co false BivalirudinBivalirudinBivalirudinBivalirudinBivalirudinBivalirudinBivalirudinBivalirudinBivalirudinBivalirudinBivalirudinBivalirudinBivalirudinBivalirudin AngiomaxBivalirudin for InjectionAngiomaxBivalirudinBivalirudinAngiomaxBivalirudinBivalirudinBivalirudinBivalirudinBivalirudinBivalirudinBivalirudin in 0.9% Sodium ChlorideBivalirudin in 0.9% Sodium Chloride Ben Venue Laboratories Inc.Oryx Pharmaceuticals Inc.Sepracor Pharmaceuticals Inc.The Medicines Co. http://www.benvenue.comhttp://www.sepracor.comhttp://www.themedicinescompany.com AngiomaxAngiomaxAngiomaxBivalirudinBivalirudinBivalirudinBivalirudinBivalirudinBivalirudinBivalirudinBivalirudinBivalirudin for InjectionBivalirudin in 0.9% Sodium ChlorideBivalirudin in 0.9% Sodium Chloride falsefalsefalsetruefalsetruetruetruetruetruetruefalsefalsefalse Sandoz Canada IncorporatedThe Medicines CompanyCardinal HealthFresenius KabiSandoz Canada IncorporatedSandozDr Reddy's LaboratoriesSandozSagent PharmaceuticalsApotex CorporationHospira, Inc.Fresenius KabiBaxter LaboratoriesBaxter Laboratories falsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalse IntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntracavernousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenous Powder, for solutionInjection, powder, lyophilized, for solutionInjection, powder, lyophilized, for solutionInjection, powder, lyophilized, for solutionPowder, for solutionInjection, powder, lyophilized, for solutionInjectionInjection, powder, lyophilized, for solutionInjection, powder, lyophilized, for solutionInjection, powder, lyophilized, for solutionInjection, powder, lyophilized, for solutionPowder, for solutionInjectionInjection DPDFDA NDCFDA NDCFDA NDCDPDFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCDPDFDA NDCFDA NDC 250 mg250 mg/1250 mg/1250 mg/1250 mg250 mg/1250 mg/1250 mg/1250 mg/1250 mg/1250 mg/1250 mg250 mg/50mL500 mg/100mL 65293-00155154-227563323-5620781-315855111-6520781-915825021-40560505-61010409-83000338-95720338-9576 NDA020873NDA020873ANDA090189NDA020873ANDA201577NDA020873ANDA091602ANDA204876ANDA090811NDA208374NDA208374 truetruetruetruetruetruetruetruetruetruetruetruetruetrue 022465330245040202435268 CanadaUSUSUSCanadaUSUSUSUSUSUSCanadaUSUS 2003-05-082000-12-152000-12-152016-06-082015-06-152017-05-312015-10-232016-10-012017-07-172015-07-142017-12-212017-12-21 2017-10-26 vial 780.0 USD Angiomax 250 mg vial 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C98H138N24O33 3.177101336420163 2.7944312684415116 11.878406919439332 901.5700000000003 543.3342000000006 DB00007 53714-56-0 Leuprolide (D-Leu(6),des-gly-NH2(10),pro-ethylamide(9))-gonadotropin-releasing hormoneL-Pyroglutamyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-leucyl-L-leucyl-L-arginyl-L-proline ethylamideLeuprorelinLeuprorelinaLeuprorelineLeuprorelinumPGlu-his-trp-ser-tyr-D-leu-leu-arg-pro-NHC2H5PGlu-his-trp-ser-tyr-D-leu-leu-arg-pro-nhet biotech EFY6W0M8TG Daniel Kadzimirzs, Gerhard Jas, Volker Autze, "Solution-Phase Synthesis of Leuprolide and Its Intermediates." U.S. Patent US20090005535, issued January 01, 2009. liquid Leuprolide belongs to the general class of drugs known as hormones or hormone antagonists. It is a synthetic 9 residue peptide analog of gonadotropin releasing hormone. Leuprolide is used to treat advanced prostate cancer. It is also used to treat uterine fibroids and endometriosis. Leuprolide is also under investigation for possible use in the treatment of mild to moderate Alzheimer's disease. Humans and other mammals KitInjection, powder, for suspension, extended releaseInjection, powder, for suspension, extended releaseInjection, powder, for suspension, extended releaseInjection, powder, for suspension, extended releaseInjection, solutionKitKitLiquidInjection, powder, for suspension, extended releaseInjection, powder, for suspension, extended releaseInjection, powder, for suspension, extended releaseInjection, powder, for suspension, extended releaseInjection, powder, for suspension, extended releaseInjection, powder, for suspension, extended releaseInjection, powder, for suspension, extended release; kitInjection, powder, for suspension, extended release; kit SubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousIntramuscularIntramuscularIntramuscularIntramuscularIntramuscularIntramuscularIntramuscularIntramuscular 28.2 mg35.8 mg58.2 mg10.2 mg1 mg/.2mL5 mg11.25 mg15 mg22.5 mg3.75 mg30 mg7.5 mg28.13 mg5.06 mg For treatment of prostate cancer, endometriosis, uterine fibroids and premature puberty Leuprolide binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion. agonist Gonadotropin-releasing hormone receptor BE0000203 Human Castellon E, Clementi M, Hitschfeld C, Sanchez C, Benitez D, Saenz L, Contreras H, Huidobro C: Effect of leuprolide and cetrorelix on cell growth, apoptosis, and GnRH receptor expression in primary cell cultures from human prostate carcinoma. Cancer Invest. 2006 Apr-May;24(3):261-8.Borroni R, Di Blasio AM, Gaffuri B, Santorsola R, Busacca M, Vigano P, Vignali M: Expression of GnRH receptor gene in human ectopic endometrial cells and inhibition of their proliferation by leuprolide acetate. Mol Cell Endocrinol. 2000 Jan 25;159(1-2):37-43.Imai A, Takagi A, Horibe S, Takagi H, Tamaya T: Fas and Fas ligand system may mediate antiproliferative activity of gonadotropin-releasing hormone receptor in endometrial cancer cells. Int J Oncol. 1998 Jul;13(1):97-100.Murase M, Uemura T, Gao M, Inada M, Funabashi T, Hirahara F: GnRH antagonist-induced down-regulation of the mRNA expression of pituitary receptors: comparisons with GnRH agonist effects. Endocr J. 2005 Feb;52(1):131-7.Khurana KK, Singh SB, Tatum AH, Schulz V, Badawy SZ: Maintenance of increased Bcl-2 expression in uterine leiomyomas after GnRH agonist therapy. J Reprod Med. 1999 Jun;44(6):487-92. 168091531068785096258091575856910394541 P30968 Gonadotropin-releasing hormone receptor 4q21.2 Human membraneplasma membraneintegral component of plasma membranegonadotropin-releasing hormone receptor activitypeptide bindingG-protein coupled receptor signaling pathwaymulticellular organismal developmentcellular response to gonadotropin-releasing hormone Peptide binding Receptor for gonadotropin releasing hormone (GnRH) that mediates the action of GnRH to stimulate the secretion of the gonadotropic hormones luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This receptor mediates its action by association with G-proteins that activate a phosphatidylinositol-calcium second messenger system. Isoform 2 may act as an inhibitor of GnRH-R signaling. 43% to 49% In rats subcutaneous administration of 250 to 500 times the recommended human dose, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is a clinical counterpart of this phenomenon. In early clinical trials with leuprolide acetate doses as high as 20 mg/day for up to two years caused no adverse effects differing from those observed with the 1 mg/day dose. ~3 hours Bioavailability by subcutaneous administration is comparable to that by intravenous administration. Primarily degraded by peptidase and not by cytochrome P450 enzymes. * 8.34 L/h [healthy male receiving a 1-mg IV bolus] * 27 L [intravenous bolus administration to healthy male volunteers] Excretion in urine Used in the palliative treatment of advanced prostate cancer. Leuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis. Trastuzumab may increase the cardiotoxic activities of Leuprolide.Leuprolide may increase the QTc-prolonging activities of Goserelin.Leuprolide may increase the QTc-prolonging activities of Erythromycin.Leuprolide may increase the QTc-prolonging activities of Azithromycin.Leuprolide may increase the QTc-prolonging activities of Moxifloxacin.Leuprolide may increase the QTc-prolonging activities of Sulfisoxazole.Leuprolide may increase the QTc-prolonging activities of Methadone.Leuprolide may increase the QTc-prolonging activities of Clozapine.Leuprolide may increase the QTc-prolonging activities of Promazine.Leuprolide may increase the QTc-prolonging activities of Droperidol.Leuprolide may increase the QTc-prolonging activities of Chlorpromazine.Leuprolide may increase the QTc-prolonging activities of Haloperidol.Leuprolide may increase the QTc-prolonging activities of Ciprofloxacin.Leuprolide may increase the QTc-prolonging activities of Perflutren.Leuprolide may increase the QTc-prolonging activities of Chloroquine.Leuprolide may increase the QTc-prolonging activities of Pentamidine.Leuprolide may increase the QTc-prolonging activities of Gadobenic acid.Leuprolide may increase the QTc-prolonging activities of Dolasetron.Leuprolide may increase the QTc-prolonging activities of Granisetron.Leuprolide may increase the QTc-prolonging activities of Ondansetron.Leuprolide may increase the QTc-prolonging activities of Telithromycin.Leuprolide may increase the QTc-prolonging activities of Primaquine.Leuprolide may increase the QTc-prolonging activities of Levofloxacin.Leuprolide may increase the QTc-prolonging activities of Gemifloxacin.Leuprolide may increase the QTc-prolonging activities of Ofloxacin.Leuprolide may increase the QTc-prolonging activities of Propafenone.Leuprolide may increase the QTc-prolonging activities of Flecainide.Leuprolide may increase the QTc-prolonging activities of Clarithromycin.Leuprolide may increase the QTc-prolonging activities of Saquinavir.Leuprolide may increase the QTc-prolonging activities of Telavancin.Leuprolide may increase the QTc-prolonging activities of Pazopanib.Leuprolide may increase the QTc-prolonging activities of Panobinostat.Leuprolide may increase the QTc-prolonging activities of Crizotinib.Leuprolide may increase the QTc-prolonging activities of Bedaquiline.Leuprolide may increase the QTc-prolonging activities of Ceritinib.Leuprolide may increase the QTc-prolonging activities of Lenvatinib.The risk or severity of cytotoxicity can be increased when Ancestim is combined with Leuprolide.Ivabradine may increase the QTc-prolonging activities of Leuprolide.The risk or severity of adverse effects can be increased when Paclitaxel is combined with Leuprolide.The risk or severity of adverse effects can be increased when Docetaxel is combined with Leuprolide.The risk or severity of adverse effects can be increased when Cabazitaxel is combined with Leuprolide.Digoxin may decrease the cardiotoxic activities of Leuprolide.Acetyldigitoxin may decrease the cardiotoxic activities of Leuprolide.Deslanoside may decrease the cardiotoxic activities of Leuprolide.Ouabain may decrease the cardiotoxic activities of Leuprolide.Digitoxin may decrease the cardiotoxic activities of Leuprolide.Cymarin may decrease the cardiotoxic activities of Leuprolide.Proscillaridin may decrease the cardiotoxic activities of Leuprolide.Metildigoxin may decrease the cardiotoxic activities of Leuprolide.Peruvoside may decrease the cardiotoxic activities of Leuprolide.Lanatoside C may decrease the cardiotoxic activities of Leuprolide.Gitoformate may decrease the cardiotoxic activities of Leuprolide.Acetyldigoxin may decrease the cardiotoxic activities of Leuprolide.Oleandrin may decrease the cardiotoxic activities of Leuprolide.Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Leuprolide.Bevacizumab may increase the cardiotoxic activities of Leuprolide.Cyclophosphamide may increase the cardiotoxic activities of Leuprolide.Octreotide may increase the QTc-prolonging activities of Leuprolide.Oxytocin may increase the QTc-prolonging activities of Leuprolide.Bortezomib may increase the QTc-prolonging activities of Leuprolide.Fluconazole may increase the QTc-prolonging activities of Leuprolide.Nelfinavir may increase the QTc-prolonging activities of Leuprolide.Ranolazine may increase the QTc-prolonging activities of Leuprolide.Isradipine may increase the QTc-prolonging activities of Leuprolide.Venlafaxine may increase the QTc-prolonging activities of Leuprolide.Atomoxetine may increase the QTc-prolonging activities of Leuprolide.Amitriptyline may increase the QTc-prolonging activities of Leuprolide.Olanzapine may increase the QTc-prolonging activities of Leuprolide.Protriptyline may increase the QTc-prolonging activities of Leuprolide.Alfuzosin may increase the QTc-prolonging activities of Leuprolide.Mefloquine may increase the QTc-prolonging activities of Leuprolide.Mirtazapine may increase the QTc-prolonging activities of Leuprolide.Treprostinil may increase the QTc-prolonging activities of Leuprolide.Sorafenib may increase the QTc-prolonging activities of Leuprolide.Trimethoprim may increase the QTc-prolonging activities of Leuprolide.Imipramine may increase the QTc-prolonging activities of Leuprolide.Ritonavir may increase the QTc-prolonging activities of Leuprolide.Foscarnet may increase the QTc-prolonging activities of Leuprolide.Nortriptyline may increase the QTc-prolonging activities of Leuprolide.Amoxapine may increase the QTc-prolonging activities of Leuprolide.Hydroxyzine may increase the QTc-prolonging activities of Leuprolide.Voriconazole may increase the QTc-prolonging activities of Leuprolide.Nicardipine may increase the QTc-prolonging activities of Leuprolide.Trazodone may increase the QTc-prolonging activities of Leuprolide.Galantamine may increase the QTc-prolonging activities of Leuprolide.Tamoxifen may increase the QTc-prolonging activities of Leuprolide.Moexipril may increase the QTc-prolonging activities of Leuprolide.Tizanidine may increase the QTc-prolonging activities of Leuprolide.Ibandronate may increase the QTc-prolonging activities of Leuprolide.Apomorphine may increase the QTc-prolonging activities of Leuprolide.Paroxetine may increase the QTc-prolonging activities of Leuprolide.Trimipramine may increase the QTc-prolonging activities of Leuprolide.Risperidone may increase the QTc-prolonging activities of Leuprolide.Isoflurane may increase the QTc-prolonging activities of Leuprolide.Indapamide may increase the QTc-prolonging activities of Leuprolide.Propofol may increase the QTc-prolonging activities of Leuprolide.Vardenafil may increase the QTc-prolonging activities of Leuprolide.Terbutaline may increase the QTc-prolonging activities of Leuprolide.Amantadine may increase the QTc-prolonging activities of Leuprolide.Metronidazole may increase the QTc-prolonging activities of Leuprolide.Famotidine may increase the QTc-prolonging activities of Leuprolide.Maprotiline may increase the QTc-prolonging activities of Leuprolide.Salmeterol may increase the QTc-prolonging activities of Leuprolide.Felbamate may increase the QTc-prolonging activities of Leuprolide.Formoterol may increase the QTc-prolonging activities of Leuprolide.Salbutamol may increase the QTc-prolonging activities of Leuprolide.Sulfamethoxazole may increase the QTc-prolonging activities of Leuprolide.Ketoconazole may increase the QTc-prolonging activities of Leuprolide.Tolterodine may increase the QTc-prolonging activities of Leuprolide.Norfloxacin may increase the QTc-prolonging activities of Leuprolide.Promethazine may increase the QTc-prolonging activities of Leuprolide.Atazanavir may increase the QTc-prolonging activities of Leuprolide.Diphenhydramine may increase the QTc-prolonging activities of Leuprolide.Sertraline may increase the QTc-prolonging activities of Leuprolide.Doxepin may increase the QTc-prolonging activities of Leuprolide.Desipramine may increase the QTc-prolonging activities of Leuprolide.Itraconazole may increase the QTc-prolonging activities of Leuprolide.Desflurane may increase the QTc-prolonging activities of Leuprolide.Metoclopramide may increase the QTc-prolonging activities of Leuprolide.Sevoflurane may increase the QTc-prolonging activities of Leuprolide.Aripiprazole may increase the QTc-prolonging activities of Leuprolide.Clomipramine may increase the QTc-prolonging activities of Leuprolide.Dasatinib may increase the QTc-prolonging activities of Leuprolide.Lapatinib may increase the QTc-prolonging activities of Leuprolide.Posaconazole may increase the QTc-prolonging activities of Leuprolide.Sunitinib may increase the QTc-prolonging activities of Leuprolide.Arformoterol may increase the QTc-prolonging activities of Leuprolide.Lithium may increase the QTc-prolonging activities of Leuprolide.Methotrimeprazine may increase the QTc-prolonging activities of Leuprolide.Solifenacin may increase the QTc-prolonging activities of Leuprolide.Thiothixene may increase the QTc-prolonging activities of Leuprolide.Vorinostat may increase the QTc-prolonging activities of Leuprolide.Ezogabine may increase the QTc-prolonging activities of Leuprolide.Indacaterol may increase the QTc-prolonging activities of Leuprolide.Pasireotide may increase the QTc-prolonging activities of Leuprolide.Degarelix may increase the QTc-prolonging activities of Leuprolide.Buserelin may increase the QTc-prolonging activities of Leuprolide.Histrelin may increase the QTc-prolonging activities of Leuprolide.Triptorelin may increase the QTc-prolonging activities of Leuprolide.Rilpivirine may increase the QTc-prolonging activities of Leuprolide.Fingolimod may increase the QTc-prolonging activities of Leuprolide.Eribulin may increase the QTc-prolonging activities of Leuprolide.Mirabegron may increase the QTc-prolonging activities of Leuprolide.Dabrafenib may increase the QTc-prolonging activities of Leuprolide.Olodaterol may increase the QTc-prolonging activities of Leuprolide.Vilanterol may increase the QTc-prolonging activities of Leuprolide.The therapeutic efficacy of Choline C 11 can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Insulin Pork can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Troglitazone can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Glimepiride can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Acarbose can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Metformin can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Miglustat can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Miglitol can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Nateglinide can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Tolazamide can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Repaglinide can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Phenformin can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Glyburide can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Glipizide can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Gliclazide can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Tolbutamide can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Gliquidone can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Mitiglinide can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Sitagliptin can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Exenatide can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Pramlintide can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Leuprolide.The therapeutic efficacy of AICA ribonucleotide can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Castanospermine can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Buformin can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Voglibose can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Alogliptin can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Sulodexide can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Saxagliptin can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Liraglutide can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Linagliptin can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Canagliflozin can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Glibornuride can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Empagliflozin can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Dulaglutide can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Ciglitazone can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Allicin can be decreased when used in combination with Leuprolide.The therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Bempedoic acid can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Gusperimus can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Balaglitazone can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Deoxyspergualin can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Carbutamide can be decreased when used in combination with Leuprolide.Leuprolide may increase the QTc-prolonging activities of Dofetilide.Leuprolide may increase the QTc-prolonging activities of Citalopram.Leuprolide may increase the QTc-prolonging activities of Ziprasidone.Leuprolide may increase the QTc-prolonging activities of Anagrelide.Leuprolide may increase the QTc-prolonging activities of Disopyramide.Leuprolide may increase the QTc-prolonging activities of Ibutilide.Leuprolide may increase the QTc-prolonging activities of Quinine.Leuprolide may increase the QTc-prolonging activities of Fluoxetine.Leuprolide may increase the QTc-prolonging activities of Sotalol.Leuprolide may increase the QTc-prolonging activities of Toremifene.Leuprolide may increase the QTc-prolonging activities of Cisapride.Leuprolide may increase the QTc-prolonging activities of Thioridazine.Leuprolide may increase the QTc-prolonging activities of Mifepristone.Leuprolide may increase the QTc-prolonging activities of Flupentixol.Leuprolide may increase the QTc-prolonging activities of Quinidine.Leuprolide may increase the QTc-prolonging activities of Procainamide.Leuprolide may increase the QTc-prolonging activities of Pimozide.Leuprolide may increase the QTc-prolonging activities of Amiodarone.Leuprolide may increase the QTc-prolonging activities of Arsenic trioxide.Leuprolide may increase the QTc-prolonging activities of Escitalopram.Leuprolide may increase the QTc-prolonging activities of Domperidone.Leuprolide may increase the QTc-prolonging activities of Quetiapine.Leuprolide may increase the QTc-prolonging activities of Paliperidone.Leuprolide may increase the QTc-prolonging activities of Lopinavir.Leuprolide may increase the QTc-prolonging activities of Zuclopenthixol.Leuprolide may increase the QTc-prolonging activities of Tetrabenazine.Leuprolide may increase the QTc-prolonging activities of Dronedarone.Leuprolide may increase the QTc-prolonging activities of Nilotinib.Leuprolide may increase the QTc-prolonging activities of Iloperidone.Leuprolide may increase the QTc-prolonging activities of Vandetanib.Leuprolide may increase the QTc-prolonging activities of Asenapine.Leuprolide may increase the QTc-prolonging activities of Artemether.Leuprolide may increase the QTc-prolonging activities of Lumefantrine.Leuprolide may increase the QTc-prolonging activities of Vemurafenib.Leuprolide may increase the QTc-prolonging activities of Eliglustat.Leuprolide may decrease effectiveness of Capromab pendetide as a diagnostic agent. 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TrastuzumabGoserelinErythromycinAzithromycinMoxifloxacinSulfisoxazoleMethadoneClozapinePromazineDroperidolChlorpromazineHaloperidolCiprofloxacinPerflutrenChloroquinePentamidineGadobenic acidDolasetronGranisetronOndansetronTelithromycinPrimaquineLevofloxacinGemifloxacinOfloxacinPropafenoneFlecainideClarithromycinSaquinavirTelavancinPazopanibPanobinostatCrizotinibBedaquilineCeritinibLenvatinibAncestimIvabradinePaclitaxelDocetaxelCabazitaxelDigoxinAcetyldigitoxinDeslanosideOuabainDigitoxinCymarinProscillaridinMetildigoxinPeruvosideLanatoside CGitoformateAcetyldigoxinOleandrinDigoxin Immune Fab (Ovine)BevacizumabCyclophosphamideOctreotideOxytocinBortezomibFluconazoleNelfinavirRanolazineIsradipineVenlafaxineAtomoxetineAmitriptylineOlanzapineProtriptylineAlfuzosinMefloquineMirtazapineTreprostinilSorafenibTrimethoprimImipramineRitonavirFoscarnetNortriptylineAmoxapineHydroxyzineVoriconazoleNicardipineTrazodoneGalantamineTamoxifenMoexiprilTizanidineIbandronateApomorphineParoxetineTrimipramineRisperidoneIsofluraneIndapamidePropofolVardenafilTerbutalineAmantadineMetronidazoleFamotidineMaprotilineSalmeterolFelbamateFormoterolSalbutamolSulfamethoxazoleKetoconazoleTolterodineNorfloxacinPromethazineAtazanavirDiphenhydramineSertralineDoxepinDesipramineItraconazoleDesfluraneMetoclopramideSevofluraneAripiprazoleClomipramineDasatinibLapatinibPosaconazoleSunitinibArformoterolLithiumMethotrimeprazineSolifenacinThiothixeneVorinostatEzogabineIndacaterolPasireotideDegarelixBuserelinHistrelinTriptorelinRilpivirineFingolimodEribulinMirabegronDabrafenibOlodaterolVilanterolCholine C 11Insulin HumanInsulin LisproInsulin GlargineInsulin PorkTroglitazoneGlimepirideAcarboseMetforminRosiglitazoneAcetohexamideMiglustatMiglitolChlorpropamideNateglinideTolazamideRepaglinidePhenforminGlyburideGlipizideGliclazideTolbutamidePioglitazoneGliquidoneMitiglinideSitagliptinExenatidePramlintideInsulin AspartInsulin DetemirInsulin GlulisineAICA ribonucleotideCastanospermineBuforminVildagliptinVogliboseAlogliptinSulodexideSaxagliptinLiraglutideLinagliptinCanagliflozinGlibornurideEmpagliflozinDulaglutideCiglitazoneAllicin2,4-thiazolidinedioneBempedoic acidGusperimusSotagliflozinBalaglitazoneDeoxyspergualinCarbutamideDofetilideCitalopramZiprasidoneAnagrelideDisopyramideIbutilideQuinineFluoxetineSotalolToremifeneCisaprideThioridazineMifepristoneFlupentixolQuinidineProcainamidePimozideAmiodaroneArsenic trioxideEscitalopramDomperidoneQuetiapinePaliperidoneLopinavirZuclopenthixolTetrabenazineDronedaroneNilotinibIloperidoneVandetanibAsenapineArtemetherLumefantrineVemurafenibEliglustatCapromab pendetide HydrophobicityMolecular WeightMolecular Formula 0.11209.3983C59H84N16O12 L02AE02 Gonadotropin releasing hormone analoguesHORMONES AND RELATED AGENTSENDOCRINE THERAPYANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L02AEL02AL02L Amino Acids, Peptides, and ProteinsAntineoplastic AgentsAntineoplastic Agents, HormonalAntineoplastic and Immunomodulating AgentsChemical Actions and UsesEndocrine TherapyFertility AgentsFertility Agents, FemaleGonadotropin Releasing Hormone Receptor AgonistGonadotropin-Releasing HormoneHormonesHormones and Related AgentsHormones, Hormone Substitutes, and Hormone AntagonistsHyperglycemia-Associated AgentsHypothalamic HormonesModerate Risk QTc-Prolonging AgentsNerve Tissue ProteinsNeuropeptidesOligopeptidesPeptide HormonesPeptidesPharmacologic ActionsPhysiological Effects of DrugsPituitary Hormone-Releasing HormonesProteinsReproductive Control AgentsTherapeutic Uses D000602D000970D018931D020164D005299D005300D007987D006728D006730D007028D009419D009479D009842D036361D010455D020228D045505D010906D011506D012102D045506 1756642746507635C07612D08113PA450203DAP000020LeuprolideCHEMBL1201199 Drugs Product Database (DPD)ChEBIPubChem SubstanceKEGG CompoundKEGG DrugPharmGKBTherapeutic Targets DatabaseWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic/eligard.htmhttp://www.drugs.com/cdi/leuprolide.html //s3-us-west-2.amazonaws.com/drugbank/fda_labels/DB00007.pdf?1265922813 Saleh FM, Niel T, Fishman MJ: Treatment of paraphilia in young adults with leuprolide acetate: a preliminary case report series. J Forensic Sci. 2004 Nov;49(6):1343-8.Geier MR, Geier DA: The potential importance of steroids in the treatment of autistic spectrum disorders and other disorders involving mercury toxicity. Med Hypotheses. 2005;64(5):946-54.Doraiswamy PM, Xiong GL: Pharmacological strategies for the prevention of Alzheimer's disease. Expert Opin Pharmacother. 2006 Jan;7(1):1-10. 155687111578049016370917 approvedinvestigational TakedaBaxter/TevaCuraxisTakeda UKTakeda UKBayer AG EnantoneLeuplinLeuProMaxxLeupromerLutrateMemryteProstap 3Prostap SRViadur Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides 60369768921326742955988158015728396615633163759786235712611393861242616395292613242059853055932547656587467737146626870928328292543078486455884091684703599539333 United StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited States 1996-12-132011-02-051999-01-132002-06-281997-01-301997-01-301998-12-171997-06-131998-07-241997-06-131997-01-301997-01-301997-01-301997-06-131998-10-281998-10-282000-03-271998-10-281998-10-281998-10-282000-11-132003-10-152000-11-13 2016-12-132031-02-052019-01-132022-06-282017-01-302017-01-302018-12-172017-06-132018-07-242017-06-132017-01-302017-01-302017-01-302017-06-132018-10-282018-10-282020-03-272018-10-282018-10-282018-10-282020-11-132023-10-152020-11-13 falsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalse LeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolide + NorethisteroneLeuprolide + NorethisteroneLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolideLeuprolide EligardEligardEligardEligardLeuprolide AcetateLeuprolide AcetateLupron Depot-PEDLupron DepotLupron DepotLupron DepotLupron DepotLupron DepotEligard 7.5mgEligard 22.5mgEligard 30 mgLupronEligard 45 mgLeuprolide Acetate InjectionLupron DepotLupron DepotLeuprolide AcetateEligardEligardEligardEligardEligardEligardEligardEligardZeulide DepotZeulide DepotLupaneta PackLupaneta PackLupron Depot-PEDLupron Depot-PEDLupron Depot-PEDLupron DepotLupron DepotLupron DepotLupron DepotLupron DepotLupron DepotLupron Depot-PEDLupron Depot-PEDLeuprolide AcetateLeuprolide Acetate Abbott Laboratories Ltd.Cardinal HealthEon LabsHospira Inc.Oso Biopharmaceuticals Manufacturing LLCPhysicians Total Care Inc.Sanofi-Aventis Inc.Sun Pharmaceutical Industries Ltd.Takeda Pharmaceutical Co. Ltd.Teva Pharmaceutical Industries Ltd.Tolmar Inc. http://www.abbott.comhttp://www.cardinal.comhttp://www.hospira.comhttp://www.physicianstotalcare.comhttp://www.sanofi-aventis.comhttp://www.sunpharma.comhttp://www.takeda.comhttp://www.tevapharm.comhttp://www.tolmar.com EligardEligardEligardEligardEligardEligardEligardEligardEligardEligardEligardEligardEligard 22.5mgEligard 30 mgEligard 45 mgEligard 7.5mgLeuprolide AcetateLeuprolide AcetateLeuprolide AcetateLeuprolide AcetateLeuprolide AcetateLeuprolide Acetate InjectionLupaneta PackLupaneta PackLupronLupron DepotLupron DepotLupron DepotLupron DepotLupron DepotLupron DepotLupron DepotLupron DepotLupron DepotLupron DepotLupron DepotLupron DepotLupron DepotLupron Depot-PEDLupron Depot-PEDLupron Depot-PEDLupron Depot-PEDLupron Depot-PEDLupron Depot-PEDZeulide DepotZeulide Depot falsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsetruetruetruetruetruefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalse Sanofi AventisSanofi AventisSanofi AventisSanofi AventisTolmar IncTolmar IncTolmar IncTolmar IncTolmar IncTolmar IncTolmar IncTolmar IncSanofi AventisSanofi AventisSanofi AventisSanofi AventisEon Labs, Inc.Teva Parenteral Medicines, Inc.Sun Pharma Global Inc.SandozSun Pharma Global FZENovopharm LimitedAbbvieAbbvieAbbvieAbbvieAbbvieAbbvieAbbvieAbbvieAbbvieAbbvieAbbvieAbbvieAbbvieAbbvieAbbvieAbbvieAbbvieAbbvieAbbvieAbbvieAbbvieRemedy RepackPendopharm Division Of De Pharmascience IncPendopharm Division Of De Pharmascience Inc falsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalse SubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousIntramuscularIntramuscularIntramuscularIntramuscularIntramuscularIntramuscularIntramuscularIntramuscularIntramuscular KitKitKitKitKitKitKitKitKitKitKitKitInjection, powder, for suspension, extended releaseInjection, powder, for suspension, extended releaseInjection, powder, for suspension, extended releaseInjection, powder, for suspension, extended releaseInjection, solutionKitKitKitKitLiquidKitKitLiquidInjection, powder, for suspension, extended releaseInjection, powder, for suspension, extended releaseInjection, powder, for suspension, extended releaseInjection, powder, for suspension, extended releaseInjection, powder, for suspension, extended releaseInjection, powder, for suspension, extended releaseInjection, powder, for suspension, extended releaseKitKitKitKitKitKitKitKitKitKitKitKitInjection, powder, for suspension, extended release; KitInjection, powder, for suspension, extended release; Kit FDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCDPDDPDDPDDPDFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCDPDFDA NDCFDA NDCDPDDPDDPDDPDDPDDPDDPDDPDFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCDPDDPD 28.2 mg35.8 mg58.2 mg10.2 mg1 mg/.2mL5 mg5 mg22.5 mg3.75 mg7.5 mg11.25 mg15 mg30 mg11.25 mg5.06 mg28.13 mg 0024-02220024-06050024-06100024-079362935-22262935-22362935-30262935-30362935-45262935-45362935-75262935-7530185-74000703-401441616-9360781-400347335-9360074-10520074-10530074-33460074-34730074-36410074-36420074-36630074-36830074-21080074-22820074-24400074-37790074-969452125-736 NDA021379NDA021731NDA021488NDA021343NDA021379NDA021379NDA021488NDA021488NDA021731NDA021731NDA021343NDA021343ANDA074728ANDA075471ANDA078885ANDA074728ANDA078885NDA203696NDA203696NDA020517NDA020517NDA020011NDA019732NDA020708NDA020517NDA020263NDA020263NDA020263NDA020263NDA020263NDA020263 truetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetrue 022482400224899902268892022482390224026400727695022302480088450200836273021487220214873002239833022398340242997702462699 USUSUSUSUSUSUSUSUSUSUSUSCanadaCanadaCanadaCanadaUSUSUSUSUSCanadaUSUSCanadaCanadaCanadaCanadaCanadaCanadaCanadaCanadaUSUSUSUSUSUSUSUSUSUSUSUSCanadaCanada 2002-01-232002-01-232002-01-232002-01-232002-08-262002-08-262003-02-262003-02-262005-01-072005-01-072002-05-152002-05-152003-12-012004-04-292005-08-152003-12-011998-08-042000-11-062009-03-031998-08-042014-12-152013-07-012013-07-011985-12-311997-01-291992-12-311989-12-311999-09-131999-09-131995-12-221995-12-221990-10-221989-01-262010-11-081995-12-221993-04-161993-04-161993-04-161993-04-161993-04-162015-07-28 2016-10-132016-10-132016-10-132016-10-132016-12-162017-09-052016-12-28 kitboxsyringekitsyringesyringesyringe 385.33400.74493.2594.371479.61972.82959.2 USDUSDUSDUSDUSDUSDUSD Leuprolide 2wk 1 mg/0.2 ml kitLeuprolide Acetate 1 mg/0.2ml Kit 2.8ml 2-Week KitEligard 7.5 mg syringeLupron 2-wk 1 mg/0.2 ml kitEligard 22.5 mg syringeEligard 30 mg syringeEligard 45 mg syringe DB00008 198153-51-4 Peginterferon alfa-2a Pegylated interferon alfa-2aPegylated interferon alpha2a biotech Q46947FE7K liquid Peginterferon alfa-2a is a form of recombinant interferon used as part of combination therapy to treat chronic Hepatitis C, an infectious liver disease caused by infection with Hepatitis C Virus (HCV). HCV is a single-stranded RNA virus that is categorized into nine distinct genotypes, with genotype 1 being the most common in the United States, and affecting 72% of all chronic HCV patients [L852]. Treatment options for chronic Hepatitis C have advanced significantly since 2011, with the development of Direct Acting Antivirals (DAAs) resulting in less use of Peginterferon alfa-2a. Peginterferon alfa-2a is derived from the alfa-2a moeity of recombinant human interferon and acts by binding to human type 1 interferon receptors. Activation and dimerization of this receptor induces the body's innate antiviral response by activating the janus kinase/signal transducer and activator of transcription (JAK/STAT) pathway. Use of Peginterferon alfa-2a is associated with a wide range of severe adverse effects including the aggravation and development of endocrine and autoimmune disorders, retinopathies, cardiovascular and neuropsychiatric complications, and increased risk of hepatic decompensation in patients with cirrhosis. The use of Peginterferon alfa-2a has largely declined since newer interferon-free antiviral therapies have been developed.In a joint recommendation published in 2016, the American Association for the Study of Liver Diseases (AASLD) and the Infectious Diseases Society of America (IDSA) no longer recommend Peginterferon alfa-2a for the treatment of Hepatitis C [A19593]. Peginterferon alfa-2a was used alongside [DB00811] with the intent to cure, or achieve a sustained virologic response (SVR), after 48 weeks of therapy. SVR and eradication of HCV infection is associated with significant long-term health benefits including reduced liver-related damage, improved quality of life, reduced incidence of Hepatocellular Carcinoma, and reduced all-cause mortality [A19626].Peginterferon alfa-2a is available as a fixed dose injector (tradename Pegasys) used for the treatment of chronic Hepatitis C. Approved in 2002 by the FDA, Pegasys is indicated for the treatment of HCV with [DB00811] or other antiviral drugs [FDA Label]. When combined together, Peginterferon alfa-2a and [DB00811] have been shown to achieve a SVR between 36% for genotype 1 and 59% for genotypes 2-6 after 48 weeks of treatment. Humans and other mammals Injection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionSolutionSolution; tablet SubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousOral; Subcutaneous 135 ug/.5mL135 μg180 ug/mL180 ug/.5mL180 μg90 μg180 mcg Peginterferon alfa-2a is indicated for the treatment of HCV in combination with other antiviral drugs in patients over 5 years of age with compensated liver disease [FDA Label]. May be used as a monotherapy in patients with contraindications to or significant intolerance to other anti-viral therapies.Peginterferon alfa-2a is also indicated as a monotherapy for adult patients with HBeAg positive and HBeAg negative chronic hepatitis B infection who havecompensated liver disease and evidence of viral replication and liver inflammation [FDA Label]. Peginterferon alfa-2a is derived from recombinant human interferon's alfa-2a moeity [FDA Label]. It binds to and activates human type 1 interferon receptors causing them to dimerize. This activates the JAK/STAT pathway. Activation of the JAK/STAT pathway increases expression of multiple genes in multiple tissues involved in the innate antiviral response. agonistagonist Interferon alpha/beta receptor 2Interferon alpha/beta receptor 1 BE0000385BE0000661 HumanHuman Dhalluin C, Ross A, Huber W, Gerber P, Brugger D, Gsell B, Senn H: Structural, kinetic, and thermodynamic analysis of the binding of the 40 kDa PEG-interferon-alpha2a and its individual positional isomers to the extracellular domain of the receptor IFNAR2. Bioconjug Chem. 2005 May-Jun;16(3):518-27.Yano H, Ogasawara S, Momosaki S, Akiba J, Kojiro S, Fukahori S, Ishizaki H, Kuratomi K, Basaki Y, Oie S, Kuwano M, Kojiro M: Growth inhibitory effects of pegylated IFN alpha-2b on human liver cancer cells in vitro and in vivo. Liver Int. 2006 Oct;26(8):964-75.Ishii K, Shinohara M, Sawa M, Kogame M, Higami K, Sano M, Morita T, Sumino Y: Interferon alpha receptor 2 expression by peripheral blood monocytes in patients with a high viral load of hepatitis C virus genotype 1 showing substitution of amino Acid 70 in the core region. Intervirology. 2010;53(2):105-10. doi: 10.1159/000264200. Epub 2009 Dec 3.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.Dhalluin C, Ross A, Huber W, Gerber P, Brugger D, Gsell B, Senn H: Structural, kinetic, and thermodynamic analysis of the binding of the 40 kDa PEG-interferon-alpha2a and its individual positional isomers to the extracellular domain of the receptor IFNAR2. Bioconjug Chem. 2005 May-Jun;16(3):518-27.Yano H, Ogasawara S, Momosaki S, Akiba J, Kojiro S, Fukahori S, Ishizaki H, Kuratomi K, Basaki Y, Oie S, Kuwano M, Kojiro M: Growth inhibitory effects of pegylated IFN alpha-2b on human liver cancer cells in vitro and in vivo. Liver Int. 2006 Oct;26(8):964-75.Ishii K, Shinohara M, Sawa M, Kogame M, Higami K, Sano M, Morita T, Sumino Y: Interferon alpha receptor 2 expression by peripheral blood monocytes in patients with a high viral load of hepatitis C virus genotype 1 showing substitution of amino Acid 70 in the core region. Intervirology. 2010;53(2):105-10. doi: 10.1159/000264200. Epub 2009 Dec 3.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. 1589871716953837199558151175235215898717169538371995581511752352 P48551P17181 Interferon alpha/beta receptor 2Interferon alpha/beta receptor 1 HumanHuman intracellularextracellular regionplasma membraneextracellular spaceintegral component of plasma membraneprotein kinase bindingtype I interferon bindingtype I interferon receptor activityJAK-STAT cascaderegulation of transcription from RNA polymerase II promoterregulation of type I interferon-mediated signaling pathwayresponse to interferon-alphacell proliferationresponse to virustype I interferon signaling pathwaycell surface receptor signaling pathwaycytokine-mediated signaling pathwayintracellularplasma membraneintegral component of plasma membranetype I interferon receptor activityregulation of type I interferon-mediated signaling pathwayresponse to virustype I interferon signaling pathwaypositive regulation of transcription, DNA-templateddefense response to viruscell surface receptor signaling pathwaypositive regulation of interleukin-1 beta secretioncytokine-mediated signaling pathwaypositive regulation of interferon-beta productionregulation of peptidyl-tyrosine phosphorylationtype I interferon biosynthetic processpositive regulation of interferon-gamma productionT cell activationJAK-STAT cascade Type i interferon receptor activityType i interferon receptor activity Associates with IFNAR1 to form the type I interferon receptor. Receptor for interferons alpha and beta. Involved in IFN-mediated STAT1, STAT2 and STAT3 activation. Isoform 1 and isoform 2 are directly involved in signal transduction due to their association with the TYR kinase, JAK1. Isoform 3 is a potent inhibitor of type I IFN receptor activity.Associates with IFNAR2 to form the type I interferon receptor. Receptor for interferons alpha and beta. Binding to type I IFNs triggers tyrosine phosphorylation of a number of proteins including JAKs, TYK2, STAT proteins and IFNR alpha- and beta-subunits themselves. Can also transduce IFNB signals without the help of IFNAR2, and not activating the Jak-STAT pathway. Peginterferon alfa-2a may manifest neuropsychiatric complications include suicide, suicidal ideation, homicidal ideation, depression, relapse of drug addiction, and drug overdose [FDA Label]. Hypertension, supraventricular arrhythmias, chest pain, and myocardial infarction have been observed in patients using Peginterferon alfa-2a. Peginterferon alfa-2a may produce myelosuppression as well as the development or aggravation of autoimmune disorders including myositis, hepatitis, thrombotic thrombocytopenic purpura, idiopathic thrombocytopenic purpura, psoriasis, rheumatoid arthritis, interstitial nephritis, thyroiditis, and systemic lupus erythematosus. Peginterferon alfa-2a causes or aggravates hypothyroidism and hyperthyroidism. Hyperglycemia, hypoglycemia, and diabetes mellitus have been observed to develop in patients treated with Peginterferon alfa-2a. Peginterferon alfa-2a may decrease or produce loss of vision, retinopathy including macular edema, retinal artery or vein thrombosis, retinal hemorrhages and cotton wool spots, optic neuritis, papilledema and serous retinal detachment. Peginterferon mayy be related to increased ischemic and hemorrhagic cerebrovascular events. Patients with cirrhosis on Peginterferon alfa-2a are at risk of hepatic decompensation. Dyspnea, pulmonary infiltrates, pneumonia, bronchiolitis obliterans, interstitial pneumonitis, pulmonary hypertension and sarcoidosis may be induced or aggravated by Peginterferon alfa-2a. Serious and severe infections (bacterial, viral, or fungal) have been reported during treatment with Peginterferon alfa-2a. Ulcerative and hemorrhagic/ischemic colitis have been observed within 12 weeks of starting Peginterferon alfa-2a treatment. Pancreatitis and peripheral nephropathy have also been reported. Peginterferon alfa-2a is associated with growth inhibition in pediatric patients. Use of Peginterferon alfa-2a while pregant may result in delopmental abnormalities or death of the fetus. The mean terminal half-life of peginterferon alfa-2a is 164 in a range of 84-353 hours [FDA Label]. Peginterferon alfa-2a reaches peak plasma concentration 72-96 hours after subcutaneous administration [FDA Label]. Trough concentrations at week 48 are approximately 2 fold higher than week 1. The peak to trough ratio at week 48 is 2. The mean systemic clearance of peginterferon alfa-2a is 94 milliliters per hour [FDA Label]. Peginterferon alfa-2a induces the body's innate antiviral response [FDA Label]. The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Aldesleukin.The serum concentration of Tizanidine can be increased when it is combined with Peginterferon alfa-2a.The therapeutic efficacy of Peginterferon alfa-2a can be decreased when used in combination with Pegloticase.The metabolism of Ambroxol acefyllinate can be decreased when combined with Peginterferon alfa-2a.The metabolism of Theophylline can be decreased when combined with Peginterferon alfa-2a.The metabolism of Dyphylline can be decreased when combined with Peginterferon alfa-2a.The metabolism of Aminophylline can be decreased when combined with Peginterferon alfa-2a.The serum concentration of Methadone can be increased when it is combined with Peginterferon alfa-2a.The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Ribavirin.The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Zidovudine.The risk or severity of myelosuppression can be increased when Metamizole is combined with Peginterferon alfa-2a.The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Clozapine.The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Telbivudine. DB00041DB00697DB09208DB13141DB00277DB00651DB01223DB00333DB00811DB00495DB04817DB00363DB01265 AldesleukinTizanidinePegloticaseAmbroxol acefyllinateTheophyllineDyphyllineAminophyllineMethadoneRibavirinZidovudineMetamizoleClozapineTelbivudine Recommended adequate hydration. Melting PointIsoelectric PointMolecular Weight 61 °C5.9960000.0 Beldarrain, A. et al., Biochemistry 38:7865-7873 (1999) L03AB61L03AB11 InterferonsIMMUNOSTIMULANTSIMMUNOSTIMULANTSANTINEOPLASTIC AND IMMUNOMODULATING AGENTSInterferonsIMMUNOSTIMULANTSIMMUNOSTIMULANTSANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L03ABL03AL03LL03ABL03AL03L Adjuvants, ImmunologicAlcoholsAlfa InterferonsAmino Acids, Peptides, and ProteinsAnti-Infective AgentsAntineoplastic and Immunomodulating AgentsAntiviral AgentsBiological FactorsBiomedical and Dental MaterialsChemical Actions and UsesCytochrome P-450 CYP1A2 InhibitorsCytochrome P-450 CYP1A2 Inhibitors (weak)Cytochrome P-450 Enzyme InhibitorsCytokinesDrug CarriersEthylene GlycolsGlycolsIntercellular Signaling Peptides and ProteinsInterferon alphaInterferon Type IInterferonsMacromolecular SubstancesManufactured MaterialsMyelosuppressive AgentsOrganic ChemicalsPeptidesPharmacologic ActionsPolymersProteinsSpecialty Uses of ChemicalsTechnology, Industry, and AgricultureTherapeutic Uses D000276D000438D000602D000890D000998D001685D001697D020164D065609D065607D016207D004337D005026D006018D036341D016898D007370D007372D046911D008420D009930D010455D020228D011108D011506D020313D013676D045506 1324646504860J00207PA164749390P01563DAP001278Peginterferon_alfa-2aCHEMBL1201560 Drugs Product Database (DPD)PubChem SubstanceGenBankPharmGKBUniProtKBTherapeutic Targets DatabaseWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic3/pegasys.htmhttp://www.drugs.com/cdi/peginterferon-alfa-2a.html //s3-us-west-2.amazonaws.com/drugbank/fda_labels/DB00008.pdf?1497564068 Bagaglio S, Uberti-Foppa C, Morsica G: Resistance Mechanisms in Hepatitis C Virus: implications for Direct-Acting Antiviral Use. Drugs. 2017 May 12. doi: 10.1007/s40265-017-0753-x.Myers RP, Shah H, Burak KW, Cooper C, Feld JJ: An update on the management of chronic hepatitis C: 2015 Consensus guidelines from the Canadian Association for the Study of the Liver. Can J Gastroenterol Hepatol. 2015 Jan-Feb;29(1):19-34. Epub 2015 Jan 13. 2849743225585348 approvedinvestigational Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides 21726642203480 CanadaCanada 2000-10-032009-06-30 2016-03-262017-04-23 falsefalse Peginterferon alfa-2aPeginterferon alfa-2aPeginterferon alfa-2aPeginterferon alfa-2aPeginterferon alfa-2aPeginterferon alfa-2aPeginterferon alfa-2aPeginterferon alfa-2aPeginterferon alfa-2aPeginterferon alfa-2aPeginterferon alfa-2aPeginterferon alfa-2aPeginterferon alfa-2aPeginterferon alfa-2aPeginterferon alfa-2aPeginterferon alfa-2aPeginterferon alfa-2aPeginterferon alfa-2aPeginterferon alfa-2aPeginterferon alfa-2a + RibavirinPeginterferon alfa-2a + RibavirinPeginterferon alfa-2aPeginterferon alfa-2aPeginterferon alfa-2aPeginterferon alfa-2a PegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasys RbvPegasys RbvPegasysPegasysPegasysPegasys F Hoffmann La Roche Ltd.F Hoffmann-La Roche Ltd. http://www.roche.comhttp://www.roche.com PegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasysPegasys RbvPegasys Rbv falsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalse Hoffmann La RocheRoche Registration Gmb HRoche Registration Gmb HRoche Registration Gmb HRoche Registration Gmb HRoche Registration Gmb HRoche Registration Gmb HRoche Registration Gmb HRoche Registration Gmb HRoche Registration Gmb HRoche Registration Gmb HRoche Registration Gmb HRoche Registration Gmb HRoche Registration Gmb HRoche Registration Gmb HRoche Registration Gmb HRoche Registration Gmb HRoche Registration Gmb HHoffmann La RocheGenentech, Inc.Genentech, Inc.Genentech, Inc.Genentech, Inc.Hoffmann La RocheHoffmann La Roche falsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalse SubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousOral; SubcutaneousOral; Subcutaneous SolutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionSolutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionSolution; TabletSolution; Tablet DPDEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMADPDFDA NDCFDA NDCFDA NDCFDA NDCDPDDPD 180 mcg135 μg135 μg180 μg180 μg135 μg135 μg180 μg180 μg135 μg180 μg135 μg135 μg135 μg180 μg180 μg180 μg90 μg180 mcg180 ug/mL180 ug/.5mL135 ug/.5mL180 ug/.5mL 0004-03500004-03570004-03600004-0365 BLA103964BLA103964BLA103964BLA103964 truetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetrue 02248077022480780225341002253429 CanadaEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUCanadaUSUSUSUSCanadaCanada 2003-08-142002-06-202002-06-202002-06-202002-06-202002-06-202002-06-202002-06-202002-06-202002-06-202002-06-202002-06-202002-06-202002-06-202002-06-202002-06-202002-06-202002-06-202003-08-142002-10-162011-03-292011-11-012011-11-012004-05-262004-05-26 2017-07-27 mleachbox 642.642533.22634.53 USDUSDUSD Pegasys 180 mcg/ml vialPegasys 180 mcg/0.5 ml conv.pkPegasys (1 Kit = Four 180 mcg/ml Vials Prefilled Syringes) Box DB00009 105857-23-6 Alteplase Alteplase (genetical recombination)Alteplase, recombinantAlteplase,recombinantPlasminogen activator (human tissue-type protein moiety)rt-PAt-PAt-plasminogen activatorTissue plasminogen activatorTissue plasminogen activator alteplaseTissue plasminogen activator, recombinanttPA biotech 1RXS4UE564 liquid Human tissue plasminogen activator, purified, glycosylated, 527 residues purified from CHO cells Humans and other mammals KitLiquid; powder, for solutionPowder, for solutionPowder, for solutionInjection, powder, lyophilized, for solutionPowder, for solution IntravenousIntravenousIntravenousIntravenous 29 m2 mg2.2 mg/2mL For management of acute myocardial infarction, acute ischemic strok and for lysis of acute pulmonary emboli Alteplase binds to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain. The protease domain then cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. activator PlasminogenFibrinogen alpha chainUrokinase plasminogen activator surface receptorPlasminogen activator inhibitor 1 BE0000211BE0000538BE0000717BE0000240 HumanHumanHumanHuman Longstaff C, Williams S, Thelwell C: Fibrin binding and the regulation of plasminogen activators during thrombolytic therapy. Cardiovasc Hematol Agents Med Chem. 2008 Jul;6(3):212-23.Melandri G, Vagnarelli F, Calabrese D, Semprini F, Nanni S, Branzi A: Review of tenecteplase (TNKase) in the treatment of acute myocardial infarction. Vasc Health Risk Manag. 2009;5(1):249-56. Epub 2009 Apr 8.Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.Longstaff C, Williams S, Thelwell C: Fibrin binding and the regulation of plasminogen activators during thrombolytic therapy. Cardiovasc Hematol Agents Med Chem. 2008 Jul;6(3):212-23.Melandri G, Vagnarelli F, Calabrese D, Semprini F, Nanni S, Branzi A: Review of tenecteplase (TNKase) in the treatment of acute myocardial infarction. Vasc Health Risk Manag. 2009;5(1):249-56. Epub 2009 Apr 8.Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70. 18673235194366561796346411752352186732351943665617963464171392841701642317963464 P00747P02671Q03405P05121 PlasminogenFibrinogen alpha chainUrokinase plasminogen activator surface receptorPlasminogen activator inhibitor 1 6q264q2819q137q21.3-q22 HumanHumanHumanHuman extracellular exosomeextrinsic component of external side of plasma membraneextracellular regionplasma membraneplatelet alpha granule lumenextracellular spaceblood microparticlecell surfaceapolipoprotein bindingserine-type endopeptidase activityreceptor bindingserine-type peptidase activityprotein domain specific bindingnegative regulation of fibrinolysisblood coagulationextracellular matrix disassemblyproteolysisextracellular matrix organizationpositive regulation of fibrinolysisnegative regulation of cell-substrate adhesiontissue remodelingcellular protein metabolic processnegative regulation of cell-cell adhesion mediated by cadherinnegative regulation of cell proliferationplatelet degranulationfibrinolysisplatelet activationblood microparticlerough endoplasmic reticulumextracellular exosomecell cortexexternal side of plasma membraneextracellular regionplasma membraneextracellular spacecell surfaceextracellular vesicleplatelet alpha granuleplatelet alpha granule lumenfibrinogen complexstructural molecule activityplatelet degranulationsignal transductionresponse to cycloheximideprotein complex assemblycellular protein complex assemblypositive regulation of peptide hormone secretionacute-phase responseprotein polymerizationpositive regulation of substrate adhesion-dependent cell spreadinginnate immune responsefibrinolysisblood coagulationadaptive immune responseliver regenerationresponse to calcium ionpositive regulation of protein secretionresponse to genisteinextracellular matrix organizationplatelet aggregationcellular response to organic cyclic compoundresponse to estradiolinduction of bacterial agglutinationpositive regulation of vasoconstrictioncell-matrix adhesionplasminogen activationcellular protein metabolic processblood coagulation, common pathwaypositive regulation of ERK1 and ERK2 cascadecellular response to interleukin-6negative regulation of extrinsic apoptotic signaling pathway via death domain receptorscellular response to granulocyte colony-stimulating factornegative regulation of endothelial cell apoptotic processpositive regulation of exocytosisnegative regulation of blood coagulation, common pathwaypositive regulation of heterotypic cell-cell adhesionplatelet activationresponse to morphineblood coagulation, fibrin clot formationintegral component of plasma membraneendoplasmic reticulum lumenanchored component of membraneplasma membraneextrinsic component of membraneendoplasmic reticulum membraneinvadopodium membranefocal adhesionintegral component of membraneextracellular exosomereceptor activityreceptor bindingprotein domain specific bindingurokinase plasminogen activator receptor activityenzyme bindingnegative regulation of intrinsic apoptotic signaling pathwayurokinase plasminogen activator signaling pathwaypositive regulation of protein phosphorylationpositive regulation of DNA bindingsignal transductionpositive regulation of epidermal growth factor receptor signaling pathwayblood coagulationpositive regulation of release of cytochrome c from mitochondriacellular protein metabolic processnegative regulation of apoptotic processpost-translational protein modificationfibrinolysisregulation of proteolysischemotaxismovement of cell or subcellular componentattachment of GPI anchor to proteinnegative regulation of cysteine-type endopeptidase activity involved in apoptotic signaling pathwayC-terminal protein lipidationextracellular matrixextracellular regionplatelet alpha granule lumenplasma membraneextracellular spaceextracellular exosomeprotease bindingreceptor bindingserine-type endopeptidase inhibitor activityangiogenesisnegative regulation of smooth muscle cell migrationextracellular matrix organizationtransforming growth factor beta receptor signaling pathwaycellular response to lipopolysaccharideblood coagulationnegative regulation of smooth muscle cell-matrix adhesionnegative regulation of extrinsic apoptotic signaling pathway via death domain receptorsnegative regulation of endopeptidase activitynegative regulation of vascular wound healingpositive regulation of transcription from RNA polymerase II promoternegative regulation of wound healingchronological cell agingpositive regulation of angiogenesisplatelet degranulationdefense response to Gram-negative bacteriumpositive regulation of interleukin-8 productionfibrinolysisnegative regulation of blood coagulationpositive regulation of leukotriene production involved in inflammatory responsenegative regulation of fibrinolysisnegative regulation of cell adhesion mediated by integrinpositive regulation of monocyte chemotaxisplatelet activationpositive regulation of blood coagulationnegative regulation of cell migrationpositive regulation of receptor-mediated endocytosisgene expressionpositive regulation of inflammatory responsenegative regulation of endothelial cell apoptotic processtranscription initiation from RNA polymerase II promoterregulation of receptor activitycircadian rhythmnegative regulation of plasminogen activationtranscription, DNA-templated Serine-type peptidase activityStructural molecule activityUrokinase plasminogen activator receptor activitySerine-type endopeptidase inhibitor activity Plasmin dissolves the fibrin of blood clots and acts as a proteolytic factor in a variety of other processes including embryonic development, tissue remodeling, tumor invasion, and inflammation. In ovulation, weakens the walls of the Graafian follicle. It activates the urokinase-type plasminogen activator, collagenases and several complement zymogens, such as C1 and C5. Cleavage of fibronectin and laminin leads to cell detachment and apoptosis. Also cleaves fibrin, thrombospondin and von Willebrand factor. Its role in tissue remodeling and tumor invasion may be modulated by CSPG4. Binds to cells.Angiostatin is an angiogenesis inhibitor that blocks neovascularization and growth of experimental primary and metastatic tumors in vivo.Cleaved by the protease thrombin to yield monomers which, together with fibrinogen beta (FGB) and fibrinogen gamma (FGG), polymerize to form an insoluble fibrin matrix. Fibrin has a major function in hemostasis as one of the primary components of blood clots. In addition, functions during the early stages of wound repair to stabilize the lesion and guide cell migration during re-epithelialization. Was originally thought to be essential for platelet aggregation, based on in vitro studies using anticoagulated blood. However, subsequent studies have shown that it is not absolutely required for thrombus formation in vivo. Enhances expression of SELP in activated platelets via an ITGB3-dependent pathway. Maternal fibrinogen is essential for successful pregnancy. Fibrin deposition is also associated with infection, where it protects against IFNG-mediated hemorrhage. May also facilitate the immune response via both innate and T-cell mediated pathways.Acts as a receptor for urokinase plasminogen activator. Plays a role in localizing and promoting plasmin formation. Mediates the proteolysis-independent signal transduction activation effects of U-PA. It is subject to negative-feedback regulation by U-PA which cleaves it into an inactive form.Serine protease inhibitor. This inhibitor acts as 'bait' for tissue plasminogen activator, urokinase, protein C and matriptase-3/TMPRSS7. Its rapid interaction with PLAT may function as a major control point in the regulation of fibrinolysis. Alteplase binds to fibrin in a thrombus and converts the entrapped plasminogen to plasmin. It also produces limited conversion of plasminogen in the absence of fibrin. The therapeutic efficacy of Alteplase can be decreased when used in combination with Aprotinin.The risk or severity of adverse effects can be increased when Limaprost is combined with Alteplase.Alteplase may increase the anticoagulant activities of Dabigatran etexilate.The serum concentration of Alteplase can be decreased when it is combined with Nitroglycerin.Alteplase may increase the anticoagulant activities of Lepirudin.Alteplase may increase the anticoagulant activities of Bivalirudin.Alteplase may increase the anticoagulant activities of Abciximab.Alteplase may increase the anticoagulant activities of Becaplermin.Alteplase may increase the anticoagulant activities of Dicoumarol.Alteplase may increase the anticoagulant activities of Argatroban.Alteplase may increase the anticoagulant activities of Ardeparin.Alteplase may increase the anticoagulant activities of Phenindione.Alteplase may increase the anticoagulant activities of Fondaparinux sodium.Alteplase may increase the anticoagulant activities of Warfarin.Alteplase may increase the anticoagulant activities of Pentosan Polysulfate.Alteplase may increase the anticoagulant activities of Phenprocoumon.Alteplase may increase the anticoagulant activities of Edetic Acid.Alteplase may increase the anticoagulant activities of Heparin.Alteplase may increase the anticoagulant activities of Enoxaparin.Alteplase may increase the anticoagulant activities of Acenocoumarol.Alteplase may increase the anticoagulant activities of Citric Acid.Alteplase may increase the anticoagulant activities of Ximelagatran.Alteplase may increase the anticoagulant activities of Ancrod.Alteplase may increase the anticoagulant activities of Pentaerythritol Tetranitrate.Alteplase may increase the anticoagulant activities of Rivaroxaban.Alteplase may increase the anticoagulant activities of Sulodexide.Alteplase may increase the anticoagulant activities of Idraparinux.Alteplase may increase the anticoagulant activities of Apixaban.Alteplase may increase the anticoagulant activities of Otamixaban.Alteplase may increase the anticoagulant activities of Danaparoid.Alteplase may increase the anticoagulant activities of Dalteparin.Alteplase may increase the anticoagulant activities of Ferulic acid.Alteplase may increase the anticoagulant activities of Ethyl biscoumacetate.Alteplase may increase the anticoagulant activities of Nadroparin.Alteplase may increase the anticoagulant activities of Edoxaban.Alteplase may increase the anticoagulant activities of Dextran.Alteplase may increase the anticoagulant activities of Reviparin.Alteplase may increase the anticoagulant activities of Certoparin.Alteplase may increase the anticoagulant activities of Dextran 70.Alteplase may increase the anticoagulant activities of Desirudin.Alteplase may increase the anticoagulant activities of Dextran 40.Alteplase may increase the anticoagulant activities of Dextran 75.Alteplase may increase the anticoagulant activities of Protocatechualdehyde.Alteplase may increase the anticoagulant activities of Protein C.Alteplase may increase the anticoagulant activities of Antithrombin III human.Alteplase may increase the anticoagulant activities of Fondaparinux.Alteplase may increase the anticoagulant activities of Letaxaban.Alteplase may increase the anticoagulant activities of Darexaban.Alteplase may increase the anticoagulant activities of Nafamostat.Alteplase may increase the anticoagulant activities of Gabexate.Alteplase may increase the anticoagulant activities of Troxerutin.Alteplase may increase the anticoagulant activities of Fluindione.Alteplase may increase the anticoagulant activities of Protein S human.Alteplase may increase the anticoagulant activities of Melagatran.The risk or severity of adverse effects can be increased when Salicylic acid is combined with Alteplase.The risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Alteplase.The risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Alteplase.The risk or severity of adverse effects can be increased when Mesalazine is combined with Alteplase.The risk or severity of adverse effects can be increased when Diflunisal is combined with Alteplase.The risk or severity of adverse effects can be increased when Balsalazide is combined with Alteplase.The risk or severity of adverse effects can be increased when Olsalazine is combined with Alteplase.The risk or severity of adverse effects can be increased when Dersalazine is combined with Alteplase.The risk or severity of adverse effects can be increased when Nitroaspirin is combined with Alteplase.The risk or severity of adverse effects can be increased when Aloxiprin is combined with Alteplase.The risk or severity of adverse effects can be increased when Guacetisal is combined with Alteplase.The risk or severity of adverse effects can be increased when Carbaspirin calcium is combined with Alteplase.The risk or severity of adverse effects can be increased when Hemoglobin crosfumaril is combined with Alteplase.The risk or severity of adverse effects can be increased when Methyl salicylate is combined with Alteplase.The risk or severity of adverse effects can be increased when Trolamine salicylate is combined with Alteplase.Eptifibatide may increase the anticoagulant activities of Alteplase.Ticlopidine may increase the anticoagulant activities of Alteplase.Tirofiban may increase the anticoagulant activities of Alteplase.Dipyridamole may increase the anticoagulant activities of Alteplase.Clopidogrel may increase the anticoagulant activities of Alteplase.Prasugrel may increase the anticoagulant activities of Alteplase.Vorapaxar may increase the anticoagulant activities of Alteplase.Milrinone may increase the anticoagulant activities of Alteplase.Anagrelide may increase the anticoagulant activities of Alteplase.Epinastine may increase the anticoagulant activities of Alteplase.Alprostadil may increase the anticoagulant activities of Alteplase.Pentoxifylline may increase the anticoagulant activities of Alteplase.Azelastine may increase the anticoagulant activities of Alteplase.Iloprost may increase the anticoagulant activities of Alteplase.Cilostazol may increase the anticoagulant activities of Alteplase.Ridogrel may increase the anticoagulant activities of Alteplase.Sevoflurane may increase the anticoagulant activities of Alteplase.Epoprostenol may increase the anticoagulant activities of Alteplase.Resveratrol may increase the anticoagulant activities of Alteplase.Nimesulide may increase the anticoagulant activities of Alteplase.Tesmilifene may increase the anticoagulant activities of Alteplase.Defibrotide may increase the anticoagulant activities of Alteplase.SRT501 may increase the anticoagulant activities of Alteplase.Beraprost may increase the anticoagulant activities of Alteplase.Ibudilast may increase the anticoagulant activities of Alteplase.Andrographolide may increase the anticoagulant activities of Alteplase.eplivanserine may increase the anticoagulant activities of Alteplase.Cangrelor may increase the anticoagulant activities of Alteplase.Tranilast may increase the anticoagulant activities of Alteplase.Triflusal may increase the anticoagulant activities of Alteplase.Icosapent ethyl may increase the anticoagulant activities of Alteplase.Ifenprodil may increase the anticoagulant activities of Alteplase.Trapidil may increase the anticoagulant activities of Alteplase.Naftopidil may increase the anticoagulant activities of Alteplase.Sarpogrelate may increase the anticoagulant activities of Alteplase.Eplivanserin may increase the anticoagulant activities of Alteplase.Ifetroban may increase the anticoagulant activities of Alteplase.Ketanserin may increase the anticoagulant activities of Alteplase.Indobufen may increase the anticoagulant activities of Alteplase.Butylphthalide may increase the anticoagulant activities of Alteplase.Hydroxytyrosol may increase the anticoagulant activities of Alteplase.Ramatroban may increase the anticoagulant activities of Alteplase.Picotamide may increase the anticoagulant activities of Alteplase.Cloricromen may increase the anticoagulant activities of Alteplase.Linsidomine may increase the anticoagulant activities of Alteplase.Buflomedil may increase the anticoagulant activities of Alteplase.Relcovaptan may increase the anticoagulant activities of Alteplase.Ticagrelor may increase the anticoagulant activities of Alteplase.The risk or severity of adverse effects can be increased when Alteplase is combined with Treprostinil. DB06692DB09211DB06695DB00727DB00001DB00006DB00054DB00102DB00266DB00278DB00407DB00498DB00569DB00682DB00686DB00946DB00974DB01109DB01225DB01418DB04272DB04898DB05099DB06154DB06228DB06271DB06406DB06605DB06635DB06754DB06779DB07767DB08794DB08813DB09075DB09255DB09259DB09261DB11076DB11095DB11122DB11241DB11268DB11312DB11598DB11728DB11984DB12289DB12598DB12831DB13124DB13136DB13149DB13616DB00936DB00945DB00233DB00244DB00861DB01014DB01250DB06251DB12445DB13509DB13538DB13612DB13864DB09543DB11079DB00063DB00208DB00775DB00975DB00758DB06209DB09030DB00235DB00261DB00751DB00770DB00806DB00972DB01088DB01166DB01207DB01236DB01240DB02709DB04743DB04905DB04932DB05073DB05229DB05266DB05767DB06392DB06441DB07615DB08814DB08887DB08954DB09283DB12092DB12163DB12177DB12321DB12465DB12545DB12749DB12771DB13036DB13327DB13367DB13400DB13510DB13929DB08816DB00374 AprotininLimaprostDabigatran etexilateNitroglycerinLepirudinBivalirudinAbciximabBecaplerminDicoumarolArgatrobanArdeparinPhenindioneFondaparinux sodiumWarfarinPentosan PolysulfatePhenprocoumonEdetic AcidHeparinEnoxaparinAcenocoumarolCitric AcidXimelagatranAncrodPentaerythritol TetranitrateRivaroxabanSulodexideIdraparinuxApixabanOtamixabanDanaparoidDalteparinFerulic acidEthyl biscoumacetateNadroparinEdoxabanDextranReviparinCertoparinDextran 70DesirudinDextran 40Dextran 75ProtocatechualdehydeProtein CAntithrombin III humanFondaparinuxLetaxabanDarexabanNafamostatGabexateTroxerutinFluindioneProtein S humanMelagatranSalicylic acidAcetylsalicylic acidAminosalicylic AcidMesalazineDiflunisalBalsalazideOlsalazineDersalazineNitroaspirinAloxiprinGuacetisalCarbaspirin calciumHemoglobin crosfumarilMethyl salicylateTrolamine salicylateEptifibatideTiclopidineTirofibanDipyridamoleClopidogrelPrasugrelVorapaxarMilrinoneAnagrelideEpinastineAlprostadilPentoxifyllineAzelastineIloprostCilostazolRidogrelSevofluraneEpoprostenolResveratrolNimesulideTesmilifeneDefibrotideSRT501BeraprostIbudilastAndrographolideeplivanserineCangrelorTranilastTriflusalIcosapent ethylIfenprodilTrapidilNaftopidilSarpogrelateEplivanserinIfetrobanKetanserinIndobufenButylphthalideHydroxytyrosolRamatrobanPicotamideCloricromenLinsidomineBuflomedilRelcovaptanTicagrelorTreprostinil Melting PointHydrophobicityIsoelectric PointMolecular WeightMolecular Formula 60 °C-0.5167.6159042.3C2569H3928N746O781S40 Novokhatny, V.V. et al., J. Biol. Chem. 266:12994-123002 (1991) S01XA13B01AD02 Other ophthalmologicalsOTHER OPHTHALMOLOGICALSOPHTHALMOLOGICALSSENSORY ORGANSEnzymesANTITHROMBOTIC AGENTSANTITHROMBOTIC AGENTSBLOOD AND BLOOD FORMING ORGANS S01XAS01XS01SB01ADB01AB01B Amino Acids, Peptides, and ProteinsBiological FactorsBlood and Blood Forming OrgansBlood Coagulation FactorsBlood ProteinsCardiovascular AgentsChemical Actions and UsesEndopeptidasesEnzymesEnzymes and CoenzymesFibrin Modulating AgentsFibrinolytic AgentsHematologic AgentsHydrolasesMolecular Mechanisms of Pharmacological ActionPeptide HydrolasesPharmacologic ActionsPlasminogen ActivatorsProteinsSerine EndopeptidasesSerine ProteasesTherapeutic Uses D000602D001685D001779D001798D002317D020164D010450D004798D045762D050299D005343D006401D006867D045504D010447D020228D010960D011506D012697D057057D045506 729746507035D02837L00153PA164776730P00750DAP000203AlteplaseCHEMBL1201593 Drugs Product Database (DPD)PubChem SubstanceKEGG DrugGenBankPharmGKBUniProtKBTherapeutic Targets DatabaseWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic/alteplas.htmhttp://www.drugs.com/cdi/alteplase.html //s3-us-west-2.amazonaws.com/drugbank/fda_labels/DB00009.pdf?1265922802 approved Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides drug_action DB00009DB01022DB01373 AlteplasePhylloquinoneCalcium P00747P00748P02452P03952P03951P00740P00451P00734P12259P00742P02671P02675P02679P00488P05160P00750P08709P13726Q9BQB6P38435 Alteplase Action Pathway SMP00280 AlteplaseAlteplase + WaterAlteplaseAlteplase + WaterAlteplase + WaterAlteplaseAlteplaseAlteplase Cathflo ActivaseLysatec RT - PaActivase RT-PA InjActivase RT-PAActivase RT-PAActivaseActivaseCathflo Genentech Inc. http://www.gene.com ActivaseActivaseActivase RT-PAActivase RT-PAActivase RT-PA InjCathfloCathflo ActivaseLysatec RT - Pa falsefalsefalsefalsefalsefalsefalsefalse Genentech, Inc.Genentech, Inc.Hoffmann La RocheHoffmann La RocheHoffmann La RocheHoffmann La RocheGenentech, Inc.Genentech, Inc. falsefalsefalsefalsefalsefalsefalsefalse IntravenousIntravenousIntravenousIntravenousIntravenous KitKitLiquid; Powder, for solutionLiquid; Powder, for solutionPowder, for solutionPowder, for solutionInjection, powder, lyophilized, for solutionPowder, for solution FDA NDCFDA NDCDPDDPDDPDDPDFDA NDCDPD 29 m2 mg2.2 mg/2mL 50242-04450242-08550242-041 BLA103172BLA103172BLA103172 truetruetruetruetruetruetruetrue 0214744002225689007714730224585902009285 USUSCanadaCanadaCanadaCanadaUSCanada 1987-11-131987-11-131996-12-311998-04-121987-12-312002-09-262001-09-041993-12-31 1998-07-311997-08-26 vialvialvial 106.332389.854779.71 USDUSDUSD Cathflo activase 2 mg vialActivase 50 mg vialActivase 100 mg vial DB00010 86168-78-7 Sermorelin biotech 89243S03TE liquid Sermorelin acetate is the acetate salt of an amidated synthetic 29-amino acid peptide (GRF 1-29 NH 2 ) that corresponds to the amino-terminal segment of the naturally occurring human growth hormone-releasing hormone (GHRH or GRF) consisting of 44 amino acid residues Humans and other mammals For the treatment of dwarfism, prevention of HIV-induced weight loss Sermorelin binds to the growth hormone releasing hormone receptor and mimics native GRF in its ability to stimulate growth hormone secretion. agonist Growth hormone-releasing hormone receptor BE0000625 Human Esposito P, Barbero L, Caccia P, Caliceti P, D'Antonio M, Piquet G, Veronese FM: PEGylation of growth hormone-releasing hormone (GRF) analogues. Adv Drug Deliv Rev. 2003 Sep 26;55(10):1279-91.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. 1449970711752352 Q02643 Growth hormone-releasing hormone receptor 7p14 Human cytoplasmplasma membranecell surfaceintegral component of membranesecretory granulenuclear inner membranenuclear outer membranenuclear matrixpeptide hormone bindingG-protein coupled receptor activitygrowth factor bindinggrowth hormone-releasing hormone receptor activityregulation of intracellular steroid hormone receptor signaling pathwaycell surface receptor signaling pathwaycell maturationregulation of protein metabolic processpositive regulation of cell proliferationhormone metabolic processsomatotropin secreting cell developmentresponse to estrogenpositive regulation of multicellular organism growthresponse to glucocorticoidcAMP-mediated signalingcellular response to insulin stimuluspositive regulation of insulin-like growth factor receptor signaling pathwaylactationpositive regulation of cAMP biosynthetic processmulticellular organismal reproductive processresponse to insulingrowth hormone secretionadenylate cyclase-activating G-protein coupled receptor signaling pathwaydetermination of adult lifespanwater homeostasispositive regulation of growth hormone secretionactivation of adenylate cyclase activity Peptide hormone binding Receptor for GRF, coupled to G proteins which activate adenylyl cyclase. Stimulates somatotroph cell growth, growth hormone gene transcription and growth hormone secretion. 11-12 min Sermorelin is used in the treatment of children with growth hormone deficiency or growth failure. Geref increases plasma growth hormone (GH) concentration by stimulating the pituitary gland to release GH. Geref is similar to the full-length native hormone (44 residues) in its ability to stimulate GH secretion in humans. HydrophobicityIsoelectric PointMolecular WeightMolecular Formula -0.3309.993357.882C149H246N44O42S V04CD03H01AC04 Tests for pituitary functionOTHER DIAGNOSTIC AGENTSDIAGNOSTIC AGENTSVARIOUSSomatropin and somatropin agonistsANTERIOR PITUITARY LOBE HORMONES AND ANALOGUESPITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUESSYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS V04CDV04CV04VH01ACH01AH01H Amino Acids, Peptides, and ProteinsAnterior Pituitary Lobe Hormones and AnaloguesChemical Actions and UsesGrowth Hormone-Releasing HormoneHormonesHormones, Hormone Substitutes, and Hormone AntagonistsHypothalamic HormonesNerve Tissue ProteinsNeuropeptidesPeptide HormonesPeptidesPharmacologic ActionsPhysiological Effects of DrugsPituitary and Hypothalamic Hormones and AnaloguesPituitary Hormone-Releasing HormonesProteinsSomatropin and Somatropin AgonistsSystemic Hormonal Preparations, Excl. Sex Hormones and Insulins D000602D020164D013007D006728D006730D007028D009419D009479D036361D010455D020228D045505D010906D011506 46507399C08192PA164749110DAP001055Sermorelin PubChem SubstanceKEGG CompoundPharmGKBTherapeutic Targets DatabaseWikipedia RxListDrugs.com http://www.rxlist.com/cgi/generic2/sermorelin.htmhttp://www.drugs.com/cdi/sermorelin-acetate.html approvedwithdrawn Serono Pharma Geref Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides Emd serono inc false Chengdu Shengnuo Bio Pharmaceutical Co. Ltd.Letco Medical Inc.Live Well Drugstore LLC http://www.letcomedical.comhttp://www.livewelldrugstore.com DB00011DB00084 74899-72-2 Interferon alfa-n1 Interferon alpha-2Interferon alpha-AInterferon alpha-n1 (Ins)LeIF A biotech 41697D4Z5C Vladimir G. Debabov, Jury D. Tsygankov, Andrei J. Chistoserdov, Evgeny D. Sverdlov, Lara S. Izotova, Sergei V. Kostrov, Viktor E. Sterkin, Vladimir P. Kuznetsov, Sergei V. Belyaev, Galina S. Monastyrskaya, Irina S. Salomatina, Grigory M. Dolganov, Sergei G. Arsenian, Sergei A. Tsarev, Jury I. Kozlov, Alexandr Y. Strongin, Vsevolod I. Ogarkov, Jury A. Ovchinnikov, "Method for producing human leukocyte interferon alpha-2." U.S. Patent US4680260, issued January, 1982. liquid Purified, natural (n is for natural) glycosylated human interferon alpha proteins 166 residues Humans and other mammals LiquidLiquid Intramuscular; SubcutaneousIntramuscular; Subcutaneous 10000000 unit3000000 unit For treatment of venereal or genital warts caused by the Human Papiloma Virus Interferon alpha binds to type I interferon receptors (IFNAR1 and IFNAR2c) which, upon dimerization, activate two Jak (Janus kinase) tyrosine kinases (Jak1 and Tyk2). These transphosphorylate themselves and phosphorylate the receptors. The phosphorylated INFAR receptors then bind to Stat1 and Stat2 (signal transducers and activators of transcription)which dimerize and activate multiple (~100) immunomodulatory and antiviral proteins. Interferon alpha binds less stably to type I interferon receptors than interferon beta. agonistagonist Interferon alpha/beta receptor 2Interferon alpha/beta receptor 1 BE0000385BE0000661 HumanHuman Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Krown SE: Interferon treatment of renal cell carcinoma. Current status and future prospects. Cancer. 1987 Feb 1;59(3 Suppl):647-51.Ishii K, Shinohara M, Sawa M, Kogame M, Higami K, Sano M, Morita T, Sumino Y: Interferon alpha receptor 2 expression by peripheral blood monocytes in patients with a high viral load of hepatitis C virus genotype 1 showing substitution of amino Acid 70 in the core region. Intervirology. 2010;53(2):105-10. doi: 10.1159/000264200. Epub 2009 Dec 3.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Krown SE: Interferon treatment of renal cell carcinoma. Current status and future prospects. Cancer. 1987 Feb 1;59(3 Suppl):647-51.Ishii K, Shinohara M, Sawa M, Kogame M, Higami K, Sano M, Morita T, Sumino Y: Interferon alpha receptor 2 expression by peripheral blood monocytes in patients with a high viral load of hepatitis C virus genotype 1 showing substitution of amino Acid 70 in the core region. Intervirology. 2010;53(2):105-10. doi: 10.1159/000264200. Epub 2009 Dec 3.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. 17139284170164231082246419955815117523521713928417016423108224641995581511752352 P48551P17181 Interferon alpha/beta receptor 2Interferon alpha/beta receptor 1 HumanHuman intracellularextracellular regionplasma membraneextracellular spaceintegral component of plasma membraneprotein kinase bindingtype I interferon bindingtype I interferon receptor activityJAK-STAT cascaderegulation of transcription from RNA polymerase II promoterregulation of type I interferon-mediated signaling pathwayresponse to interferon-alphacell proliferationresponse to virustype I interferon signaling pathwaycell surface receptor signaling pathwaycytokine-mediated signaling pathwayintracellularplasma membraneintegral component of plasma membranetype I interferon receptor activityregulation of type I interferon-mediated signaling pathwayresponse to virustype I interferon signaling pathwaypositive regulation of transcription, DNA-templateddefense response to viruscell surface receptor signaling pathwaypositive regulation of interleukin-1 beta secretioncytokine-mediated signaling pathwaypositive regulation of interferon-beta productionregulation of peptidyl-tyrosine phosphorylationtype I interferon biosynthetic processpositive regulation of interferon-gamma productionT cell activationJAK-STAT cascade Type i interferon receptor activityType i interferon receptor activity Associates with IFNAR1 to form the type I interferon receptor. Receptor for interferons alpha and beta. Involved in IFN-mediated STAT1, STAT2 and STAT3 activation. Isoform 1 and isoform 2 are directly involved in signal transduction due to their association with the TYR kinase, JAK1. Isoform 3 is a potent inhibitor of type I IFN receptor activity.Associates with IFNAR2 to form the type I interferon receptor. Receptor for interferons alpha and beta. Binding to type I IFNs triggers tyrosine phosphorylation of a number of proteins including JAKs, TYK2, STAT proteins and IFNR alpha- and beta-subunits themselves. Can also transduce IFNB signals without the help of IFNAR2, and not activating the Jak-STAT pathway. 1.2 hours (mammalian reticulocytes, in vitro); >20 hours (yeast, in vivo); >10 hours (Escherichia coli, in vivo). Upregulates the expression of MHC I proteins, allowing for increased presentation of peptides derived from viral antigens. This enhances the activation of CD8+ T cells that are the precursors for cytotoxic T lymphocytes (CTLs) and makes the macrophage a better target for CTL-mediated killing. Interferon alpha also induce the synthesis of several key antiviral mediators, including 2'-5' oligoadenylate synthetase (2'-5' A synthetase) and protein kinase R. The metabolism of Ambroxol acefyllinate can be decreased when combined with Interferon alfa-n1.The metabolism of Theophylline can be decreased when combined with Interferon alfa-n1.The metabolism of Dyphylline can be decreased when combined with Interferon alfa-n1.The metabolism of Aminophylline can be decreased when combined with Interferon alfa-n1.The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Zidovudine. DB13141DB00277DB00651DB01223DB00495 Ambroxol acefyllinateTheophyllineDyphyllineAminophyllineZidovudine Avoid alcohol. Melting PointHydrophobicityIsoelectric PointMolecular WeightMolecular Formula 61 °C-0.3365.9919241.1C860H1353N227O255S9 Beldarrain, A. et al., Biochemistry 38:7865-7873 (1999) L03AB06 InterferonsIMMUNOSTIMULANTSIMMUNOSTIMULANTSANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L03ABL03AL03L Adjuvants, ImmunologicAmino Acids, Peptides, and ProteinsAnti-Infective AgentsAntineoplastic and Immunomodulating AgentsAntiviral AgentsBiological FactorsChemical Actions and UsesCytokinesImmunologic FactorsIntercellular Signaling Peptides and ProteinsInterferon Type IInterferonsPeptidesPharmacologic ActionsPhysiological Effects of DrugsProteinsTherapeutic Uses D000276D000602D000890D000998D001685D020164D016207D007155D036341D007370D007372D010455D020228D045505D011506D045506 765146506227J00207PA164746538P01563DAP001280CHEMBL2108509 Drugs Product Database (DPD)PubChem SubstanceGenBankPharmGKBUniProtKBTherapeutic Targets DatabaseChEMBL approvedinvestigational GlaxoSmithKline Wellferon Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides Interferon alfa-n1Interferon alfa-n1 Wellferon Inj 10 000 000unit/mlWellferon Inj 3000000unit/ml Wellferon Inj 10 000 000unit/mlWellferon Inj 3000000unit/ml falsefalse The Wellcome Foundation Ltd.The Wellcome Foundation Ltd. falsefalse Intramuscular; SubcutaneousIntramuscular; Subcutaneous LiquidLiquid DPDDPD 10000000 unit3000000 unit truetrue 0195906901959077 CanadaCanada 1992-12-311992-12-31 2000-08-012000-08-01 DB00012 209810-58-2 Darbepoetin alfa DarbepoetinDarbepoetin alfa,recombinant biotech 15UQ94PT4P liquid Human erythropoietin with 2 aa substitutions to enhance glycosylation (5 N-linked chains), 165 residues (MW=37 kD). Produced in Chinese hamster ovary (CHO) cells by recombinant DNA technology. Humans and other mammals Injection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolution Intravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; Subcutaneous 10 ug/.4mL10 μg100 ug/.5mL100 μg130 μg15 μg150 μg150 ug/.3mL20 μg200 ug/.4mL200 μg25 ug/.42mL25 μg30 μg300 μg300 ug/.6mL40 ug/.4mL40 μg50 μg500 μg500 ug/mL60 ug/.3mL60 μg80 μg10 μg100 μg130 μg15 μg150 μg20 μg30 μg300 μg40 μg50 μg500 μg60 μg80 μg100 ug/mL150 ug/.75mL200 ug/mL25 ug/mL300 ug/mL40 ug/mL60 ug/mL100 mcg15 mcg200 mcg25 mcg325 mcg40 mcg500 mcg60 mcg For the treatment of anemia (from renal transplants or certain HIV treatment) Darbepoetin alfa stimulates erythropoiesis by the same mechanism as endogenous erythropoietin. Erythropoietin interacts withprogenitor stem cells to increase red cell production. Binding of erythropoietin to the erythropoietin receptor leads to receptor dimerization, which facilitates activation of JAK-STAT signaling pathways within the cytosol. Activated STAT (signal transducers and activators of transcription) proteins are then translocated to the nucleus where they serve as transcription factors which regulate the activation of specific genes involved in cell division or differentiation. agonist Erythropoietin receptor BE0000654 Human LaMontagne KR, Butler J, Marshall DJ, Tullai J, Gechtman Z, Hall C, Meshaw A, Farrell FX: Recombinant epoetins do not stimulate tumor growth in erythropoietin receptor-positive breast carcinoma models. Mol Cancer Ther. 2006 Feb;5(2):347-55.Kokhaei P, Abdalla AO, Hansson L, Mikaelsson E, Kubbies M, Haselbeck A, Jernberg-Wiklund H, Mellstedt H, Osterborg A: Expression of erythropoietin receptor and in vitro functional effects of epoetins in B-cell malignancies. Clin Cancer Res. 2007 Jun 15;13(12):3536-44.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. 165051081757521611752352 P19235 Erythropoietin receptor 19p13.3-p13.2 Human extracellular regioncytosolintegral component of plasma membraneidentical protein bindingerythropoietin receptor activitysignal transductionerythropoietin-mediated signaling pathwaypositive regulation of cytosolic calcium ion concentrationheart developmentbrain developmentnegative regulation of neuron apoptotic processdecidualization Identical protein binding Receptor for erythropoietin. Mediates erythropoietin-induced erythroblast proliferation and differentiation. Upon EPO stimulation, EPOR dimerizes triggering the JAK2/STAT5 signaling cascade. In some cell types, can also activate STAT1 and STAT3. May also activate the LYN tyrosine kinase.Isoform EPOR-T acts as a dominant-negative receptor of EPOR-mediated signaling. Darbepoetin alfa is used in the treatment of anemia. It is involved in the regulation of erythrocyte differentiation and the maintenance of a physiological level of circulating erythrocyte mass. Nandrolone phenpropionate may increase the stimulatory activities of Darbepoetin alfa.Nandrolone decanoate may increase the stimulatory activities of Darbepoetin alfa.Darbepoetin alfa may increase the thrombogenic activities of Lenalidomide.Darbepoetin alfa may increase the thrombogenic activities of Thalidomide. DB00984DB08804DB00480DB01041 Nandrolone phenpropionateNandrolone decanoateLenalidomideThalidomide Melting PointHydrophobicityIsoelectric PointMolecular WeightMolecular Formula 53 °C-0.1888.7518396.1C815H1317N233O241S5 Arakawa, T. et al., Biosci. Biotechnol. Biochem. 65:1321-1327 (2001) B03XA02 Other antianemic preparationsOTHER ANTIANEMIC PREPARATIONSANTIANEMIC PREPARATIONSBLOOD AND BLOOD FORMING ORGANS B03XAB03XB03B Amino Acids, Peptides, and ProteinsAntianemic PreparationsBiological FactorsBlood and Blood Forming OrgansCarbohydratesChemical Actions and UsesColony-Stimulating FactorsCytokinesErythropoiesis-Stimulating AgentsErythropoietinGlycoconjugatesGlycoproteinsHematinicsHematologic AgentsHematopoietic Cell Growth FactorsIntercellular Signaling Peptides and ProteinsPeptidesPharmacologic ActionsProteinsTherapeutic Uses D000602D001685D002241D020164D003115D016207D004921D006001D006023D006397D006401D016298D036341D010455D020228D011506D045506 1255046504480X02158PA164743138P01588DAP000800Darbepoetin_alfaCHEMBL1201566 Drugs Product Database (DPD)PubChem SubstanceGenBankPharmGKBUniProtKBTherapeutic Targets DatabaseWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic/aranesp.htmhttp://www.drugs.com/cdi/darbepoetin-alfa-albumin.html approvedinvestigational Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides 21656942147124 CanadaCanada 2003-03-182002-11-05 2010-10-152014-08-16 falsefalse Amgen Inc. false Darbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfaDarbepoetin alfa AranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free) Amgen Inc.Physicians Total Care Inc. http://www.amgen.comhttp://www.physicianstotalcare.com AranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranespAranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)Aranesp -(hsa-free)NespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespoNespo 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S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A. 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Intravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousSubcutaneousSubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousSubcutaneousSubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; Subcutaneous SolutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, 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solutionInjection, solutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, 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NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMA 300 ug/mL300 ug/.6mL10 μg10 μg15 μg15 μg20 μg20 μg30 μg30 μg40 μg40 μg50 μg50 μg60 μg60 μg80 μg80 μg100 μg100 μg150 μg150 μg300 μg300 μg500 μg500 μg10 μg15 μg20 μg30 μg40 μg50 μg60 μg80 μg100 μg150 μg300 μg500 μg10 μg15 μg20 μg30 μg40 μg50 μg60 μg80 μg100 μg150 μg300 μg500 μg10 μg15 μg20 μg30 μg40 μg50 μg60 μg80 μg100 μg150 μg300 μg500 μg130 μg130 μg130 μg130 μg130 μg10 μg10 μg15 μg15 μg20 μg20 μg30 μg30 μg40 μg40 μg50 μg50 μg60 μg60 μg80 μg80 μg100 μg100 μg130 μg130 μg150 μg150 μg300 μg300 μg500 μg500 μg25 μg25 μg40 μg40 μg60 μg60 μg100 μg100 μg200 μg200 μg300 μg300 μg25 ug/mL40 ug/mL60 ug/mL100 ug/mL200 ug/mL40 ug/.4mL60 ug/.3mL100 ug/.5mL150 ug/.3mL200 ug/.4mL500 ug/mL150 ug/.75mL25 ug/.42mL10 ug/.4mL500 mcg500 mcg25 mcg40 mcg100 mcg200 mcg500 mcg100 mcg100 mcg200 mcg200 mcg200 mcg500 mcg500 mcg500 mcg25 mcg40 mcg100 mcg200 mcg500 mcg15 mcg60 mcg325 mcg40 mcg10 μg15 μg20 μg30 μg40 μg50 μg60 μg80 μg100 μg150 μg300 μg500 μg10 μg15 μg20 μg30 μg40 μg50 μg60 μg80 μg100 μg150 μg300 μg500 μg130 μg130 μg130 μg130 μg130 μg10 μg10 μg15 μg15 μg20 μg20 μg30 μg30 μg40 μg40 μg50 μg50 μg60 μg60 μg80 μg80 μg100 μg100 μg150 μg150 μg300 μg300 μg15 μg15 μg25 μg25 μg40 μg40 μg60 μg60 μg500 μg500 μg10 μg15 μg20 μg30 μg40 μg50 μg60 μg80 μg100 μg150 μg300 μg500 μg 55513-11055513-11155513-00255513-00355513-00455513-00555513-00655513-02155513-02355513-02555513-02755513-02855513-03255513-05355513-05755513-098 BLA103951BLA103951BLA103951BLA103951BLA103951BLA103951BLA103951BLA103951BLA103951BLA103951BLA103951BLA103951BLA103951BLA103951BLA103951BLA103951 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2008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-112008-12-11 mlvialmlmlvialmlmlmlvialboxboxbox 156.36162.61250.2375.3390.31625.441250.881876.321951.372601.832601.833902.75 USDUSDUSDUSDUSDUSDUSDUSDUSDUSDUSDUSD Aranesp 25 mcg/ml vialAranesp (Albumin Free) 25 mcg/ml vialAranesp 40 mcg/ml vialAranesp 60 mcg/ml vialAranesp (Albumin Free) 60 mcg/ml vialAranesp 100 mcg/ml vialAranesp 200 mcg/ml vialAranesp 300 mcg/ml vialAranesp (Albumin Free) 300 mcg/ml vialAranesp (Albumin Free) 100 mcg/0.5ml Solution (1 Box = Four 0.5ml Syringes)Aranesp (Albumin Free) 100 mcg/ml Solution Four 1ml Vials Per BoxAranesp (Albumin Free) 150 mcg/0.75ml Solution (1 Box = Four 0.75ml Vials) DB00013 9039-53-6 Urokinase U-plasminogen activatoruPAUrokinase-type plasminogen activator precursor biotech 83G67E21XI Koji Sasaki, Yasukazu Harada, "Urokinase preparation for oral administration." U.S. Patent US4258030, issued November, 1975. liquid Low molecular weight form of human urokinase, that consists of an A chain of 2,000 daltons linked by a sulfhydryl bond to a B chain of 30,400 daltons. Recombinant urokinase plasminogen activator Humans and other mammals Powder, for solutionPowder, for solution IntravenousIntravenous 250000 unit5000 unit Urokinase can be used for the treatment of pulminary embolism, coronary artery thrombosis, IV catheter clearance, and venous and arterial blood clots. Urokinase acts on the endogenous fibrinolytic system. It cleaves the Arg-Val bond in plasminogen to produce active plasmin. Plasmin degrades fibrin clots as well as fibrinogen and other plasma proteins. activator PlasminogenUrokinase plasminogen activator surface receptorUrokinase-type plasminogen activatorTissue-type plasminogen activatorPlasminogen activator inhibitor 1Plasminogen activator inhibitor 2Plasma serine protease inhibitorLow-density lipoprotein receptor-related protein 2Suppressor of tumorigenicity 14 proteinNidogen-1 BE0000211BE0000717BE0000895BE0001088BE0000240BE0000969BE0002112BE0000942BE0001656BE0002113 HumanHumanHumanHumanHumanHumanHumanHumanHumanHuman Zhang X, Zhou H, Shen G, Liu Z, Hu Y, Wei W, Song S: Study on the mechanism of the annexin II-mediated co-assembly of t-PA and plasminogen. J Huazhong Univ Sci Technolog Med Sci. 2002;22(1):21-3, 76.Lopez-Alemany R, Longstaff C, Hawley S, Mirshahi M, Fabregas P, Jardi M, Merton E, Miles LA, Felez J: Inhibition of cell surface mediated plasminogen activation by a monoclonal antibody against alpha-Enolase. Am J Hematol. 2003 Apr;72(4):234-42.Hashimoto M, Oiwa K, Matsuo O, Ueshima S, Okada K, Okada Y, Okamoto S, Giddings JC, Yamamoto J: Suppression of argatroban-induced endogenous thrombolysis by PKSI-527, and antibodies to TPA and UPA, evaluated in a rat arterial thrombolysis model. Thromb Haemost. 2003 May;89(5):820-5.Guda K, Claffey KP, Dong M, Nambiar PR, Rosenberg DW: Defective processing of the transforming growth factor-beta1 in azoxymethane-induced mouse colon tumors. Mol Carcinog. 2003 May;37(1):51-9.Chang H, Shyu KG, Lin S, Wang BW, Liu YC, Lee CC: Cell adhesion induces the plasminogen activator inhibitor-1 gene expression through phosphatidylinositol 3-kinase/Akt activation in anchorage dependent cells. Cell Commun Adhes. 2002 Sep-Dec;9(5-6):239-47.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.Czekay RP, Aertgeerts K, Curriden SA, Loskutoff DJ: Plasminogen activator inhibitor-1 detaches cells from extracellular matrices by inactivating integrins. J Cell Biol. 2003 Mar 3;160(5):781-91.Fuchs T, Allgayer H: Transcriptional regulation of the urokinase receptor (u-PAR)--a central molecule of invasion and metastasis. Biol Chem. 2003 May;384(5):755-61.Kanse SM, Chavakis T, Al-Fakhri N, Hersemeyer K, Monard D, Preissner KT: Reciprocal regulation of urokinase receptor (CD87)-mediated cell adhesion by plasminogen activator inhibitor-1 and protease nexin-1. J Cell Sci. 2004 Jan 26;117(Pt 3):477-85. Epub 2003 Dec 16.Beaufort N, Leduc D, Rousselle JC, Magdolen V, Luther T, Namane A, Chignard M, Pidard D: Proteolytic regulation of the urokinase receptor/CD87 on monocytic cells by neutrophil elastase and cathepsin G. J Immunol. 2004 Jan 1;172(1):540-9.Guerrero J, Santibanez JF, Gonzalez A, Martinez J: EGF receptor transactivation by urokinase receptor stimulus through a mechanism involving Src and matrix metalloproteinases. Exp Cell Res. 2004 Jan 1;292(1):201-8.Gutova M, Najbauer J, Gevorgyan A, Metz MZ, Weng Y, Shih CC, Aboody KS: Identification of uPAR-positive chemoresistant cells in small cell lung cancer. PLoS One. 2007 Feb 28;2(2):e243.Bell WR: Present-day thrombolytic therapy: therapeutic agents--pharmacokinetics and pharmacodynamics. Rev Cardiovasc Med. 2002;3 Suppl 2:S34-44.Gamberi G, Serra M, Ragazzini P, Magagnoli G, Pazzaglia L, Ponticelli F, Ferrari C, Zanasi M, Bertoni F, Picci P, Benassi MS: Identification of markers of possible prognostic value in 57 giant cell tumors of bone. Oncol Rep. 2003 Mar-Apr;10(2):351-6.Zhang G, Kim H, Cai X, Lopez-Guisa JM, Alpers CE, Liu Y, Carmeliet P, Eddy AA: Urokinase receptor deficiency accelerates renal fibrosis in obstructive nephropathy. J Am Soc Nephrol. 2003 May;14(5):1254-71.Chang H, Shyu KG, Lin S, Wang BW, Liu YC, Lee CC: Cell adhesion induces the plasminogen activator inhibitor-1 gene expression through phosphatidylinositol 3-kinase/Akt activation in anchorage dependent cells. Cell Commun Adhes. 2002 Sep-Dec;9(5-6):239-47.Wielockx B, Libert C: Serine proteases of the fibrinolysis pathway are not involved in lethal hepatitis and fibrinogen breakdown induced by tumor necrosis factor. Cytokine. 2003 Mar 21;21(6):281-5.Chang H, Shyu KG, Lin S, Wang BW, Liu YC, Lee CC: Cell adhesion induces the plasminogen activator inhibitor-1 gene expression through phosphatidylinositol 3-kinase/Akt activation in anchorage dependent cells. Cell Commun Adhes. 2002 Sep-Dec;9(5-6):239-47.Lindholt JS, Jorgensen B, Shi GP, Henneberg EW: Relationships between activators and inhibitors of plasminogen, and the progression of small abdominal aortic aneurysms. Eur J Vasc Endovasc Surg. 2003 Jun;25(6):546-51.Aleman C, Alegre J, Monasterio J, Segura RM, Armadans L, Angles A, Varela E, Ruiz E, Fernandez de Sevilla T: Association between inflammatory mediators and the fibrinolysis system in infectious pleural effusions. Clin Sci (Lond). 2003 Nov;105(5):601-7.Wells RG, Havens PL: Intrapleural fibrinolysis for parapneumonic effusion and empyema in children. Radiology. 2003 Aug;228(2):370-8.Stief TW, Bunder R, Richter A, Maisch B, Renz H, Fareed J: In vitro simulation of therapeutic plasmatic fibrinolysis. Clin Appl Thromb Hemost. 2003 Jul;9(3):211-20.Gamberi G, Serra M, Ragazzini P, Magagnoli G, Pazzaglia L, Ponticelli F, Ferrari C, Zanasi M, Bertoni F, Picci P, Benassi MS: Identification of markers of possible prognostic value in 57 giant cell tumors of bone. Oncol Rep. 2003 Mar-Apr;10(2):351-6.Shetty S, Bdeir K, Cines DB, Idell S: Induction of plasminogen activator inhibitor-1 by urokinase in lung epithelial cells. J Biol Chem. 2003 May 16;278(20):18124-31. Epub 2003 Mar 17.Hellgren M: Hemostasis during normal pregnancy and puerperium. Semin Thromb Hemost. 2003 Apr;29(2):125-30.Chang H, Shyu KG, Lin S, Wang BW, Liu YC, Lee CC: Cell adhesion induces the plasminogen activator inhibitor-1 gene expression through phosphatidylinositol 3-kinase/Akt activation in anchorage dependent cells. Cell Commun Adhes. 2002 Sep-Dec;9(5-6):239-47.Gerstein ES, Shcherbakov AM, Kaz'min AI, Ognerubov NA, Kushlinskii NE: [Urokinase and tissue type plasminogen activators and their type-1 inhibitor (PAI-1) in gastric cancer]. Vopr Onkol. 2003;49(2):165-9.Swartz JM, Bystrom J, Dyer KD, Nitto T, Wynn TA, Rosenberg HF: Plasminogen activator inhibitor-2 (PAI-2) in eosinophilic leukocytes. J Leukoc Biol. 2004 Oct;76(4):812-9. Epub 2004 Jul 26.Wygrecka M, Markart P, Ruppert C, Kuchenbuch T, Fink L, Bohle RM, Grimminger F, Seeger W, Gunther A: Compartment- and cell-specific expression of coagulation and fibrinolysis factors in the murine lung undergoing inhalational versus intravenous endotoxin application. Thromb Haemost. 2004 Sep;92(3):529-40.Iglesias D, Alegre J, Aleman C, Ruiz E, Soriano T, Armadans LI, Segura RM, Angles A, Monasterio J, de Sevilla TF: Metalloproteinases and tissue inhibitors of metalloproteinases in exudative pleural effusions. Eur Respir J. 2005 Jan;25(1):104-9.Grebenchtchikov N, Maguire TM, Riisbro R, Geurts-Moespot A, O'Donovan N, Schmitt M, McGreal G, McDermott E, O'Higgins N, Brunner N, Sweep CG, Duffy MJ: Measurement of plasminogen activator system components in plasma and tumor tissue extracts obtained from patients with breast cancer: an EORTC Receptor and Biomarker Group collaboration. Oncol Rep. 2005 Jul;14(1):235-9.Fernandez-Soria V, Lleonart ME, Diaz-Fuertes M, Villuendas R, Sanchez-Prieto R, Fabra A, Ramon Y Cajal S: Adenovirus E1A orchestrates the urokinase-plasminogen activator system and upregulates PAI-2 expression, supporting a tumor suppressor effect. Int J Oncol. 2006 Jan;28(1):143-8.Uhrin P, Schofer C, Zaujec J, Ryban L, Hilpert M, Weipoltshammer K, Jerabek I, Pirtzkall I, Furtmuller M, Dewerchin M, Binder BR, Geiger M: Male fertility and protein C inhibitor/plasminogen activator inhibitor-3 (PCI): localization of PCI in mouse testis and failure of single plasminogen activator knockout to restore spermatogenesis in PCI-deficient mice. Fertil Steril. 2007 Oct;88(4 Suppl):1049-57. Epub 2007 Apr 16.Espana F, Navarro S, Medina P, Zorio E, Estelles A: The role of protein C inhibitor in human reproduction. Semin Thromb Hemost. 2007 Feb;33(1):41-5.Odet F, Guyot R, Leduque P, Le Magueresse-Battistoni B: Evidence for similar expression of protein C inhibitor and the urokinase-type plasminogen activator system during mouse testis development. Endocrinology. 2004 Mar;145(3):1481-9. Epub 2003 Nov 26.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Kanalas JJ: Effect of the nephritogenic autoantibody of Heymann's nephritis on plasminogen-binding to gp330 and activation by urokinase. Biochim Biophys Acta. 1993 Nov 25;1225(1):101-6.Kanalas JJ: Analysis of plasmin binding and urokinase activation of plasminogen bound to the Heymann nephritis autoantigen, gp330. Arch Biochem Biophys. 1992 Dec;299(2):255-60.Korenberg JR, Argraves KM, Chen XN, Tran H, Strickland DK, Argraves WS: Chromosomal localization of human genes for the LDL receptor family member glycoprotein 330 (LRP2) and its associated protein RAP (LRPAP1). Genomics. 1994 Jul 1;22(1):88-93.Suzuki M, Kobayashi H, Kanayama N, Saga Y, Suzuki M, Lin CY, Dickson RB, Terao T: Inhibition of tumor invasion by genomic down-regulation of matriptase through suppression of activation of receptor-bound pro-urokinase. J Biol Chem. 2004 Apr 9;279(15):14899-908. Epub 2004 Jan 27.Kirchhofer D, Peek M, Li W, Stamos J, Eigenbrot C, Kadkhodayan S, Elliott JM, Corpuz RT, Lazarus RA, Moran P: Tissue expression, protease specificity, and Kunitz domain functions of hepatocyte growth factor activator inhibitor-1B (HAI-1B), a new splice variant of HAI-1. J Biol Chem. 2003 Sep 19;278(38):36341-9. Epub 2003 Jun 18.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Stephens RW, Aumailley M, Timpl R, Reisberg T, Tapiovaara H, Myohanen H, Murphy-Ullrich J, Vaheri A: Urokinase binding to laminin-nidogen. Structural requirements and interactions with heparin. Eur J Biochem. 1992 Aug 1;207(3):937-42. 12658774126661331271977812720300127454351175235212615913128174721467930414688365147205191732790812556741125792711270739412745435128240011274543512787697128260211289389814507109125792711264258712709915127454351278519815277569153518491564033015944795163279901743450717253188146451121713928417016423824128612800657959795147474691281503917139284170164231499567 P00747Q03405P00749P00750P05121P05120P05154P98164Q9Y5Y6P14543 PlasminogenUrokinase plasminogen activator surface receptorUrokinase-type plasminogen activatorTissue-type plasminogen activatorPlasminogen activator inhibitor 1Plasminogen activator inhibitor 2Plasma serine protease inhibitorLow-density lipoprotein receptor-related protein 2Suppressor of tumorigenicity 14 proteinNidogen-1 6q2619q1310q248p127q21.3-q2218q21.314q32.12q24-q3111q24-q251q43 HumanHumanHumanHumanHumanHumanHumanHumanHumanHuman extracellular exosomeextrinsic component of external side of plasma membraneextracellular regionplasma membraneplatelet alpha granule lumenextracellular spaceblood microparticlecell surfaceapolipoprotein bindingserine-type endopeptidase activityreceptor bindingserine-type peptidase activityprotein domain specific bindingnegative regulation of fibrinolysisblood coagulationextracellular matrix disassemblyproteolysisextracellular matrix organizationpositive regulation of fibrinolysisnegative regulation of cell-substrate adhesiontissue remodelingcellular protein metabolic processnegative regulation of cell-cell adhesion mediated by cadherinnegative regulation of cell proliferationplatelet degranulationfibrinolysisplatelet activationintegral component of plasma membraneendoplasmic reticulum lumenanchored component of membraneplasma membraneextrinsic component of membraneendoplasmic reticulum membraneinvadopodium membranefocal adhesionintegral component of membraneextracellular exosomereceptor activityreceptor bindingprotein domain specific bindingurokinase plasminogen activator receptor activityenzyme bindingnegative regulation of intrinsic apoptotic signaling pathwayurokinase plasminogen activator signaling pathwaypositive regulation of protein phosphorylationpositive regulation of DNA bindingsignal transductionpositive regulation of epidermal growth factor receptor signaling pathwayblood coagulationpositive regulation of release of cytochrome c from mitochondriacellular protein metabolic processnegative regulation of apoptotic processpost-translational protein modificationfibrinolysisregulation of proteolysischemotaxismovement of cell or subcellular componentattachment of GPI anchor to proteinnegative regulation of cysteine-type endopeptidase activity involved in apoptotic signaling pathwayC-terminal protein lipidationextracellular regionplasma membraneextracellular spacefocal adhesioncell surfaceextracellular exosomeserine-type endopeptidase activityembryo implantationsignal transductionneuron deathfibrinolysisspermatogenesisblood coagulationcellular response to staurosporinepositive regulation of cell proliferationcellular response to glucose stimuluspositive regulation of ovulationpositive regulation of reactive oxygen species metabolic processcellular response to fluid shear stressproteolysisregulation of smooth muscle cell-matrix adhesionresponse to activityregulation of hepatocyte proliferationregulation of wound healingangiogenesisplasminogen activationcellular response to lipopolysaccharidesmooth muscle cell migrationcellular response to hepatocyte growth factor stimuluspositive regulation of smooth muscle cell migrationregulation of cell adhesion mediated by integrinchemotaxiscellular response to hypoxiaskeletal muscle tissue regenerationregulation of receptor activityregulation of smooth muscle cell migrationresponse to hyperoxiacytoplasmsecretory granuleextracellular regionapical part of cellextracellular spacecell surfaceextracellular exosomeserine-type endopeptidase activityreceptor bindingglycoprotein bindingphosphoprotein bindingblood coagulationresponse to peptide hormoneresponse to hypoxiaproteolysisfibrinolysisnegative regulation of proteolysisplasminogen activationcellular protein modification processsmooth muscle cell migrationplatelet-derived growth factor receptor signaling pathwayextracellular matrixextracellular regionplatelet alpha granule lumenplasma membraneextracellular spaceextracellular exosomeprotease bindingreceptor bindingserine-type endopeptidase inhibitor activityangiogenesisnegative regulation of smooth muscle cell migrationextracellular matrix organizationtransforming growth factor beta receptor signaling pathwaycellular response to lipopolysaccharideblood coagulationnegative regulation of smooth muscle cell-matrix adhesionnegative regulation of extrinsic apoptotic signaling pathway via death domain receptorsnegative regulation of endopeptidase activitynegative regulation of vascular wound healingpositive regulation of transcription from RNA polymerase II promoternegative regulation of wound healingchronological cell agingpositive regulation of angiogenesisplatelet degranulationdefense response to Gram-negative bacteriumpositive regulation of interleukin-8 productionfibrinolysisnegative regulation of blood coagulationpositive regulation of leukotriene production involved in inflammatory responsenegative regulation of fibrinolysisnegative regulation of cell adhesion mediated by integrinpositive regulation of monocyte chemotaxisplatelet activationpositive regulation of blood coagulationnegative regulation of cell migrationpositive regulation of receptor-mediated endocytosisgene expressionpositive regulation of inflammatory responsenegative regulation of endothelial cell apoptotic processtranscription initiation from RNA polymerase II promoterregulation of receptor activitycircadian rhythmnegative regulation of plasminogen activationtranscription, DNA-templatedcytoplasmextracellular regionplasma membraneextracellular spaceserine-type endopeptidase inhibitor activityblood coagulationnegative regulation of apoptotic processfibrinolysisnegative regulation of endopeptidase activityprotein C inhibitor-coagulation factor V complexmembraneprotein C inhibitor-coagulation factor Xa complexprotein complexprotein C inhibitor-coagulation factor XI complexprotein C inhibitor-KLK3 complexextracellular regionprotein C inhibitor-plasma kallikrein complexprotein C inhibitor-PLAT complexprotein C inhibitor-PLAU complexextracellular spaceplatelet dense tubular networkprotein C inhibitor-thrombin complexprotein C inhibitor-TMPRSS11E complexplatelet alpha granuleprotein C inhibitor-TMPRSS7 complexextracellular exosomeacrosomal membraneexternal side of plasma membraneprotease bindingheparin bindingserine-type endopeptidase inhibitor activityretinoic acid bindingphosphatidylcholine bindingglycosaminoglycan bindingacrosin bindingnegative regulation of endopeptidase activityblood coagulationspermatogenesisnegative regulation of hydrolase activitylipid transportfusion of sperm to egg plasma membraneendoplasmic reticulumplasma membranereceptor complexendosomelysosomecoated pitapical plasma membranebrush border membraneGolgi apparatusendocytic vesicleintegral component of membranelysosomal membraneextracellular exosomecalcium ion bindingretinoid metabolic processreceptor-mediated endocytosisforebrain developmentsteroid metabolic processendocytosislipid metabolic processvitamin D metabolic processphototransduction, visible lightcell proliferationsmall molecule metabolic processprotein glycosylationplasma membraneextracellular spaceextracellular exosomeintegral component of plasma membranebasolateral plasma membraneextrinsic component of plasma membraneserine-type endopeptidase activityserine-type peptidase activitycell morphogenesisproteolysisepithelial cell morphogenesis involved in placental branchingneural tube closurekeratinocyte differentiationextracellular matrixcell peripheryextracellular regionbasement membraneextracellular exosomebasal laminalaminin bindingcalcium ion bindingproteoglycan bindingcollagen bindingcell-matrix adhesionglomerular basement membrane developmentbasement membrane organizationextracellular matrix disassemblyextracellular matrix organizationpositive regulation of cell-substrate adhesion Serine-type peptidase activityUrokinase plasminogen activator receptor activitySerine-type endopeptidase activitySerine-type endopeptidase activitySerine-type endopeptidase inhibitor activitySerine-type endopeptidase inhibitor activitySerine-type endopeptidase inhibitor activityCalcium ion bindingSerine-type peptidase activityProteoglycan binding Plasmin dissolves the fibrin of blood clots and acts as a proteolytic factor in a variety of other processes including embryonic development, tissue remodeling, tumor invasion, and inflammation. In ovulation, weakens the walls of the Graafian follicle. It activates the urokinase-type plasminogen activator, collagenases and several complement zymogens, such as C1 and C5. Cleavage of fibronectin and laminin leads to cell detachment and apoptosis. Also cleaves fibrin, thrombospondin and von Willebrand factor. Its role in tissue remodeling and tumor invasion may be modulated by CSPG4. Binds to cells.Angiostatin is an angiogenesis inhibitor that blocks neovascularization and growth of experimental primary and metastatic tumors in vivo.Acts as a receptor for urokinase plasminogen activator. Plays a role in localizing and promoting plasmin formation. Mediates the proteolysis-independent signal transduction activation effects of U-PA. It is subject to negative-feedback regulation by U-PA which cleaves it into an inactive form.Specifically cleaves the zymogen plasminogen to form the active enzyme plasmin.Converts the abundant, but inactive, zymogen plasminogen to plasmin by hydrolyzing a single Arg-Val bond in plasminogen. By controlling plasmin-mediated proteolysis, it plays an important role in tissue remodeling and degradation, in cell migration and many other physiopathological events. Plays a direct role in facilitating neuronal migration.Serine protease inhibitor. This inhibitor acts as 'bait' for tissue plasminogen activator, urokinase, protein C and matriptase-3/TMPRSS7. Its rapid interaction with PLAT may function as a major control point in the regulation of fibrinolysis.Inhibits urokinase-type plasminogen activator. The monocyte derived PAI-2 is distinct from the endothelial cell-derived PAI-1.Heparin-dependent serine protease inhibitor acting in body fluids and secretions. Inactivates serine proteases by binding irreversibly to their serine activation site. Involved in the regulation of intravascular and extravascular proteolytic activities. Plays hemostatic roles in the blood plasma. Acts as a procoagulant and proinflammatory factor by inhibiting the anticoagulant activated protein C factor as well as the generation of activated protein C factor by the thrombin/thrombomodulin complex. Acts as an anticoagulant factor by inhibiting blood coagulation factors like prothrombin, factor XI, factor Xa, plasma kallikrein and fibrinolytic enzymes such as tissue- and urinary-type plasminogen activators. In seminal plasma, inactivates several serine proteases implicated in the reproductive system. Inhibits the serpin acrosin; indirectly protects component of the male genital tract from being degraded by excessive released acrosin. Inhibits tissue-and urinary-type plasminogen activator, prostate-specific antigen and kallikrein activities; has a control on the sperm motility and fertilization. Inhibits the activated protein C-catalyzed degradation of SEMG1 and SEMG2; regulates the degradation of semenogelin during the process of transfer of spermatozoa from the male reproductive tract into the female tract. In urine, inhibits urinary-type plasminogen activator and kallikrein activities. Inactivates membrane-anchored serine proteases activities such as MPRSS7 and TMPRSS11E. Inhibits urinary-type plasminogen activator-dependent tumor cell invasion and metastasis. May also play a non-inhibitory role in seminal plasma and urine as a hydrophobic hormone carrier by its binding to retinoic acid.Acts together with cubilin to mediate HDL endocytosis (By similarity). May participate in regulation of parathyroid-hormone and para-thyroid-hormone-related protein release.Degrades extracellular matrix. Proposed to play a role in breast cancer invasion and metastasis. Exhibits trypsin-like activity as defined by cleavage of synthetic substrates with Arg or Lys as the P1 site. Involved in the terminal differentiation of keratinocytes through prostasin (PRSS8) activation and filaggrin (FLG) processing.Sulfated glycoprotein widely distributed in basement membranes and tightly associated with laminin. Also binds to collagen IV and perlecan. It probably has a role in cell-extracellular matrix interactions. 12 minutes. Small fractions of the administered dose are excreted in bile and urine Proteolysis Urokinase administered by intravenous infusion is rapidly cleared by the liver. Small fractions of the administered dose are excreted in bile and urine Urokinase is used for the treatment of pulmonary embolisms. The low molecular weight form of human urokinase consists of an A chain of 2,000 daltons linked by a sulfhydryl bond to a B chain of 30,400 daltons. Urokinase is an enzyme (protein) produced by the kidney, and found in the urine. There are two forms of urokinase which differ in molecular weight but have similar clinical effects. Urokinase is the low molecular weight form. Urokinase acts on the endogenous fibrinolytic system. It converts plasminogen to the enzyme plasmin. Plasmin degrades fibrin clots as well as fibrinogen and some other plasma proteins. The therapeutic efficacy of Urokinase can be decreased when used in combination with Aprotinin.The risk or severity of adverse effects can be increased when Limaprost is combined with Urokinase.Urokinase may increase the anticoagulant activities of Dabigatran etexilate.The risk or severity of adverse effects can be increased when Salicylic acid is combined with Urokinase.The risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Urokinase.The risk or severity of adverse effects can be increased when Mesalazine is combined with Urokinase.The risk or severity of adverse effects can be increased when Diflunisal is combined with Urokinase.The risk or severity of adverse effects can be increased when Balsalazide is combined with Urokinase.The risk or severity of adverse effects can be increased when Olsalazine is combined with Urokinase.The risk or severity of adverse effects can be increased when Dersalazine is combined with Urokinase.The risk or severity of adverse effects can be increased when Aloxiprin is combined with Urokinase.The risk or severity of adverse effects can be increased when Guacetisal is combined with Urokinase.The risk or severity of adverse effects can be increased when Carbaspirin calcium is combined with Urokinase.The risk or severity of adverse effects can be increased when Hemoglobin crosfumaril is combined with Urokinase.The risk or severity of adverse effects can be increased when Methyl salicylate is combined with Urokinase.The risk or severity of adverse effects can be increased when Trolamine salicylate is combined with Urokinase.The risk or severity of adverse effects can be increased when Urokinase is combined with Treprostinil.Urokinase may increase the anticoagulant activities of Lepirudin.Urokinase may increase the anticoagulant activities of Bivalirudin.Urokinase may increase the anticoagulant activities of Abciximab.Urokinase may increase the anticoagulant activities of Becaplermin.Urokinase may increase the anticoagulant activities of Dicoumarol.Urokinase may increase the anticoagulant activities of Argatroban.Urokinase may increase the anticoagulant activities of Ardeparin.Urokinase may increase the anticoagulant activities of Phenindione.Urokinase may increase the anticoagulant activities of Fondaparinux sodium.Urokinase may increase the anticoagulant activities of Warfarin.Urokinase may increase the anticoagulant activities of Pentosan Polysulfate.Urokinase may increase the anticoagulant activities of Phenprocoumon.Urokinase may increase the anticoagulant activities of Edetic Acid.Urokinase may increase the anticoagulant activities of Heparin.Urokinase may increase the anticoagulant activities of Enoxaparin.Urokinase may increase the anticoagulant activities of Acenocoumarol.Urokinase may increase the anticoagulant activities of Citric Acid.Urokinase may increase the anticoagulant activities of Ximelagatran.Urokinase may increase the anticoagulant activities of Ancrod.Urokinase may increase the anticoagulant activities of Pentaerythritol Tetranitrate.Urokinase may increase the anticoagulant activities of Rivaroxaban.Urokinase may increase the anticoagulant activities of Sulodexide.Urokinase may increase the anticoagulant activities of Idraparinux.Urokinase may increase the anticoagulant activities of Apixaban.Urokinase may increase the anticoagulant activities of Otamixaban.Urokinase may increase the anticoagulant activities of Danaparoid.Urokinase may increase the anticoagulant activities of Dalteparin.Urokinase may increase the anticoagulant activities of Ferulic acid.Urokinase may increase the anticoagulant activities of Ethyl biscoumacetate.Urokinase may increase the anticoagulant activities of Nadroparin.Urokinase may increase the anticoagulant activities of Edoxaban.Urokinase may increase the anticoagulant activities of Dextran.Urokinase may increase the anticoagulant activities of Reviparin.Urokinase may increase the anticoagulant activities of Certoparin.Urokinase may increase the anticoagulant activities of Dextran 70.Urokinase may increase the anticoagulant activities of Desirudin.Urokinase may increase the anticoagulant activities of Dextran 40.Urokinase may increase the anticoagulant activities of Dextran 75.Urokinase may increase the anticoagulant activities of Protocatechualdehyde.Urokinase may increase the anticoagulant activities of Protein C.Urokinase may increase the anticoagulant activities of Antithrombin III human.Urokinase may increase the anticoagulant activities of Fondaparinux.Urokinase may increase the anticoagulant activities of Letaxaban.Urokinase may increase the anticoagulant activities of Darexaban.Urokinase may increase the anticoagulant activities of Nafamostat.Urokinase may increase the anticoagulant activities of Gabexate.Urokinase may increase the anticoagulant activities of Troxerutin.Urokinase may increase the anticoagulant activities of Fluindione.Urokinase may increase the anticoagulant activities of Protein S human.Urokinase may increase the anticoagulant activities of Melagatran.Eptifibatide may increase the anticoagulant activities of Urokinase.Ticlopidine may increase the anticoagulant activities of Urokinase.Tirofiban may increase the anticoagulant activities of Urokinase.Dipyridamole may increase the anticoagulant activities of Urokinase.Clopidogrel may increase the anticoagulant activities of Urokinase.Acetylsalicylic acid may increase the anticoagulant activities of Urokinase.Prasugrel may increase the anticoagulant activities of Urokinase.Vorapaxar may increase the anticoagulant activities of Urokinase.Milrinone may increase the anticoagulant activities of Urokinase.Anagrelide may increase the anticoagulant activities of Urokinase.Epinastine may increase the anticoagulant activities of Urokinase.Alprostadil may increase the anticoagulant activities of Urokinase.Pentoxifylline may increase the anticoagulant activities of Urokinase.Azelastine may increase the anticoagulant activities of Urokinase.Iloprost may increase the anticoagulant activities of Urokinase.Cilostazol may increase the anticoagulant activities of Urokinase.Ridogrel may increase the anticoagulant activities of Urokinase.Sevoflurane may increase the anticoagulant activities of Urokinase.Epoprostenol may increase the anticoagulant activities of Urokinase.Resveratrol may increase the anticoagulant activities of Urokinase.Nimesulide may increase the anticoagulant activities of Urokinase.Tesmilifene may increase the anticoagulant activities of Urokinase.Defibrotide may increase the anticoagulant activities of Urokinase.SRT501 may increase the anticoagulant activities of Urokinase.Beraprost may increase the anticoagulant activities of Urokinase.Ibudilast may increase the anticoagulant activities of Urokinase.Andrographolide may increase the anticoagulant activities of Urokinase.eplivanserine may increase the anticoagulant activities of Urokinase.Cangrelor may increase the anticoagulant activities of Urokinase.Tranilast may increase the anticoagulant activities of Urokinase.Triflusal may increase the anticoagulant activities of Urokinase.Icosapent ethyl may increase the anticoagulant activities of Urokinase.Ifenprodil may increase the anticoagulant activities of Urokinase.Trapidil may increase the anticoagulant activities of Urokinase.Naftopidil may increase the anticoagulant activities of Urokinase.Sarpogrelate may increase the anticoagulant activities of Urokinase.Eplivanserin may increase the anticoagulant activities of Urokinase.Ifetroban may increase the anticoagulant activities of Urokinase.Nitroaspirin may increase the anticoagulant activities of Urokinase.Ketanserin may increase the anticoagulant activities of Urokinase.Indobufen may increase the anticoagulant activities of Urokinase.Butylphthalide may increase the anticoagulant activities of Urokinase.Hydroxytyrosol may increase the anticoagulant activities of Urokinase.Ramatroban may increase the anticoagulant activities of Urokinase.Picotamide may increase the anticoagulant activities of Urokinase.Cloricromen may increase the anticoagulant activities of Urokinase.Linsidomine may increase the anticoagulant activities of Urokinase.Buflomedil may increase the anticoagulant activities of Urokinase.Relcovaptan may increase the anticoagulant activities of Urokinase.Ticagrelor may increase the anticoagulant activities of Urokinase. DB06692DB09211DB06695DB00936DB00233DB00244DB00861DB01014DB01250DB06251DB13509DB13538DB13612DB13864DB09543DB11079DB00374DB00001DB00006DB00054DB00102DB00266DB00278DB00407DB00498DB00569DB00682DB00686DB00946DB00974DB01109DB01225DB01418DB04272DB04898DB05099DB06154DB06228DB06271DB06406DB06605DB06635DB06754DB06779DB07767DB08794DB08813DB09075DB09255DB09259DB09261DB11076DB11095DB11122DB11241DB11268DB11312DB11598DB11728DB11984DB12289DB12598DB12831DB13124DB13136DB13149DB13616DB00063DB00208DB00775DB00975DB00758DB00945DB06209DB09030DB00235DB00261DB00751DB00770DB00806DB00972DB01088DB01166DB01207DB01236DB01240DB02709DB04743DB04905DB04932DB05073DB05229DB05266DB05767DB06392DB06441DB07615DB08814DB08887DB08954DB09283DB12092DB12163DB12177DB12321DB12445DB12465DB12545DB12749DB12771DB13036DB13327DB13367DB13400DB13510DB13929DB08816 AprotininLimaprostDabigatran etexilateSalicylic acidAminosalicylic AcidMesalazineDiflunisalBalsalazideOlsalazineDersalazineAloxiprinGuacetisalCarbaspirin calciumHemoglobin crosfumarilMethyl salicylateTrolamine salicylateTreprostinilLepirudinBivalirudinAbciximabBecaplerminDicoumarolArgatrobanArdeparinPhenindioneFondaparinux sodiumWarfarinPentosan PolysulfatePhenprocoumonEdetic AcidHeparinEnoxaparinAcenocoumarolCitric AcidXimelagatranAncrodPentaerythritol TetranitrateRivaroxabanSulodexideIdraparinuxApixabanOtamixabanDanaparoidDalteparinFerulic acidEthyl biscoumacetateNadroparinEdoxabanDextranReviparinCertoparinDextran 70DesirudinDextran 40Dextran 75ProtocatechualdehydeProtein CAntithrombin III humanFondaparinuxLetaxabanDarexabanNafamostatGabexateTroxerutinFluindioneProtein S humanMelagatranEptifibatideTiclopidineTirofibanDipyridamoleClopidogrelAcetylsalicylic acidPrasugrelVorapaxarMilrinoneAnagrelideEpinastineAlprostadilPentoxifyllineAzelastineIloprostCilostazolRidogrelSevofluraneEpoprostenolResveratrolNimesulideTesmilifeneDefibrotideSRT501BeraprostIbudilastAndrographolideeplivanserineCangrelorTranilastTriflusalIcosapent ethylIfenprodilTrapidilNaftopidilSarpogrelateEplivanserinIfetrobanNitroaspirinKetanserinIndobufenButylphthalideHydroxytyrosolRamatrobanPicotamideCloricromenLinsidomineBuflomedilRelcovaptanTicagrelor Melting PointHydrophobicityIsoelectric PointMolecular WeightMolecular Formula 76 °C at pH 4.5-0.4668.6631126.5C1376H2145N383O406S18 Nowak, U.K. et al., Biochemistry 33:2951-2960 (1994) B01AD04 EnzymesANTITHROMBOTIC AGENTSANTITHROMBOTIC AGENTSBLOOD AND BLOOD FORMING ORGANS B01ADB01AB01B Amino Acids, Peptides, and ProteinsBiological FactorsBlood and Blood Forming OrgansBlood Coagulation FactorsBlood ProteinsEndopeptidasesEnzymesEnzymes and CoenzymesFibrinolytic AgentsHydrolasesPeptide HydrolasesPlasminogen ActivatorsProteinsSerine EndopeptidasesSerine Proteases D000602D001685D001779D001798D010450D004798D045762D005343D006867D010447D010960D011506D012697D057057 201246506299X02419PA451836P00749DAP001194UrokinaseCHEMBL1201420 Drugs Product Database (DPD)PubChem SubstanceGenBankPharmGKBUniProtKBTherapeutic Targets DatabaseWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/pharmclips2.cgi?keyword=%20Abbokinase%AEhttp://www.drugs.com/mtm/urokinase.html Housley C: Contract purchasing means a buyer's market. Dimens Health Serv. 1976 Apr;53(4):16, 19-20. 5328 approvedinvestigationalwithdrawn Abbott LaboratoriesMicrobix Biosystems Inc. AbbokinaseKinlytic Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides drug_action DB00013DB01022DB01373 UrokinasePhylloquinoneCalcium P00747P00748P02452P03952P03951P00740P00451P00734P12259P00742P02671P02675P02679P00488P05160P00750P08709P13726Q9BQB6P38435 Urokinase Action Pathway SMP00284 Microbix biosystems inc false UrokinaseUrokinase Kinlytic Open-cathKinlytic (urokinase for Injection) Hospira Inc.ImaRx TherapeuticsMicrobix Biosystems Inc. http://www.hospira.comhttp://www.imarx.comhttp://www.microbix.com Kinlytic (urokinase for Injection)Kinlytic Open-cath falsefalse Microbix Biosystems IncMicrobix Biosystems Inc falsefalse IntravenousIntravenous Powder, for solutionPowder, for solution DPDDPD 250000 unit5000 unit truetrue 0074970200886777 CanadaCanada 1988-12-311991-12-31 2009-10-282009-10-28 !BL[~wPPkIm}Msrm{Fa_ibm{Fa_ilBYJwmeXAh_GqjlFBm{pIg~@ELXFa_iah_Jwo`YYNgwzXZGyb@JlivU`Jwlk^xa}bGw_ih`BJwmeXM~fFa_ibm{YV@k^qh_wz[_im~fpIdk^rm{JwlZG}~fwzXk^|BYf]_ij[@Fa_iah_Jwo@fRm{wzXZGvU`Jwlk^{}NIm|ZGvHS\~wRm{@haah_Xc@fRm{_y}mvH }yv:jU;vhjfzUgnx:rxyEbnbs7zripLfn:CvhipquBnr5jj1_emK8Jp1fot@mB9N_Y0lV DB00014 65807-02-5 Goserelin small molecule 0F65R8P09N 1269.4105 Kripa S. Srivastava, Matthew R. Davis, "Solid Phase Peptide for the Production of Goserelin." U.S. Patent US20100311946, issued December 09, 2010. solid Goserelin is a synthetic hormone. In men, it stops the production of the hormone testosterone, which may stimulate the growth of cancer cells. In women, goserelin decreases the production of the hormone estradiol (which may stimulate the growth of cancer cells) to levels similar to a postmenopausal state. When the medication is stopped, hormone levels return to normal. Humans and other mammals ImplantImplantImplantImplant SubcutaneousSubcutaneousSubcutaneousSubcutaneous 10.8 mg/13.6 mg/13.6 mg10.8 mg Used to treat hormone-sensitive cancers of the breast (in pre- and peri- menopausal women) and prostate, and some benign gynaecological disorders (endometriosis, uterine fibroids and endometrial thinning). In addition, goserelin is used in assisted reproduction and in the treatment of precocious puberty. Goserelin is a synthetic decapeptide analogue of LHRH. Goserelin acts as a potent inhibitor of pituitary gonadotropin secretion when administered in the biodegradable formulation. The result is sustained suppression of LH and serum testosterone levels. agonistagonist Lutropin-choriogonadotropic hormone receptorGonadotropin-releasing hormone receptor BE0000134BE0000203 HumanHuman Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Kirby RS, Fitzpatrick JM, Clarke N: Abarelix and other gonadotrophin-releasing hormone antagonists in prostate cancer. BJU Int. 2009 Dec;104(11):1580-4. doi: 10.1111/j.1464-410X.2009.08924.x.Kirby RS, Fitzpatrick JM, Clarke N: Abarelix and other gonadotrophin-releasing hormone antagonists in prostate cancer. BJU Int. 2009 Dec;104(11):1580-4. doi: 10.1111/j.1464-410X.2009.08924.x. 17139284170164232005318920053189 P22888P30968 Lutropin-choriogonadotropic hormone receptorGonadotropin-releasing hormone receptor 2p214q21.2 HumanHuman plasma membraneintegral component of plasma membraneendosomeG-protein coupled peptide receptor activitychoriogonadotropin hormone bindingchoriogonadotropin hormone receptor activityluteinizing hormone receptor activitypositive regulation of cAMP-mediated signalingspermatogenesispositive regulation of inositol trisphosphate biosynthetic processuterus developmentactivation of adenylate cyclase activityG-protein coupled receptor signaling pathwayphospholipase C-activating G-protein coupled receptor signaling pathwaycellular response to gonadotropin stimulusG-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerfemale gonad developmentcognitionluteinizing hormone signaling pathwayadenylate cyclase-activating G-protein coupled receptor signaling pathwaymale genitalia developmenthormone-mediated signaling pathwayovulation cycle processmale gonad developmentmembraneplasma membraneintegral component of plasma membranegonadotropin-releasing hormone receptor activitypeptide bindingG-protein coupled receptor signaling pathwaymulticellular organismal developmentcellular response to gonadotropin-releasing hormone Luteinizing hormone receptor activityPeptide binding Receptor for lutropin-choriogonadotropic hormone. The activity of this receptor is mediated by G proteins which activate adenylate cyclase.Receptor for gonadotropin releasing hormone (GnRH) that mediates the action of GnRH to stimulate the secretion of the gonadotropic hormones luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This receptor mediates its action by association with G-proteins that activate a phosphatidylinositol-calcium second messenger system. Isoform 2 may act as an inhibitor of GnRH-R signaling. 27.3% No experience of overdosage from clinical trials. 4-5 hours Inactive orally, rapidly absorbed following subcutaneous administration. Hepatic * 121 +/- 42.4 mL/min [prostate cancer with 10.8 mg depot] * 44.1 ± 13.6 L [subcutaneous administration of 250 mcg] Clearance of goserelin following subcutaneous administration of a radiolabeled solution of goserelin was very rapid and occurred via a combination of hepatic and urinary excretion. More than 90% of a subcutaneous radiolabeled solution formulation dose of goserelin was excreted in urine. The pharmacokinetics of goserelin have been determined in both male and female healthy volunteers and patients. In these studies, goserelin was administered as a single 250µg (aqueous solution) dose and as a single or multiple 3.6 mg depot dose by subcutaneous route. Trastuzumab may increase the cardiotoxic activities of Goserelin.Leuprolide may increase the QTc-prolonging activities of Goserelin.Goserelin may increase the QTc-prolonging activities of Erythromycin.Goserelin may increase the QTc-prolonging activities of Azithromycin.Goserelin may increase the QTc-prolonging activities of Moxifloxacin.Goserelin may increase the QTc-prolonging activities of Sulfisoxazole.Goserelin may increase the QTc-prolonging activities of Methadone.Goserelin may increase the QTc-prolonging activities of Clozapine.Goserelin may increase the QTc-prolonging activities of Promazine.Goserelin may increase the QTc-prolonging activities of Droperidol.Goserelin may increase the QTc-prolonging activities of Chlorpromazine.Goserelin may increase the QTc-prolonging activities of Haloperidol.Goserelin may increase the QTc-prolonging activities of Ciprofloxacin.Goserelin may increase the QTc-prolonging activities of Perflutren.Goserelin may increase the QTc-prolonging activities of Chloroquine.Goserelin may increase the QTc-prolonging activities of Pentamidine.Goserelin may increase the QTc-prolonging activities of Gadobenic acid.Goserelin may increase the QTc-prolonging activities of Dolasetron.Goserelin may increase the QTc-prolonging activities of Granisetron.Goserelin may increase the QTc-prolonging activities of Ondansetron.Goserelin may increase the QTc-prolonging activities of Telithromycin.Goserelin may increase the QTc-prolonging activities of Primaquine.Goserelin may increase the QTc-prolonging activities of Levofloxacin.Goserelin may increase the QTc-prolonging activities of Gemifloxacin.Goserelin may increase the QTc-prolonging activities of Ofloxacin.Goserelin may increase the QTc-prolonging activities of Propafenone.Goserelin may increase the QTc-prolonging activities of Flecainide.Goserelin may increase the QTc-prolonging activities of Clarithromycin.Goserelin may increase the QTc-prolonging activities of Saquinavir.Goserelin may increase the QTc-prolonging activities of Telavancin.Goserelin may increase the QTc-prolonging activities of Pazopanib.Goserelin may increase the QTc-prolonging activities of Panobinostat.Goserelin may increase the QTc-prolonging activities of Crizotinib.Goserelin may increase the QTc-prolonging activities of Bedaquiline.Goserelin may increase the QTc-prolonging activities of Ceritinib.Goserelin may increase the QTc-prolonging activities of Lenvatinib.The risk or severity of cytotoxicity can be increased when Ancestim is combined with Goserelin.Ivabradine may increase the QTc-prolonging activities of Goserelin.The risk or severity of adverse effects can be increased when Paclitaxel is combined with Goserelin.The risk or severity of adverse effects can be increased when Docetaxel is combined with Goserelin.The risk or severity of adverse effects can be increased when Cabazitaxel is combined with Goserelin.Digoxin may decrease the cardiotoxic activities of Goserelin.Acetyldigitoxin may decrease the cardiotoxic activities of Goserelin.Deslanoside may decrease the cardiotoxic activities of Goserelin.Ouabain may decrease the cardiotoxic activities of Goserelin.Digitoxin may decrease the cardiotoxic activities of Goserelin.Cymarin may decrease the cardiotoxic activities of Goserelin.Proscillaridin may decrease the cardiotoxic activities of Goserelin.Metildigoxin may decrease the cardiotoxic activities of Goserelin.Peruvoside may decrease the cardiotoxic activities of Goserelin.Lanatoside C may decrease the cardiotoxic activities of Goserelin.Gitoformate may decrease the cardiotoxic activities of Goserelin.Acetyldigoxin may decrease the cardiotoxic activities of Goserelin.Oleandrin may decrease the cardiotoxic activities of Goserelin.Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Goserelin.Bevacizumab may increase the cardiotoxic activities of Goserelin.Cyclophosphamide may increase the cardiotoxic activities of Goserelin.Octreotide may increase the QTc-prolonging activities of Goserelin.Oxytocin may increase the QTc-prolonging activities of Goserelin.Bortezomib may increase the QTc-prolonging activities of Goserelin.Fluconazole may increase the QTc-prolonging activities of Goserelin.Nelfinavir may increase the QTc-prolonging activities of Goserelin.Ranolazine may increase the QTc-prolonging activities of Goserelin.Isradipine may increase the QTc-prolonging activities of Goserelin.Venlafaxine may increase the QTc-prolonging activities of Goserelin.Atomoxetine may increase the QTc-prolonging activities of Goserelin.Amitriptyline may increase the QTc-prolonging activities of Goserelin.Olanzapine may increase the QTc-prolonging activities of Goserelin.Protriptyline may increase the QTc-prolonging activities of Goserelin.Alfuzosin may increase the QTc-prolonging activities of Goserelin.Mefloquine may increase the QTc-prolonging activities of Goserelin.Mirtazapine may increase the QTc-prolonging activities of Goserelin.Treprostinil may increase the QTc-prolonging activities of Goserelin.Sorafenib may increase the QTc-prolonging activities of Goserelin.Trimethoprim may increase the QTc-prolonging activities of Goserelin.Imipramine may increase the QTc-prolonging activities of Goserelin.Ritonavir may increase the QTc-prolonging activities of Goserelin.Foscarnet may increase the QTc-prolonging activities of Goserelin.Nortriptyline may increase the QTc-prolonging activities of Goserelin.Amoxapine may increase the QTc-prolonging activities of Goserelin.Hydroxyzine may increase the QTc-prolonging activities of Goserelin.Voriconazole may increase the QTc-prolonging activities of Goserelin.Nicardipine may increase the QTc-prolonging activities of Goserelin.Trazodone may increase the QTc-prolonging activities of Goserelin.Galantamine may increase the QTc-prolonging activities of Goserelin.Tamoxifen may increase the QTc-prolonging activities of Goserelin.Moexipril may increase the QTc-prolonging activities of Goserelin.Tizanidine may increase the QTc-prolonging activities of Goserelin.Ibandronate may increase the QTc-prolonging activities of Goserelin.Apomorphine may increase the QTc-prolonging activities of Goserelin.Paroxetine may increase the QTc-prolonging activities of Goserelin.Trimipramine may increase the QTc-prolonging activities of Goserelin.Risperidone may increase the QTc-prolonging activities of Goserelin.Isoflurane may increase the QTc-prolonging activities of Goserelin.Indapamide may increase the QTc-prolonging activities of Goserelin.Propofol may increase the QTc-prolonging activities of Goserelin.Vardenafil may increase the QTc-prolonging activities of Goserelin.Terbutaline may increase the QTc-prolonging activities of Goserelin.Amantadine may increase the QTc-prolonging activities of Goserelin.Metronidazole may increase the QTc-prolonging activities of Goserelin.Famotidine may increase the QTc-prolonging activities of Goserelin.Maprotiline may increase the QTc-prolonging activities of Goserelin.Salmeterol may increase the QTc-prolonging activities of Goserelin.Felbamate may increase the QTc-prolonging activities of Goserelin.Formoterol may increase the QTc-prolonging activities of Goserelin.Salbutamol may increase the QTc-prolonging activities of Goserelin.Sulfamethoxazole may increase the QTc-prolonging activities of Goserelin.Ketoconazole may increase the QTc-prolonging activities of Goserelin.Tolterodine may increase the QTc-prolonging activities of Goserelin.Norfloxacin may increase the QTc-prolonging activities of Goserelin.Promethazine may increase the QTc-prolonging activities of Goserelin.Atazanavir may increase the QTc-prolonging activities of Goserelin.Diphenhydramine may increase the QTc-prolonging activities of Goserelin.Sertraline may increase the QTc-prolonging activities of Goserelin.Doxepin may increase the QTc-prolonging activities of Goserelin.Desipramine may increase the QTc-prolonging activities of Goserelin.Itraconazole may increase the QTc-prolonging activities of Goserelin.Desflurane may increase the QTc-prolonging activities of Goserelin.Metoclopramide may increase the QTc-prolonging activities of Goserelin.Sevoflurane may increase the QTc-prolonging activities of Goserelin.Aripiprazole may increase the QTc-prolonging activities of Goserelin.Clomipramine may increase the QTc-prolonging activities of Goserelin.Dasatinib may increase the QTc-prolonging activities of Goserelin.Lapatinib may increase the QTc-prolonging activities of Goserelin.Posaconazole may increase the QTc-prolonging activities of Goserelin.Sunitinib may increase the QTc-prolonging activities of Goserelin.Arformoterol may increase the QTc-prolonging activities of Goserelin.Lithium may increase the QTc-prolonging activities of Goserelin.Methotrimeprazine may increase the QTc-prolonging activities of Goserelin.Solifenacin may increase the QTc-prolonging activities of Goserelin.Thiothixene may increase the QTc-prolonging activities of Goserelin.Vorinostat may increase the QTc-prolonging activities of Goserelin.Ezogabine may increase the QTc-prolonging activities of Goserelin.Indacaterol may increase the QTc-prolonging activities of Goserelin.Pasireotide may increase the QTc-prolonging activities of Goserelin.Degarelix may increase the QTc-prolonging activities of Goserelin.Buserelin may increase the QTc-prolonging activities of Goserelin.Histrelin may increase the QTc-prolonging activities of Goserelin.Triptorelin may increase the QTc-prolonging activities of Goserelin.Rilpivirine may increase the QTc-prolonging activities of Goserelin.Fingolimod may increase the QTc-prolonging activities of Goserelin.Eribulin may increase the QTc-prolonging activities of Goserelin.Mirabegron may increase the QTc-prolonging activities of Goserelin.Dabrafenib may increase the QTc-prolonging activities of Goserelin.Olodaterol may increase the QTc-prolonging activities of Goserelin.Vilanterol may increase the QTc-prolonging activities of Goserelin.The therapeutic efficacy of Choline C 11 can be decreased when used in combination with Goserelin.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Goserelin.The therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Goserelin.The therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Goserelin.The therapeutic efficacy of Insulin Pork can be decreased when used in combination with Goserelin.The therapeutic efficacy of Troglitazone can be decreased when used in combination with Goserelin.The therapeutic efficacy of Glimepiride can be decreased when used in combination with Goserelin.The therapeutic efficacy of Acarbose can be decreased when used in combination with Goserelin.The therapeutic efficacy of Metformin can be decreased when used in combination with Goserelin.The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Goserelin.The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Goserelin.The therapeutic efficacy of Miglustat can be decreased when used in combination with Goserelin.The therapeutic efficacy of Miglitol can be decreased when used in combination with Goserelin.The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Goserelin.The therapeutic efficacy of Nateglinide can be decreased when used in combination with Goserelin.The therapeutic efficacy of Tolazamide can be decreased when used in combination with Goserelin.The therapeutic efficacy of Repaglinide can be decreased when used in combination with Goserelin.The therapeutic efficacy of Phenformin can be decreased when used in combination with Goserelin.The therapeutic efficacy of Glyburide can be decreased when used in combination with Goserelin.The therapeutic efficacy of Glipizide can be decreased when used in combination with Goserelin.The therapeutic efficacy of Gliclazide can be decreased when used in combination with Goserelin.The therapeutic efficacy of Tolbutamide can be decreased when used in combination with Goserelin.The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Goserelin.The therapeutic efficacy of Gliquidone can be decreased when used in combination with Goserelin.The therapeutic efficacy of Mitiglinide can be decreased when used in combination with Goserelin.The therapeutic efficacy of Sitagliptin can be decreased when used in combination with Goserelin.The therapeutic efficacy of Exenatide can be decreased when used in combination with Goserelin.The therapeutic efficacy of Pramlintide can be decreased when used in combination with Goserelin.The therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Goserelin.The therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Goserelin.The therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Goserelin.The therapeutic efficacy of AICA ribonucleotide can be decreased when used in combination with Goserelin.The therapeutic efficacy of Castanospermine can be decreased when used in combination with Goserelin.The therapeutic efficacy of Buformin can be decreased when used in combination with Goserelin.The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Goserelin.The therapeutic efficacy of Voglibose can be decreased when used in combination with Goserelin.The therapeutic efficacy of Alogliptin can be decreased when used in combination with Goserelin.The therapeutic efficacy of Sulodexide can be decreased when used in combination with Goserelin.The therapeutic efficacy of Saxagliptin can be decreased when used in combination with Goserelin.The therapeutic efficacy of Liraglutide can be decreased when used in combination with Goserelin.The therapeutic efficacy of Linagliptin can be decreased when used in combination with Goserelin.The therapeutic efficacy of Canagliflozin can be decreased when used in combination with Goserelin.The therapeutic efficacy of Glibornuride can be decreased when used in combination with Goserelin.The therapeutic efficacy of Empagliflozin can be decreased when used in combination with Goserelin.The therapeutic efficacy of Dulaglutide can be decreased when used in combination with Goserelin.The therapeutic efficacy of Ciglitazone can be decreased when used in combination with Goserelin.The therapeutic efficacy of Allicin can be decreased when used in combination with Goserelin.The therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Goserelin.The therapeutic efficacy of Bempedoic acid can be decreased when used in combination with Goserelin.The therapeutic efficacy of Gusperimus can be decreased when used in combination with Goserelin.The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Goserelin.The therapeutic efficacy of Balaglitazone can be decreased when used in combination with Goserelin.The therapeutic efficacy of Deoxyspergualin can be decreased when used in combination with Goserelin.The therapeutic efficacy of Carbutamide can be decreased when used in combination with Goserelin.Goserelin may increase the QTc-prolonging activities of Dofetilide.Goserelin may increase the QTc-prolonging activities of Citalopram.Goserelin may increase the QTc-prolonging activities of Ziprasidone.Goserelin may increase the QTc-prolonging activities of Anagrelide.Goserelin may increase the QTc-prolonging activities of Disopyramide.Goserelin may increase the QTc-prolonging activities of Ibutilide.Goserelin may increase the QTc-prolonging activities of Quinine.Goserelin may increase the QTc-prolonging activities of Fluoxetine.Goserelin may increase the QTc-prolonging activities of Sotalol.Goserelin may increase the QTc-prolonging activities of Toremifene.Goserelin may increase the QTc-prolonging activities of Cisapride.Goserelin may increase the QTc-prolonging activities of Thioridazine.Goserelin may increase the QTc-prolonging activities of Mifepristone.Goserelin may increase the QTc-prolonging activities of Flupentixol.Goserelin may increase the QTc-prolonging activities of Quinidine.Goserelin may increase the QTc-prolonging activities of Procainamide.Goserelin may increase the QTc-prolonging activities of Pimozide.Goserelin may increase the QTc-prolonging activities of Amiodarone.Goserelin may increase the QTc-prolonging activities of Arsenic trioxide.Goserelin may increase the QTc-prolonging activities of Escitalopram.Goserelin may increase the QTc-prolonging activities of Domperidone.Goserelin may increase the QTc-prolonging activities of Quetiapine.Goserelin may increase the QTc-prolonging activities of Paliperidone.Goserelin may increase the QTc-prolonging activities of Lopinavir.Goserelin may increase the QTc-prolonging activities of Zuclopenthixol.Goserelin may increase the QTc-prolonging activities of Tetrabenazine.Goserelin may increase the QTc-prolonging activities of Dronedarone.Goserelin may increase the QTc-prolonging activities of Nilotinib.Goserelin may increase the QTc-prolonging activities of Iloperidone.Goserelin may increase the QTc-prolonging activities of Vandetanib.Goserelin may increase the QTc-prolonging activities of Asenapine.Goserelin may increase the QTc-prolonging activities of Artemether.Goserelin may increase the QTc-prolonging activities of Lumefantrine.Goserelin may increase the QTc-prolonging activities of Vemurafenib.Goserelin may increase the QTc-prolonging activities of Eliglustat.Goserelin may decrease effectiveness of Capromab pendetide as a diagnostic agent. 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TrastuzumabLeuprolideErythromycinAzithromycinMoxifloxacinSulfisoxazoleMethadoneClozapinePromazineDroperidolChlorpromazineHaloperidolCiprofloxacinPerflutrenChloroquinePentamidineGadobenic acidDolasetronGranisetronOndansetronTelithromycinPrimaquineLevofloxacinGemifloxacinOfloxacinPropafenoneFlecainideClarithromycinSaquinavirTelavancinPazopanibPanobinostatCrizotinibBedaquilineCeritinibLenvatinibAncestimIvabradinePaclitaxelDocetaxelCabazitaxelDigoxinAcetyldigitoxinDeslanosideOuabainDigitoxinCymarinProscillaridinMetildigoxinPeruvosideLanatoside CGitoformateAcetyldigoxinOleandrinDigoxin Immune Fab (Ovine)BevacizumabCyclophosphamideOctreotideOxytocinBortezomibFluconazoleNelfinavirRanolazineIsradipineVenlafaxineAtomoxetineAmitriptylineOlanzapineProtriptylineAlfuzosinMefloquineMirtazapineTreprostinilSorafenibTrimethoprimImipramineRitonavirFoscarnetNortriptylineAmoxapineHydroxyzineVoriconazoleNicardipineTrazodoneGalantamineTamoxifenMoexiprilTizanidineIbandronateApomorphineParoxetineTrimipramineRisperidoneIsofluraneIndapamidePropofolVardenafilTerbutalineAmantadineMetronidazoleFamotidineMaprotilineSalmeterolFelbamateFormoterolSalbutamolSulfamethoxazoleKetoconazoleTolterodineNorfloxacinPromethazineAtazanavirDiphenhydramineSertralineDoxepinDesipramineItraconazoleDesfluraneMetoclopramideSevofluraneAripiprazoleClomipramineDasatinibLapatinibPosaconazoleSunitinibArformoterolLithiumMethotrimeprazineSolifenacinThiothixeneVorinostatEzogabineIndacaterolPasireotideDegarelixBuserelinHistrelinTriptorelinRilpivirineFingolimodEribulinMirabegronDabrafenibOlodaterolVilanterolCholine C 11Insulin HumanInsulin LisproInsulin GlargineInsulin PorkTroglitazoneGlimepirideAcarboseMetforminRosiglitazoneAcetohexamideMiglustatMiglitolChlorpropamideNateglinideTolazamideRepaglinidePhenforminGlyburideGlipizideGliclazideTolbutamidePioglitazoneGliquidoneMitiglinideSitagliptinExenatidePramlintideInsulin AspartInsulin DetemirInsulin GlulisineAICA ribonucleotideCastanospermineBuforminVildagliptinVogliboseAlogliptinSulodexideSaxagliptinLiraglutideLinagliptinCanagliflozinGlibornurideEmpagliflozinDulaglutideCiglitazoneAllicin2,4-thiazolidinedioneBempedoic acidGusperimusSotagliflozinBalaglitazoneDeoxyspergualinCarbutamideDofetilideCitalopramZiprasidoneAnagrelideDisopyramideIbutilideQuinineFluoxetineSotalolToremifeneCisaprideThioridazineMifepristoneFlupentixolQuinidineProcainamidePimozideAmiodaroneArsenic trioxideEscitalopramDomperidoneQuetiapinePaliperidoneLopinavirZuclopenthixolTetrabenazineDronedaroneNilotinibIloperidoneVandetanibAsenapineArtemetherLumefantrineVemurafenibEliglustatCapromab pendetide Water SolubilitylogP Soluble-2 L02AE03 Gonadotropin releasing hormone analoguesHORMONES AND RELATED AGENTSENDOCRINE THERAPYANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L02AEL02AL02L Amino Acids, Peptides, and ProteinsAntineoplastic AgentsAntineoplastic Agents, HormonalAntineoplastic and Immunomodulating AgentsChemical Actions and UsesEndocrine TherapyGonadotropin Releasing Hormone Receptor AgonistGonadotropin-Releasing HormoneGonadotropinsHormonesHormones and Related AgentsHormones, Hormone Substitutes, and Hormone AntagonistsHyperglycemia-Associated AgentsHypothalamic HormonesMiscellaneous Therapeutic AgentsModerate Risk QTc-Prolonging AgentsNerve Tissue ProteinsNeuropeptidesOligopeptidesPeptide HormonesPeptidesPharmacologic ActionsPhysiological Effects of DrugsPituitary Hormone-Releasing HormonesProteinsTherapeutic Uses D000602D000970D018931D020164D007987D006062D006728D006730D007028D009419D009479D009842D036361D010455D020228D045505D010906D011506D045506 111675523531112846507336D005734470656PA164747674DAP000023GoserelinCHEMBL1201247 Drugs Product Database (DPD)ChEBIPubChem CompoundPubChem SubstanceKEGG DrugChemSpiderPharmGKBTherapeutic Targets DatabaseWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic/goserel.htmhttp://www.drugs.com/cdi/goserelin.html //s3-us-west-2.amazonaws.com/drugbank/fda_labels/DB00014.pdf?1265922794 approved Zoladex Organic compounds Organic acids and derivatives Carboxylic acids and derivatives Amino acids, peptides, and analogues This compound belongs to the class of organic compounds known as oligopeptides. These are organic compounds containing a sequence of between three and ten alpha-amino acids joined by peptide bonds. Oligopeptides 1-hydroxy-2-unsubstituted benzenoids3-alkylindolesAlpha amino acid amidesAmphetamines and derivativesAzacyclic compoundsCarbonyl compoundsCarboximidamidesCarboxylic acid hydrazidesDialkyl ethersGuanidinesHeteroaromatic compoundsHistidine and derivativesHydrazinecarboxamidesHydrocarbon derivativesImidazolesLactamsLeucine and derivativesN-acyl aminesN-acyl-alpha amino acids and derivativesN-acylpyrrolidinesOrganic carbonic acids and derivativesOrganic oxidesOrganopnictogen compoundsPhenylalanine and derivativesPrimary alcoholsProline and derivativesPropargyl-type 1,3-dipolar organic compoundsPyrrolidine-2-onesPyrrolidinecarboxamidesSecondary carboxylic acid amidesSemicarbazidesSerine and derivativesSubstituted pyrrolesTertiary carboxylic acid amidesTryptamines and derivativesTyrosine and derivatives 1-hydroxy-2-unsubstituted benzenoid2-pyrrolidone3-alkylindoleAlcoholAlpha-amino acid amideAlpha-amino acid or derivativesAlpha-oligopeptideAmphetamine or derivativesAromatic heteropolycyclic compoundAzacycleAzoleBenzenoidCarbonic acid derivativeCarbonyl groupCarboxamide groupCarboximidamideCarboxylic acid hydrazideDialkyl etherEtherFatty acylFatty amideGuanidineHeteroaromatic compoundHistidine or derivativesHydrazinecarboxamideHydrocarbon derivativeImidazoleIndoleIndole or derivativesLactamLeucine or derivativesMonocyclic benzene moietyN-acyl-alpha amino acid or derivativesN-acyl-amineN-acylpyrrolidineN-substituted-alpha-amino acidOrganic 1,3-dipolar compoundOrganic nitrogen compoundOrganic oxideOrganic oxygen compoundOrganoheterocyclic compoundOrganonitrogen compoundOrganooxygen compoundOrganopnictogen compoundPhenolPhenylalanine or derivativesPrimary alcoholProline or derivativesPropargyl-type 1,3-dipolar organic compoundPyrrolePyrrolidinePyrrolidine carboxylic acid or derivativesPyrrolidine-2-carboxamidePyrrolidoneSecondary carboxylic acid amideSemicarbazideSerine or derivativesSubstituted pyrroleTertiary carboxylic acid amideTriptanTyrosine or derivatives 711855272202477500964 United StatesUnited StatesUnited States 2002-04-132002-04-092001-02-26 2022-04-132022-04-092021-02-26 falsefalsefalse Astrazeneca uk ltd false GoserelinGoserelinGoserelinGoserelinGoserelinGoserelin ZoladexZoladexZoladexZoladexZoladex LAZoladex AstraZeneca Inc. http://www.astrazeneca.ca ZoladexZoladexZoladexZoladexZoladexZoladex LA falsefalsefalsefalsefalsefalse Astra Zeneca LpAstra Zeneca LpTer Sera Therapeutics LlcA S Medication SolutionsTersera Therapeutics LlcTersera Therapeutics Llc falsefalsefalsefalsefalsefalse SubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneous ImplantImplantImplantImplantImplantImplant FDA NDCFDA NDCFDA NDCFDA NDCDPDDPD 3.6 mg/110.8 mg/110.8 mg/13.6 mg/13.6 mg10.8 mg 0310-09500310-095170720-95150090-2027 NDA019726NDA020578NDA020578NDA019726 truetruetruetruetruetrue 0204932502225905 USUSUSUSCanadaCanada 2003-05-052003-05-052018-01-262003-05-051994-12-311996-08-28 2017-06-20 syringesyringe 451.191380.65 USDUSD Zoladex 3.6 mg implant syringeZoladex 10.8 mg implant syringe gmhMHx@@D@bpDj]@RKUV`rXnVjuzkPG@ptaXeQYln@bTlwHhdmLhhlhhdhjhhheDd]ihlhhdhdTeEIhfhhXmDhdh\hcBE@iT^@jWKMv|aVjfjZijfjZBZBJZ`hFbjjfjjZjjfZii`iABRExTqLeZ`yXUiP@ CC(C)C[C@H](NC(=O)[C@@H](COC(C)(C)C)NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)[C@H](CO)NC(=O)[C@H](CC1=CNC2=CC=CC=C12)NC(=O)[C@H](CC1=CN=CN1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NNC(N)=O InChI=1S/C59H84N18O14/c1-31(2)22-40(49(82)68-39(12-8-20-64-57(60)61)56(89)77-21-9-13-46(77)55(88)75-76-58(62)90)69-54(87)45(29-91-59(3,4)5)74-50(83)41(23-32-14-16-35(79)17-15-32)70-53(86)44(28-78)73-51(84)42(24-33-26-65-37-11-7-6-10-36(33)37)71-52(85)43(25-34-27-63-30-66-34)72-48(81)38-18-19-47(80)67-38/h6-7,10-11,14-17,26-27,30-31,38-46,65,78-79H,8-9,12-13,18-25,28-29H2,1-5H3,(H,63,66)(H,67,80)(H,68,82)(H,69,87)(H,70,86)(H,71,85)(H,72,81)(H,73,84)(H,74,83)(H,75,88)(H4,60,61,64)(H3,62,76,90)/t38-,39-,40-,41-,42-,43-,44-,45+,46-/m0/s1 BLCLNMBMMGCOAS-URPVMXJPSA-N C59H84N18O14 9.818594492171766 9.267832115311407 10.816089522841512 495.8899999999997 325.83880000000016 DB00015 133652-38-7 Reteplase Human t-PA (residues 1-3 and 176-527)Reteplase, recombinantReteplase,recombinant biotech DQA630RIE9 liquid Human tissue plasminogen activator, purified, glycosylated, 355 residues purified from CHO cells. Retavase is considered a "third-generation" thrombolytic agent, genetically engineered to retain and delete certain portions of human tPA. Retavase is a deletion mutein of human tPA formed by deleting various amino acids present in endogenous human tPA. Retavase contains 355 of the 527 amino acids of native human tPA (amino acids 1-3 and 176-527), and retains the activity-related kringle-2 and serine protease domains of human tPA. Three domains are deleted from retavase - kringle-1, finger, and epidermal growth factor (EGF). Humans and other mammals KitPowder, for solution Intravenous 10.4 unit For lysis of acute pulmonary emboli, intracoronary emboli and management of myocardial infarction Reteplase binds to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain. The protease domain then cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. activator PlasminogenFibrinogen alpha chainUrokinase plasminogen activator surface receptorPlasminogen activator inhibitor 1 BE0000211BE0000538BE0000717BE0000240 HumanHumanHumanHuman Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70.Longstaff C, Williams S, Thelwell C: Fibrin binding and the regulation of plasminogen activators during thrombolytic therapy. Cardiovasc Hematol Agents Med Chem. 2008 Jul;6(3):212-23.Melandri G, Vagnarelli F, Calabrese D, Semprini F, Nanni S, Branzi A: Review of tenecteplase (TNKase) in the treatment of acute myocardial infarction. Vasc Health Risk Manag. 2009;5(1):249-56. Epub 2009 Apr 8.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.Longstaff C, Williams S, Thelwell C: Fibrin binding and the regulation of plasminogen activators during thrombolytic therapy. Cardiovasc Hematol Agents Med Chem. 2008 Jul;6(3):212-23.Melandri G, Vagnarelli F, Calabrese D, Semprini F, Nanni S, Branzi A: Review of tenecteplase (TNKase) in the treatment of acute myocardial infarction. Vasc Health Risk Manag. 2009;5(1):249-56. Epub 2009 Apr 8.Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70. 17963464186732351943665611752352186732351943665617963464171392841701642317963464 P00747P02671Q03405P05121 PlasminogenFibrinogen alpha chainUrokinase plasminogen activator surface receptorPlasminogen activator inhibitor 1 6q264q2819q137q21.3-q22 HumanHumanHumanHuman extracellular exosomeextrinsic component of external side of plasma membraneextracellular regionplasma membraneplatelet alpha granule lumenextracellular spaceblood microparticlecell surfaceapolipoprotein bindingserine-type endopeptidase activityreceptor bindingserine-type peptidase activityprotein domain specific bindingnegative regulation of fibrinolysisblood coagulationextracellular matrix disassemblyproteolysisextracellular matrix organizationpositive regulation of fibrinolysisnegative regulation of cell-substrate adhesiontissue remodelingcellular protein metabolic processnegative regulation of cell-cell adhesion mediated by cadherinnegative regulation of cell proliferationplatelet degranulationfibrinolysisplatelet activationblood microparticlerough endoplasmic reticulumextracellular exosomecell cortexexternal side of plasma membraneextracellular regionplasma membraneextracellular spacecell surfaceextracellular vesicleplatelet alpha granuleplatelet alpha granule lumenfibrinogen complexstructural molecule activityplatelet degranulationsignal transductionresponse to cycloheximideprotein complex assemblycellular protein complex assemblypositive regulation of peptide hormone secretionacute-phase responseprotein polymerizationpositive regulation of substrate adhesion-dependent cell spreadinginnate immune responsefibrinolysisblood coagulationadaptive immune responseliver regenerationresponse to calcium ionpositive regulation of protein secretionresponse to genisteinextracellular matrix organizationplatelet aggregationcellular response to organic cyclic compoundresponse to estradiolinduction of bacterial agglutinationpositive regulation of vasoconstrictioncell-matrix adhesionplasminogen activationcellular protein metabolic processblood coagulation, common pathwaypositive regulation of ERK1 and ERK2 cascadecellular response to interleukin-6negative regulation of extrinsic apoptotic signaling pathway via death domain receptorscellular response to granulocyte colony-stimulating factornegative regulation of endothelial cell apoptotic processpositive regulation of exocytosisnegative regulation of blood coagulation, common pathwaypositive regulation of heterotypic cell-cell adhesionplatelet activationresponse to morphineblood coagulation, fibrin clot formationintegral component of plasma membraneendoplasmic reticulum lumenanchored component of membraneplasma membraneextrinsic component of membraneendoplasmic reticulum membraneinvadopodium membranefocal adhesionintegral component of membraneextracellular exosomereceptor activityreceptor bindingprotein domain specific bindingurokinase plasminogen activator receptor activityenzyme bindingnegative regulation of intrinsic apoptotic signaling pathwayurokinase plasminogen activator signaling pathwaypositive regulation of protein phosphorylationpositive regulation of DNA bindingsignal transductionpositive regulation of epidermal growth factor receptor signaling pathwayblood coagulationpositive regulation of release of cytochrome c from mitochondriacellular protein metabolic processnegative regulation of apoptotic processpost-translational protein modificationfibrinolysisregulation of proteolysischemotaxismovement of cell or subcellular componentattachment of GPI anchor to proteinnegative regulation of cysteine-type endopeptidase activity involved in apoptotic signaling pathwayC-terminal protein lipidationextracellular matrixextracellular regionplatelet alpha granule lumenplasma membraneextracellular spaceextracellular exosomeprotease bindingreceptor bindingserine-type endopeptidase inhibitor activityangiogenesisnegative regulation of smooth muscle cell migrationextracellular matrix organizationtransforming growth factor beta receptor signaling pathwaycellular response to lipopolysaccharideblood coagulationnegative regulation of smooth muscle cell-matrix adhesionnegative regulation of extrinsic apoptotic signaling pathway via death domain receptorsnegative regulation of endopeptidase activitynegative regulation of vascular wound healingpositive regulation of transcription from RNA polymerase II promoternegative regulation of wound healingchronological cell agingpositive regulation of angiogenesisplatelet degranulationdefense response to Gram-negative bacteriumpositive regulation of interleukin-8 productionfibrinolysisnegative regulation of blood coagulationpositive regulation of leukotriene production involved in inflammatory responsenegative regulation of fibrinolysisnegative regulation of cell adhesion mediated by integrinpositive regulation of monocyte chemotaxisplatelet activationpositive regulation of blood coagulationnegative regulation of cell migrationpositive regulation of receptor-mediated endocytosisgene expressionpositive regulation of inflammatory responsenegative regulation of endothelial cell apoptotic processtranscription initiation from RNA polymerase II promoterregulation of receptor activitycircadian rhythmnegative regulation of plasminogen activationtranscription, DNA-templated Serine-type peptidase activityStructural molecule activityUrokinase plasminogen activator receptor activitySerine-type endopeptidase inhibitor activity Plasmin dissolves the fibrin of blood clots and acts as a proteolytic factor in a variety of other processes including embryonic development, tissue remodeling, tumor invasion, and inflammation. In ovulation, weakens the walls of the Graafian follicle. It activates the urokinase-type plasminogen activator, collagenases and several complement zymogens, such as C1 and C5. Cleavage of fibronectin and laminin leads to cell detachment and apoptosis. Also cleaves fibrin, thrombospondin and von Willebrand factor. Its role in tissue remodeling and tumor invasion may be modulated by CSPG4. Binds to cells.Angiostatin is an angiogenesis inhibitor that blocks neovascularization and growth of experimental primary and metastatic tumors in vivo.Cleaved by the protease thrombin to yield monomers which, together with fibrinogen beta (FGB) and fibrinogen gamma (FGG), polymerize to form an insoluble fibrin matrix. Fibrin has a major function in hemostasis as one of the primary components of blood clots. In addition, functions during the early stages of wound repair to stabilize the lesion and guide cell migration during re-epithelialization. Was originally thought to be essential for platelet aggregation, based on in vitro studies using anticoagulated blood. However, subsequent studies have shown that it is not absolutely required for thrombus formation in vivo. Enhances expression of SELP in activated platelets via an ITGB3-dependent pathway. Maternal fibrinogen is essential for successful pregnancy. Fibrin deposition is also associated with infection, where it protects against IFNG-mediated hemorrhage. May also facilitate the immune response via both innate and T-cell mediated pathways.Acts as a receptor for urokinase plasminogen activator. Plays a role in localizing and promoting plasmin formation. Mediates the proteolysis-independent signal transduction activation effects of U-PA. It is subject to negative-feedback regulation by U-PA which cleaves it into an inactive form.Serine protease inhibitor. This inhibitor acts as 'bait' for tissue plasminogen activator, urokinase, protein C and matriptase-3/TMPRSS7. Its rapid interaction with PLAT may function as a major control point in the regulation of fibrinolysis. Reteplase cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that cause myocardial infarction. The therapeutic efficacy of Reteplase can be decreased when used in combination with Aprotinin.The risk or severity of adverse effects can be increased when Limaprost is combined with Reteplase.Reteplase may increase the anticoagulant activities of Dabigatran etexilate.Reteplase may increase the anticoagulant activities of Lepirudin.Reteplase may increase the anticoagulant activities of Bivalirudin.Reteplase may increase the anticoagulant activities of Abciximab.Reteplase may increase the anticoagulant activities of Becaplermin.Reteplase may increase the anticoagulant activities of Dicoumarol.Reteplase may increase the anticoagulant activities of Argatroban.Reteplase may increase the anticoagulant activities of Ardeparin.Reteplase may increase the anticoagulant activities of Phenindione.Reteplase may increase the anticoagulant activities of Fondaparinux sodium.Reteplase may increase the anticoagulant activities of Warfarin.Reteplase may increase the anticoagulant activities of Pentosan Polysulfate.Reteplase may increase the anticoagulant activities of Phenprocoumon.Reteplase may increase the anticoagulant activities of Edetic Acid.Reteplase may increase the anticoagulant activities of Heparin.Reteplase may increase the anticoagulant activities of Enoxaparin.Reteplase may increase the anticoagulant activities of Acenocoumarol.Reteplase may increase the anticoagulant activities of Citric Acid.Reteplase may increase the anticoagulant activities of Ximelagatran.Reteplase may increase the anticoagulant activities of Ancrod.Reteplase may increase the anticoagulant activities of Pentaerythritol Tetranitrate.Reteplase may increase the anticoagulant activities of Rivaroxaban.Reteplase may increase the anticoagulant activities of Sulodexide.Reteplase may increase the anticoagulant activities of Idraparinux.Reteplase may increase the anticoagulant activities of Apixaban.Reteplase may increase the anticoagulant activities of Otamixaban.Reteplase may increase the anticoagulant activities of Danaparoid.Reteplase may increase the anticoagulant activities of Dalteparin.Reteplase may increase the anticoagulant activities of Ferulic acid.Reteplase may increase the anticoagulant activities of Ethyl biscoumacetate.Reteplase may increase the anticoagulant activities of Nadroparin.Reteplase may increase the anticoagulant activities of Edoxaban.Reteplase may increase the anticoagulant activities of Dextran.Reteplase may increase the anticoagulant activities of Reviparin.Reteplase may increase the anticoagulant activities of Certoparin.Reteplase may increase the anticoagulant activities of Dextran 70.Reteplase may increase the anticoagulant activities of Desirudin.Reteplase may increase the anticoagulant activities of Dextran 40.Reteplase may increase the anticoagulant activities of Dextran 75.Reteplase may increase the anticoagulant activities of Protocatechualdehyde.Reteplase may increase the anticoagulant activities of Protein C.Reteplase may increase the anticoagulant activities of Antithrombin III human.Reteplase may increase the anticoagulant activities of Fondaparinux.Reteplase may increase the anticoagulant activities of Letaxaban.Reteplase may increase the anticoagulant activities of Darexaban.Reteplase may increase the anticoagulant activities of Nafamostat.Reteplase may increase the anticoagulant activities of Gabexate.Reteplase may increase the anticoagulant activities of Troxerutin.Reteplase may increase the anticoagulant activities of Fluindione.Reteplase may increase the anticoagulant activities of Protein S human.Reteplase may increase the anticoagulant activities of Melagatran.The risk or severity of adverse effects can be increased when Salicylic acid is combined with Reteplase.The risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Reteplase.The risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Reteplase.The risk or severity of adverse effects can be increased when Mesalazine is combined with Reteplase.The risk or severity of adverse effects can be increased when Diflunisal is combined with Reteplase.The risk or severity of adverse effects can be increased when Balsalazide is combined with Reteplase.The risk or severity of adverse effects can be increased when Olsalazine is combined with Reteplase.The risk or severity of adverse effects can be increased when Dersalazine is combined with Reteplase.The risk or severity of adverse effects can be increased when Nitroaspirin is combined with Reteplase.The risk or severity of adverse effects can be increased when Aloxiprin is combined with Reteplase.The risk or severity of adverse effects can be increased when Guacetisal is combined with Reteplase.The risk or severity of adverse effects can be increased when Carbaspirin calcium is combined with Reteplase.The risk or severity of adverse effects can be increased when Hemoglobin crosfumaril is combined with Reteplase.The risk or severity of adverse effects can be increased when Methyl salicylate is combined with Reteplase.The risk or severity of adverse effects can be increased when Trolamine salicylate is combined with Reteplase.Eptifibatide may increase the anticoagulant activities of Reteplase.Ticlopidine may increase the anticoagulant activities of Reteplase.Tirofiban may increase the anticoagulant activities of Reteplase.Dipyridamole may increase the anticoagulant activities of Reteplase.Clopidogrel may increase the anticoagulant activities of Reteplase.Prasugrel may increase the anticoagulant activities of Reteplase.Vorapaxar may increase the anticoagulant activities of Reteplase.Milrinone may increase the anticoagulant activities of Reteplase.Anagrelide may increase the anticoagulant activities of Reteplase.Epinastine may increase the anticoagulant activities of Reteplase.Alprostadil may increase the anticoagulant activities of Reteplase.Pentoxifylline may increase the anticoagulant activities of Reteplase.Azelastine may increase the anticoagulant activities of Reteplase.Iloprost may increase the anticoagulant activities of Reteplase.Cilostazol may increase the anticoagulant activities of Reteplase.Ridogrel may increase the anticoagulant activities of Reteplase.Sevoflurane may increase the anticoagulant activities of Reteplase.Epoprostenol may increase the anticoagulant activities of Reteplase.Resveratrol may increase the anticoagulant activities of Reteplase.Nimesulide may increase the anticoagulant activities of Reteplase.Tesmilifene may increase the anticoagulant activities of Reteplase.Defibrotide may increase the anticoagulant activities of Reteplase.SRT501 may increase the anticoagulant activities of Reteplase.Beraprost may increase the anticoagulant activities of Reteplase.Ibudilast may increase the anticoagulant activities of Reteplase.Andrographolide may increase the anticoagulant activities of Reteplase.eplivanserine may increase the anticoagulant activities of Reteplase.Cangrelor may increase the anticoagulant activities of Reteplase.Tranilast may increase the anticoagulant activities of Reteplase.Triflusal may increase the anticoagulant activities of Reteplase.Icosapent ethyl may increase the anticoagulant activities of Reteplase.Ifenprodil may increase the anticoagulant activities of Reteplase.Trapidil may increase the anticoagulant activities of Reteplase.Naftopidil may increase the anticoagulant activities of Reteplase.Sarpogrelate may increase the anticoagulant activities of Reteplase.Eplivanserin may increase the anticoagulant activities of Reteplase.Ifetroban may increase the anticoagulant activities of Reteplase.Ketanserin may increase the anticoagulant activities of Reteplase.Indobufen may increase the anticoagulant activities of Reteplase.Butylphthalide may increase the anticoagulant activities of Reteplase.Hydroxytyrosol may increase the anticoagulant activities of Reteplase.Ramatroban may increase the anticoagulant activities of Reteplase.Picotamide may increase the anticoagulant activities of Reteplase.Cloricromen may increase the anticoagulant activities of Reteplase.Linsidomine may increase the anticoagulant activities of Reteplase.Buflomedil may increase the anticoagulant activities of Reteplase.Relcovaptan may increase the anticoagulant activities of Reteplase.Ticagrelor may increase the anticoagulant activities of Reteplase.The risk or severity of adverse effects can be increased when Reteplase is combined with Treprostinil. DB06692DB09211DB06695DB00001DB00006DB00054DB00102DB00266DB00278DB00407DB00498DB00569DB00682DB00686DB00946DB00974DB01109DB01225DB01418DB04272DB04898DB05099DB06154DB06228DB06271DB06406DB06605DB06635DB06754DB06779DB07767DB08794DB08813DB09075DB09255DB09259DB09261DB11076DB11095DB11122DB11241DB11268DB11312DB11598DB11728DB11984DB12289DB12598DB12831DB13124DB13136DB13149DB13616DB00936DB00945DB00233DB00244DB00861DB01014DB01250DB06251DB12445DB13509DB13538DB13612DB13864DB09543DB11079DB00063DB00208DB00775DB00975DB00758DB06209DB09030DB00235DB00261DB00751DB00770DB00806DB00972DB01088DB01166DB01207DB01236DB01240DB02709DB04743DB04905DB04932DB05073DB05229DB05266DB05767DB06392DB06441DB07615DB08814DB08887DB08954DB09283DB12092DB12163DB12177DB12321DB12465DB12545DB12749DB12771DB13036DB13327DB13367DB13400DB13510DB13929DB08816DB00374 AprotininLimaprostDabigatran etexilateLepirudinBivalirudinAbciximabBecaplerminDicoumarolArgatrobanArdeparinPhenindioneFondaparinux sodiumWarfarinPentosan PolysulfatePhenprocoumonEdetic AcidHeparinEnoxaparinAcenocoumarolCitric AcidXimelagatranAncrodPentaerythritol TetranitrateRivaroxabanSulodexideIdraparinuxApixabanOtamixabanDanaparoidDalteparinFerulic acidEthyl biscoumacetateNadroparinEdoxabanDextranReviparinCertoparinDextran 70DesirudinDextran 40Dextran 75ProtocatechualdehydeProtein CAntithrombin III humanFondaparinuxLetaxabanDarexabanNafamostatGabexateTroxerutinFluindioneProtein S humanMelagatranSalicylic acidAcetylsalicylic acidAminosalicylic AcidMesalazineDiflunisalBalsalazideOlsalazineDersalazineNitroaspirinAloxiprinGuacetisalCarbaspirin calciumHemoglobin crosfumarilMethyl salicylateTrolamine salicylateEptifibatideTiclopidineTirofibanDipyridamoleClopidogrelPrasugrelVorapaxarMilrinoneAnagrelideEpinastineAlprostadilPentoxifyllineAzelastineIloprostCilostazolRidogrelSevofluraneEpoprostenolResveratrolNimesulideTesmilifeneDefibrotideSRT501BeraprostIbudilastAndrographolideeplivanserineCangrelorTranilastTriflusalIcosapent ethylIfenprodilTrapidilNaftopidilSarpogrelateEplivanserinIfetrobanKetanserinIndobufenButylphthalideHydroxytyrosolRamatrobanPicotamideCloricromenLinsidomineBuflomedilRelcovaptanTicagrelorTreprostinil Melting PointHydrophobicityIsoelectric PointMolecular WeightMolecular Formula 60 °C-0.4356.8639589.6C1736H2671N499O522S22 Novokhatny, V.V. et al., J. Biol. Chem. 266:12994-123002 (1991) B01AD07 EnzymesANTITHROMBOTIC AGENTSANTITHROMBOTIC AGENTSBLOOD AND BLOOD FORMING ORGANS B01ADB01AB01B Amino Acids, Peptides, and ProteinsBiological FactorsBlood and Blood Forming OrgansBlood Coagulation FactorsBlood ProteinsCardiovascular AgentsChemical Actions and UsesEndopeptidasesEnzymesEnzymes and CoenzymesFibrin Modulating AgentsFibrinolytic AgentsHematologic AgentsHydrolasesMolecular Mechanisms of Pharmacological ActionPeptide HydrolasesPharmacologic ActionsPlasminogen ActivatorsProteinsSerine EndopeptidasesSerine ProteasesTherapeutic Uses D000602D001685D001779D001798D002317D020164D010450D004798D045762D050299D005343D006401D006867D045504D010447D020228D010960D011506D012697D057057D045506 1153446506092L00153PA164743728P00750DAP001195ReteplaseCHEMBL2107885 Drugs Product Database (DPD)PubChem SubstanceGenBankPharmGKBUniProtKBTherapeutic Targets DatabaseWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic2/reteplase.htmhttp://www.drugs.com/cdi/reteplase.html approvedinvestigational Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides 2107476 Canada 2007-12-18 2012-04-15 false drug_action DB00015DB01022DB01373 ReteplasePhylloquinoneCalcium P00747P00748P02452P03952P03951P00740P00451P00734P12259P00742P02671P02675P02679P00488P05160P00750P08709P13726Q9BQB6P38435 Reteplase Action Pathway SMP00285 ReteplaseReteplaseReteplaseReteplaseReteplase RetavaseRetavaseRetavaseRetavaseRetavase EKR Therapeutics Inc.Hospira Inc.PDL BioPharma Inc. http://www.ekrtx.comhttp://www.hospira.comhttp://www.pdl.com RetavaseRetavaseRetavaseRetavaseRetavase falsefalsefalsefalsefalse Chiesi Pharmaceuticals Inc.Chiesi Pharmaceuticals Inc.Ekr TherapeuticsEkr TherapeuticsEkr Therapeutics falsefalsefalsefalsefalse Intravenous KitKitKitKitPowder, for solution FDA NDCFDA NDCFDA NDCFDA NDCDPD 10.4 unit 10122-14110122-14324477-04024477-041 BLA103786BLA103786BLA103786BLA103786 truetruetruetruetrue 02233013 USUSUSUSCanada 1996-10-301996-10-301996-10-301996-10-301999-02-19 2017-03-142017-03-142013-08-29 vial 2605.93 USD Retavase vial half-kit DB00016DB08923 11096-26-7 Erythropoietin E.P.O.Epoetin alfaEpoetin alfa rDNAEpoetin alfa, recombinantEpoetin betaEpoetin beta rDNAEpoetin epsilonEpoetin gammaEpoetin gamma rDNAEpoetin kappaEpoetin omegaEpoetin thetaEpoetin zetaEpoetina dsetaEpoétine zêtaEpoetinum zetaErythropoiesis stimulating factorErythropoietin (human, recombinant)Erythropoietin (recombinant human)ESFSH-polypeptide-72 biotech 64FS3BFH5W liquid Erythropoietin is a 165-amino acid erythropoiesis-stimulating glycoprotein manufactured by recombinant DNA technology. It has a molecular weight of approximately 30,400 daltons and is produced by mammalian cells into which the human erythropoietin gene has been introduced. The product contains the identical amino acid sequence of isolated natural erythropoietin. Humans and other mammals Injection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionSolutionSolutionSolutionSolutionSolutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solution Intravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; Subcutaneous 1000 IU/0.5ml10000 IU/1.0ml2000 IU/1.0ml20000 IU/0.5ml3000 IU/0.3ml30000 IU/0.75ml4000 IU/0.4ml40000 IU/1ml40000 IU/1.0ml5000 IU/0.5ml6000 IU/0.6ml7000 IU/0.7ml8000 IU/0.8ml9000 IU/0.9ml10000 IU/1ml10000 [iU]/mL2000 [iU]/mL20000 [iU]/mL3000 [iU]/mL4000 [iU]/mL2000 IU/0.5ml20000 IU/1.0ml3000 IU/0.5ml30000 IU/1.0ml4000 IU/0.5ml20000 unit30000 unit10000 unit1000 unit2000 unit3000 unit40000 unit4000 unit5000 unit6000 unit8000 unit10000 [iU]/mL2000 [iU]/mL20000 [iU]/mL3000 [iU]/mL4000 [iU]/mL40000 [iU]/mL1000 IU/0.3ml2000 IU/0.6ml3000 IU/0.9ml For use in the treatment of symptomatic anaemia associated with chronic renal failure (CRF) in adult and paediatric patients. Also for use in the treatment of anaemia and reduction of transfusion requirements in adult patients receiving chemotherapy for solid tumours, malignant lymphoma or multiple myeloma, and at risk of transfusion as assessed by the patient's general status (e.g. cardiovascular status, pre-existing anaemia at the start of chemotherapy). Also for used to increase the yield of autologous blood from patients in a predonation program. When administered subcutaneously, Epoetin Zeta is equivalent to Epoetin Alfa in terms of clinical effectiveness. Binding of erythropoietin to the erythropoietin receptor leads to receptor dimerization, which facilitates activation of JAK-STAT signaling pathways within the cytosol. Activated STAT (signal transducers and activators of transcription) proteins are then translocated to the nucleus where they serve as transcription factors which regulate the activation of specific genes involved in cell division or differentiation. agonist Erythropoietin receptor BE0000654 Human LaMontagne KR, Butler J, Marshall DJ, Tullai J, Gechtman Z, Hall C, Meshaw A, Farrell FX: Recombinant epoetins do not stimulate tumor growth in erythropoietin receptor-positive breast carcinoma models. Mol Cancer Ther. 2006 Feb;5(2):347-55.Kokhaei P, Abdalla AO, Hansson L, Mikaelsson E, Kubbies M, Haselbeck A, Jernberg-Wiklund H, Mellstedt H, Osterborg A: Expression of erythropoietin receptor and in vitro functional effects of epoetins in B-cell malignancies. Clin Cancer Res. 2007 Jun 15;13(12):3536-44.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. 165051081757521611752352 P19235 Erythropoietin receptor 19p13.3-p13.2 Human extracellular regioncytosolintegral component of plasma membraneidentical protein bindingerythropoietin receptor activitysignal transductionerythropoietin-mediated signaling pathwaypositive regulation of cytosolic calcium ion concentrationheart developmentbrain developmentnegative regulation of neuron apoptotic processdecidualization Identical protein binding Receptor for erythropoietin. Mediates erythropoietin-induced erythroblast proliferation and differentiation. Upon EPO stimulation, EPOR dimerizes triggering the JAK2/STAT5 signaling cascade. In some cell types, can also activate STAT1 and STAT3. May also activate the LYN tyrosine kinase.Isoform EPOR-T acts as a dominant-negative receptor of EPOR-mediated signaling. Toxicokinetic results from rats in a 13 week toxicity study after a single subcutaneous dose:* 7.37 hours (+/- 0.70) with 500 IU/kg [test 1]* 8.63 hours (+/- 2.78) with 2500 IU/kg [test 2]* 8.76 hours (+/- 1.46) with 2500 IU/kg [reference dose] * 20.2 +/- 15.9 mL/h/kg [150 Units/kg SC TIW, Week 1 when anemic cancer patients were receiving chemotherapy]* 23.6 +/- 9.5 mL/h/kg [150 Units/kg SC TIW, Week 3 when anemic cancer patients were not receiving chemotherapy]* 9.2 +/- 4.7 mL/h/kg [40,000 Units/kg SC TIW, Week 1 when anemic cancer patients were receiving chemotherapy]* 13.9 +/- 7.6 mL/h/kg [40,000 Units/kg SC TIW, Week 3 when anemic cancer patients were not receiving chemotherapy] Used in the treatment of anemia. Involved in the regulation of erythrocyte differentiation and the maintenance of a physiological level of circulating erythrocyte mass. Nandrolone phenpropionate may increase the stimulatory activities of Erythropoietin.Nandrolone decanoate may increase the stimulatory activities of Erythropoietin.Erythropoietin may increase the thrombogenic activities of Lenalidomide.Erythropoietin may increase the thrombogenic activities of Thalidomide. DB00984DB08804DB00480DB01041 Nandrolone phenpropionateNandrolone decanoateLenalidomideThalidomide Melting PointIsoelectric PointMolecular WeightMolecular Formula 53 °C8.7518396.1C815H1317N233O241S5 Arakawa, T. et al., Biosci. Biotechnol. Biochem. 65:1321-1327 (2001) B03XA01 Other antianemic preparationsOTHER ANTIANEMIC PREPARATIONSANTIANEMIC PREPARATIONSBLOOD AND BLOOD FORMING ORGANS B03XAB03XB03B Amino Acids, Peptides, and ProteinsAntianemic PreparationsBiological FactorsBlood and Blood Forming OrgansCarbohydratesChemical Actions and UsesColony-Stimulating FactorsCytokinesErythropoiesis-Stimulating AgentsErythropoietinGlycoconjugatesGlycoproteinsHematinicsHematologic AgentsHematopoietic Cell Growth FactorsIntercellular Signaling Peptides and ProteinsPeptidesPharmacologic ActionsProteinsTherapeutic Uses D000602D001685D002241D020164D003115D016207D004921D006001D006023D006397D006401D016298D036341D010455D020228D011506D045506 29946508122X02158PA10072P01588DAP000202Epoetin_alfaCHEMBL1201565 Drugs Product Database (DPD)PubChem SubstanceGenBankPharmGKBUniProtKBTherapeutic Targets DatabaseWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic/epoetin.htmhttp://www.drugs.com/cdi/epoetin-alfa.html //s3-us-west-2.amazonaws.com/drugbank/fda_labels/DB00016.pdf?1265922800 Wizemann V, Rutkowski B, Baldamus C, Scigalla P, Koytchev R: Comparison of the therapeutic effects of epoetin zeta to epoetin alfa in the maintenance phase of renal anaemia treatment. Curr Med Res Opin. 2008 Mar;24(3):625-37. doi: 10.1185/030079908X273264.Krivoshiev S, Wizemann V, Czekalski S, Schiller A, Pljesa S, Wolf-Pflugmann M, Siebert-Weigel M, Koytchev R, Bronn A: Therapeutic equivalence of epoetin zeta and alfa, administered subcutaneously, for maintenance treatment of renal anemia. Adv Ther. 2010 Feb;27(2):105-17. doi: 10.1007/s12325-010-0012-y. Epub 2010 Mar 30.Brinks V, Hawe A, Basmeleh AH, Joachin-Rodriguez L, Haselberg R, Somsen GW, Jiskoot W, Schellekens H: Quality of original and biosimilar epoetin products. Pharm Res. 2011 Feb;28(2):386-93. doi: 10.1007/s11095-010-0288-2. Epub 2010 Oct 1. 182086422036931220886265 approved SandozNobel Ilac Pazarlama ve Sanayii Ltd. STI., TurkeyLupin pharmaIntas pharmaChugaiHemofarm ADNanogen Pharmaceutical biotechnology, Vietnam)Hospira, Inc.Cell Pharm GmbH BinocritEpobelEpoceptEpofitEpoginEqralysNanokineRetacritSilapo Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides 1339047 Canada 1997-05-27 2014-05-27 false 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Eprex Sterile Solution 1000iu/0.5mlEprex Sterile Solution 2000iu/0.5mlEprex Sterile Solution 3000iu/0.3mlEprex Sterile Solution 4000iu/0.4mlEprex Sterile Solution 10000iu/1.0mlEprex Sterile Solution 40000iu/mlEprex Sterile SolutionEprex Sterile Solution 5000iu/0.5mlEprex Sterile Solution 6000 Iu/0.6 MlEprex Sterile Solution 8000 Iu/0.8 MlEprex Sterile SolutionEprex Sterile Solution 10000iu/mlEprex Sterile Solution 4000iu/mlEprex Sterile Solution 2000iu/mlEprex Sterile Solution 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Amgen Inc.Centocor Ortho Biotech Inc.DSM Corp.Janssen-Ortho Inc.JHP Pharmaceuticals LLCOrtho-McNeil-Janssen Pharmaceuticals Inc.Physicians Total Care Inc. http://www.amgen.comhttp://www.centocororthobiotech.comhttp://www.dsm.comhttp://www.janssen-ortho.comhttp://www.jhppharma.comhttp://www.ortho-mcneil.comhttp://www.physicianstotalcare.com 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Medice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. KgMedice Arzneimittel Pütter Gmb H & Co. 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IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncRatiopharm IncJanssen PharmaceuticalsJanssen PharmaceuticalsJanssen PharmaceuticalsJanssen PharmaceuticalsJanssen PharmaceuticalsJanssen PharmaceuticalsJanssen PharmaceuticalsJanssen PharmaceuticalsJanssen PharmaceuticalsJanssen PharmaceuticalsJanssen PharmaceuticalsJanssen PharmaceuticalsJanssen PharmaceuticalsJanssen PharmaceuticalsJanssen PharmaceuticalsJanssen, LpJanssen, LpJanssen, LpJanssen, LpJanssen, LpJanssen, LpJanssen, LpPhysicians Total Care, Inc.Physicians Total Care, Inc.Physicians Total Care, Inc.Stada Arzneimittel AgStada 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Intravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; Subcutaneous Injection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionSolutionSolutionSolutionSolutionSolutionSolutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solution EMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMADPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMA 20000 IU/0.5ml30000 IU/0.75ml40000 IU/1ml1000 IU/0.5ml1000 IU/0.5ml2000 IU/1.0ml2000 IU/1.0ml3000 IU/0.3ml3000 IU/0.3ml4000 IU/0.4ml4000 IU/0.4ml5000 IU/0.5ml5000 IU/0.5ml6000 IU/0.6ml6000 IU/0.6ml8000 IU/0.8ml8000 IU/0.8ml10000 IU/1.0ml10000 IU/1.0ml7000 IU/0.7ml7000 IU/0.7ml9000 IU/0.9ml9000 IU/0.9ml20000 IU/0.5ml20000 IU/0.5ml30000 IU/0.75ml30000 IU/0.75ml40000 IU/1.0ml40000 IU/1.0ml1000 IU/0.5ml1000 IU/0.5ml2000 IU/1.0ml2000 IU/1.0ml3000 IU/0.3ml3000 IU/0.3ml4000 IU/0.4ml4000 IU/0.4ml5000 IU/0.5ml5000 IU/0.5ml6000 IU/0.6ml6000 IU/0.6ml7000 IU/0.7ml7000 IU/0.7ml8000 IU/0.8ml8000 IU/0.8ml9000 IU/0.9ml9000 IU/0.9ml10000 IU/1.0ml10000 IU/1.0ml20000 IU/0.5ml20000 IU/0.5ml30000 IU/0.75ml30000 IU/0.75ml40000 IU/1.0ml40000 IU/1.0ml1000 IU/0.5ml1000 IU/0.5ml2000 IU/1.0ml2000 IU/1.0ml3000 IU/0.3ml3000 IU/0.3ml4000 IU/0.4ml4000 IU/0.4ml5000 IU/0.5ml5000 IU/0.5ml6000 IU/0.6ml6000 IU/0.6ml8000 IU/0.8ml8000 IU/0.8ml10000 IU/1.0ml10000 IU/1.0ml7000 IU/0.7ml7000 IU/0.7ml9000 IU/0.9ml9000 IU/0.9ml20000 IU/0.5ml20000 IU/0.5ml30000 IU/0.75ml30000 IU/0.75ml40000 IU/1ml40000 IU/1ml1000 IU/0.5ml1000 IU/0.5ml2000 IU/1.0ml2000 IU/1.0ml3000 IU/0.3ml3000 IU/0.3ml4000 IU/0.4ml4000 IU/0.4ml5000 IU/0.5ml5000 IU/0.5ml6000 IU/0.6ml6000 IU/0.6ml7000 IU/0.7ml7000 IU/0.7ml8000 IU/0.8ml8000 IU/0.8ml9000 IU/0.9ml9000 IU/0.9ml10000 IU/1ml10000 IU/1ml20000 IU/0.5ml20000 IU/0.5ml30000 IU/0.75ml30000 IU/0.75ml40000 IU/1ml40000 IU/1ml20000 IU/0.5ml30000 IU/0.75ml40000 IU/1ml5000 IU/0.5ml10000 IU/1.0ml10000 IU/1.0ml10000 IU/1.0ml10000 IU/1.0ml10000 IU/1.0ml10000 IU/1.0ml20000 IU/1.0ml20000 IU/1.0ml20000 IU/1.0ml20000 IU/1.0ml20000 IU/1.0ml20000 IU/1.0ml30000 IU/1.0ml30000 IU/1.0ml30000 IU/1.0ml30000 IU/1.0ml30000 IU/1.0ml30000 IU/1.0ml1000 IU/0.5ml2000 IU/0.5ml3000 IU/0.5ml4000 IU/0.5ml5000 IU/0.5ml10000 IU/1.0ml10000 IU/1.0ml10000 IU/1.0ml20000 IU/1.0ml20000 IU/1.0ml20000 IU/1.0ml30000 IU/1.0ml30000 IU/1.0ml30000 IU/1.0ml1000 IU/0.5ml1000 IU/0.5ml2000 IU/0.5ml2000 IU/0.5ml3000 IU/0.5ml3000 IU/0.5ml4000 IU/0.5ml4000 IU/0.5ml5000 IU/0.5ml1000 IU/0.5ml1000 IU/0.5ml2000 IU/1.0ml2000 IU/1.0ml3000 IU/0.3ml3000 IU/0.3ml4000 IU/0.4ml4000 IU/0.4ml5000 IU/0.5ml5000 IU/0.5ml6000 IU/0.6ml6000 IU/0.6ml8000 IU/0.8ml8000 IU/0.8ml7000 IU/0.7ml7000 IU/0.7ml9000 IU/0.9ml9000 IU/0.9ml30000 IU/0.75ml30000 IU/0.75ml1000 IU/0.5ml1000 IU/0.5ml2000 IU/1.0ml2000 IU/1.0ml3000 IU/0.3ml3000 IU/0.3ml4000 IU/0.4ml4000 IU/0.4ml5000 IU/0.5ml5000 IU/0.5ml6000 IU/0.6ml6000 IU/0.6ml7000 IU/0.7ml7000 IU/0.7ml8000 IU/0.8ml8000 IU/0.8ml9000 IU/0.9ml9000 IU/0.9ml30000 IU/0.75ml30000 IU/0.75ml30000 IU/0.75ml40000 IU/1ml2000 [iU]/mL10000 [iU]/mL4000 [iU]/mL3000 [iU]/mL10000 [iU]/mL20000 [iU]/mL1000 IU/0.5ml1000 IU/0.5ml2000 IU/0.5ml2000 IU/0.5ml3000 IU/0.5ml3000 IU/0.5ml4000 IU/0.5ml4000 IU/0.5ml5000 IU/0.5ml5000 IU/0.5ml10000 IU/1.0ml10000 IU/1.0ml10000 IU/1.0ml10000 IU/1.0ml10000 IU/1.0ml10000 IU/1.0ml20000 IU/1.0ml20000 IU/1.0ml20000 IU/1.0ml20000 IU/1.0ml20000 IU/1.0ml20000 IU/1.0ml30000 IU/1.0ml30000 IU/1.0ml30000 IU/1.0ml30000 IU/1.0ml30000 IU/1.0ml30000 IU/1.0ml1000 IU/0.5ml2000 IU/0.5ml3000 IU/0.5ml4000 IU/0.5ml5000 IU/0.5ml10000 IU/1.0ml10000 IU/1.0ml10000 IU/1.0ml20000 IU/1.0ml20000 IU/1.0ml20000 IU/1.0ml30000 IU/1.0ml30000 IU/1.0ml30000 IU/1.0ml30000 unit20000 unit10000 unit10000 unit1000 unit20000 unit2000 unit2000 unit3000 unit40000 unit4000 unit4000 unit5000 unit6000 unit8000 unit2000 [iU]/mL3000 [iU]/mL4000 [iU]/mL10000 [iU]/mL10000 [iU]/mL20000 [iU]/mL40000 [iU]/mL10000 [iU]/mL20000 [iU]/mL40000 [iU]/mL1000 IU/0.3ml1000 IU/0.3ml2000 IU/0.6ml2000 IU/0.6ml3000 IU/0.9ml3000 IU/0.9ml4000 IU/0.4ml4000 IU/0.4ml5000 IU/0.5ml5000 IU/0.5ml6000 IU/0.6ml6000 IU/0.6ml8000 IU/0.8ml8000 IU/0.8ml10000 IU/1.0ml10000 IU/1.0ml20000 IU/0.5ml30000 IU/0.75ml40000 IU/1.0ml20000 IU/0.5ml30000 IU/0.75ml40000 IU/1.0ml 55513-12655513-14455513-14855513-26755513-28355513-47859676-30259676-30359676-30459676-31059676-31259676-32059676-34054868-252354868-567354868-5802 BLA103234BLA103234BLA103234BLA103234BLA103234BLA103234BLA103234BLA103234BLA103234BLA103234BLA103234BLA103234BLA103234BLA103234BLA103234BLA103234 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022886800224323902231587021265910223158302206072022315840212657502231585022407220223158602126583022434000224340102243403 EUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUUSUSUSUSUSUSEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUCanadaCanadaCanadaCanadaCanadaCanadaCanadaCanadaCanadaCanadaCanadaCanadaCanadaCanadaCanadaUSUSUSUSUSUSUSUSUSUSEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEUEU 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2014-10-092010-04-292014-09-252014-10-09 vialvialvialvialvialvialmlmlvialvialmlmlmlvialvialboxboxbox 34.1437.0947.5355.6361.3474.17151.8303.6315.74358.02378.14388.97640.37710.87767.031578.723157.446852.3 USDUSDUSDUSDUSDUSDUSDUSDUSDUSDUSDUSDUSDUSDUSDUSDUSDUSD Epogen 2000 unit/ml vialProcrit 2000 unit/ml vialEpogen 3000 unit/ml vialProcrit 3000 unit/ml vialEpogen 4000 unit/ml vialProcrit 4000 unit/ml vialEpogen 10000 unit/ml vialEpogen 20000 unit/ml vialEpogen 10000 unit/ml Solution 2ml VialProcrit 10000 unit/ml Solution 2ml VialProcrit 20000 unit/ml SolutionProcrit 20000 unit/ml vialEpogen 40000 unit/ml vialProcrit 10000 unit/ml vialProcrit 40000 unit/ml vialEpogen 10000 unit/ml Solution 1 Box Contains Ten 1ml VialsEpogen 20000 unit/ml Solution 1 Box Contains Ten 1ml VialsEpogen 40000 unit/ml Solution 1 Box Contains Ten 1ml Vials DB00017 47931-85-1 Salmon Calcitonin Calcitonin (Salmon Synthetic)Calcitonin SalmonCalcitonin salmon recombinantCalcitonin-salmonCalcitonin, salmonRecombinant salmon calcitoninSalmon calcitonin biotech 7SFC6U2VI5 Marcos C. Poblet, Berta P. Obiols, Gemma J. Farres, "Procedure for preparing salmon calcitonin." U.S. Patent US5527881, issued October, 1991. liquid Synthetic peptide, 32 residues long formulated as a nasal spray. Humans and other mammals LiquidSolutionSolutionSpray, meteredLiquidInjection, solutionSpray, meteredInjection, solutionInjection, solutionSpray, meteredLiquidSprayLiquid Intramuscular; SubcutaneousNasalIntramuscular; SubcutaneousNasalIntramuscular; SubcutaneousIntramuscular; Intravenous; SubcutaneousNasalIntramuscularIntramuscular; SubcutaneousNasalIntramuscular; Intravenous; SubcutaneousNasalNasal 200 unit200 unit200 unit200 [iU]/.09mL100 unit100 IU2200 [iU]/mL200 [iU]/mL200 [iU]/mL200 [iU]/1200 unit200 unit200 unit Used in the treatment of symptomatic Paget's disease for patients unresponsive to alternate treatments or intolerant to such treatments. In addition, it is used in emergency situations when serum calcium levels must be decreased quickly until the underlying condition is identified. It can also be added to existing therapeutic regimens for hypercalcemia such as intravenous fluids and furosemide, oral phosphate or corticosteroids, or other agents. Calcitonin can be used in patients with azotemia and cases where intravenous fluids would be contraindicated due to limited cardiac reserves. Also for the treatment of post-menopausal osteoporosis in women more than 5 years post-menopause. Calcitonin binds to the calcitonin receptor (found primarily in osteoclasts) which then enhances the production of vitamin D producing enzymes (25-hydroxyvitamine D-24-hydroxylase), leading to greater calcium retention and enhanced bone density. Binding of calcitonin to its receptor also activates adenylyl cyclase and the phosphatidyl-inositol-calcium pathway. agonist Calcitonin receptor BE0000431 Human Bouizar Z, Fouchereau-Peron M, Taboulet J, Moukhtar MS, Milhaud G: Purification and characterization of calcitonin receptors in rat kidney membranes by covalent cross-linking techniques. Eur J Biochem. 1986 Feb 17;155(1):141-7.Stroop SD, Moore EE: Intracellular calcium increases mediated by a recombinant human calcitonin receptor. J Bone Miner Res. 1995 Apr;10(4):524-32.Sarkar A, Dickerson IM: Cloning, characterization, and expression of a calcitonin receptor from guinea pig brain. J Neurochem. 1997 Aug;69(2):455-64.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. 30049877610922923170311752352 P30988 Calcitonin receptor 7q21.3 Human plasma membranecytosolintegral component of plasma membranereceptor activitycalcitonin receptor activityprotein transporter activitycalcitonin bindingprotein localization to plasma membraneprotein transportresponse to glucocorticoidpositive regulation of cAMP biosynthetic processadenylate cyclase-activating G-protein coupled receptor signaling pathwaypositive regulation of adenylate cyclase activitypositive regulation of cytosolic calcium ion concentrationreceptor internalizationG-protein coupled receptor signaling pathwaycell surface receptor signaling pathway Receptor activity This is a receptor for calcitonin. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase. The calcitonin receptor is thought to couple to the heterotrimeric guanosine triphosphate-binding protein that is sensitive to cholera toxin. 30 to 40% Salmon calcitonin was shown to inhibit lactation in animals and is not recommend in nursing mothers. While research in animals have shown a decrease in fetal weight, no studies have yet shown similar results in humans. It is recommended however to proceed carefully when administering salmon calcitonin to pregnant women and consider if the benefits outweigh the risks. Because of its protein nature, salmon calcitonin may provoke an allergy reaction (bronchospams and swelling of the tongue/throat) that can turn into a full-blown anaphylactic response. The manufacturer also reports an increase in the risk of malignancies from oral route (0.7%) to intranasal route (2.4%) compared to placebo. The same may apply to IV, IM and SC routes since the systemic exposure is higher in those cases.Nausea is noticeable in some patients but tends to decrease with continued administration. Rhinitis, headaches and back pain have also been reported among others. Half-life elimination (terminal): I.M. 58 minutes; SubQ 59 to 64 minutes; Nasal: ~18 to 23 minutes Salmon calcitonin is rapidly absorbed and eliminated. Bioavailability following subcutaneous and intramuscular injection in humans is high and similar for the two routes of administration (71% and 66%, respectively). Via the nasal route, the bioavailability varies between 3 to 5% relative to IM. Salmon calcitonin is primarily and almost exclusively degraded in the kidneys, forming pharmacologically inactive fragments of the molecule. It is also metabolized in the blood and the peripheral tissue. 0.15 to 0.3 L/kg Urine. Studies with injectable calcitonin show increases in the excretion of filtered phosphate, calcium, and sodium by decreasing their tubular reabsorption in the kidney. Calcitonin inhibits bone resorption by osteoclasts (bone remodeling cells) and promotes bone formation by osteoblasts. This leads to a net increase in bone mass and a reduction in plasma calcium levels. It also promotes the renal excretion of ions such as calcium, phosphate, sodium, magnesium, and potassium by decreasing tubular reabsorption. In consequence, there is an increase in the jejunal secretion of water, sodium, potassium, and chloride. Salmon Calcitonin may increase the hypocalcemic activities of Zoledronic acid.The serum concentration of Lithium can be decreased when it is combined with Salmon Calcitonin. DB00399DB01356 Zoledronic acidLithium HydrophobicityIsoelectric PointMolecular WeightMolecular Formula -0.5378.863431.853C145H240N44O48S2 H05BA01 Calcitonin preparationsANTI-PARATHYROID AGENTSCALCIUM HOMEOSTASISSYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS H05BAH05BH05H Amino Acids, Peptides, and ProteinsAnti-Parathyroid AgentsBone Density Conservation AgentsBone Density, drug effectsCalcitonin PreparationsCalcium HomeostasisChemical Actions and UsesHormonesHormones, Hormone Substitutes, and Hormone AntagonistsNerve Tissue ProteinsNeuropeptidesParathyroidPeptide HormonesPeptidesPharmacologic ActionsPhysiological Effects of DrugsProteinsSystemic Hormonal Preparations, Excl. Sex Hormones and Insulins D000602D050071D002116D020164D006728D006730D009419D009479D036361D010455D020228D045505D011506 1318646506061C06865D00249Y00765PA448715P01263DAP001302Calcitonin Drugs Product Database (DPD)PubChem SubstanceKEGG CompoundKEGG DrugGenBankPharmGKBUniProtKBTherapeutic Targets DatabaseWikipedia RxList http://www.rxlist.com/cgi/generic2/calcit.htm approvedinvestigational Calcimar Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides 57335696440392RE43580RE40812 United StatesUnited StatesUnited StatesUnited States 1995-03-312001-02-022001-02-022001-02-02 2015-03-312021-02-022021-02-022021-02-02 falsefalsefalsefalse Sanofi aventis us llcAstrazeneca lpNovartis pharmaceuticals corpApotex incPar pharmaceutical incUpsher smith laboratories inc falsefalsefalsefalsefalsefalse Salmon CalcitoninSalmon CalcitoninSalmon CalcitoninSalmon CalcitoninSalmon CalcitoninSalmon CalcitoninSalmon CalcitoninSalmon CalcitoninSalmon CalcitoninSalmon CalcitoninSalmon CalcitoninSalmon CalcitoninSalmon CalcitoninSalmon CalcitoninSalmon CalcitoninSalmon CalcitoninSalmon CalcitoninSalmon CalcitoninSalmon CalcitoninSalmon CalcitoninSalmon Calcitonin MiacalcinMiacalcinForticalCalcitonin SalmonCalcitonin SalmonCalcimar Solution Inj 200unit/mlCaltine Inj 100 Unit/ml (1ml Amp)Caltine Inj 100unit/ml (0.5ml Amp)Miacalcin Nasal Spray 200 IuApo-calcitonin InjectableApo-calcitonin Nasal SpraySandoz-calcitonin NSPro-calcitonin - 200Calcitonin (salmon) Injection, BPMiacalcin Injection 200iu/mlForcaltoninMiacalcinCalcitonin SalmonMiacalcinForticalCalcitonin Salmon Apotex Inc.Novartis AGPar PharmaceuticalsSandozUpsher Smith Laboratories http://www.apotex.comhttp://www.novartis.comhttp://www.parpharm.comhttp://www.sandoz.cahttp://www.upsher-smith.com Apo-calcitonin InjectableApo-calcitonin Nasal SprayCalcimar Solution Inj 200unit/mlCalcitonin (salmon) Injection, BPCalcitonin SalmonCalcitonin SalmonCalcitonin SalmonCalcitonin SalmonCaltine Inj 100 Unit/ml (1ml Amp)Caltine Inj 100unit/ml (0.5ml Amp)ForcaltoninForticalForticalMiacalcinMiacalcinMiacalcinMiacalcinMiacalcin Injection 200iu/mlMiacalcin Nasal Spray 200 IuPro-calcitonin - 200Sandoz-calcitonin NS truetruefalsefalsetruetruetruetruefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsetruetrue Apotex CorporationApotex CorporationSanofi AventisMylan PharmaceuticalsPhysicians Total Care, Inc.SandozPar PharmaceuticalApotex CorporationFerring PharmaceuticalsFerring PharmaceuticalsUnigene Laboratories Inc.Upsher Smith LaboratoriesPhysicians Total Care, Inc.Sebela Pharmaceuticals Inc.NovartisNovartisMylan InstitutionalNovartisNovartisPro Doc LimiteeSandoz Canada Incorporated falsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalse Intramuscular; SubcutaneousNasalIntramuscular; SubcutaneousIntramuscular; SubcutaneousNasalNasalNasalNasalIntramuscular; SubcutaneousIntramuscular; SubcutaneousIntramuscular; Intravenous; SubcutaneousNasalNasalIntramuscularIntramuscular; SubcutaneousNasalIntramuscular; SubcutaneousIntramuscular; Intravenous; SubcutaneousNasalNasalNasal LiquidSolutionSolutionSolutionSpray, meteredSpray, meteredSpray, meteredSpray, meteredLiquidLiquidInjection, solutionSpray, meteredSpray, meteredInjection, solutionInjection, solutionSpray, meteredInjection, solutionLiquidSpraySolutionLiquid DPDDPDDPDDPDFDA NDCFDA NDCFDA NDCFDA NDCDPDDPDEMAFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCDPDDPDDPDDPD 200 unit200 unit200 unit200 unit200 [iU]/.09mL200 [iU]/1200 [iU]/.09mL200 [iU]/1100 unit100 unit100 IU2200 [iU]/mL2200 [iU]/mL200 [iU]/mL200 [iU]/mL200 [iU]/1200 [iU]/mL200 unit200 unit200 unit200 unit 54868-63230781-632049884-16160505-08230245-000854868-549954766-1490078-01490078-031167457-675 ANDA076979NDA020313ANDA076979ANDA076396NDA021406NDA021406NDA017808NDA017808NDA020313NDA017808 truetruetruetruetruetruetruetruetruetruefalsetruetruetruetruetruetruetruetruetruetrue 02246058022475850192669102383233020071340194037602144301022407750231104602261766 CanadaCanadaCanadaCanadaUSUSUSUSCanadaCanadaEUUSUSUSUSUSUSCanadaCanadaCanadaCanada 2003-05-012003-09-121983-12-312011-12-091995-08-012009-06-082008-12-091993-12-311993-12-311999-01-112005-08-122005-12-301986-07-031986-07-031995-08-012016-09-161999-09-082008-07-042004-12-01 2013-08-022013-10-012014-07-252002-01-302008-11-172017-02-282017-04-142013-10-012011-07-272013-10-01 mlmlmlmlmlmlvialbottlebottle 8.8129.9430.7334.339.5144.6863.59123.28139.39 USDUSDUSDUSDUSDUSDUSDUSDUSD Caltine 100 (100 Iu/Ml) 100 iu/mlCalcimar 200 iu/mlMiacalcin 200 unit/ml vialFortical 200 unit nasal sprayCalcitonin-salmon 200 unit spMiacalcin 200 unit nasal sprayMiacalcin For Inj, 2 unit = 1 Box 2ml VialCalcitonin (Salmon) 200 unit/act Solution 3.7ml BottleMiacalcin 200 unit/act Solution 3.7ml Bottle DB00018 Interferon alfa-n3 biotech 47BPR3V3MP liquid Purified, natural (n is for natural) human interferon alpha proteins (consists of 3 forms or polymorphisms including 2a, 2b and 2c). 166 residues, some are glycosylated (MW range from 16 kD to 27 kD). Humans and other mammals Injection Subcutaneous 5000000 [arb'U]/mL For the intralesional treatment of refractory or recurring external condylomata acuminata. Interferon alpha binds to type I interferon receptors (IFNAR1 and IFNAR2c) which, upon dimerization, activate two Jak (Janus kinase) tyrosine kinases (Jak1 and Tyk2). These transphosphorylate themselves and phosphorylate the receptors. The phosphorylated INFAR receptors then bind to Stat1 and Stat2 (signal transducers and activators of transcription) which dimerize and activate multiple (~100) immunomodulatory and antiviral proteins. Interferon alpha binds less stably to type I interferon receptors than interferon beta. agonistagonist Interferon alpha/beta receptor 1Interferon alpha/beta receptor 2 BE0000661BE0000385 HumanHuman Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Dhalluin C, Ross A, Huber W, Gerber P, Brugger D, Gsell B, Senn H: Structural, kinetic, and thermodynamic analysis of the binding of the 40 kDa PEG-interferon-alpha2a and its individual positional isomers to the extracellular domain of the receptor IFNAR2. Bioconjug Chem. 2005 May-Jun;16(3):518-27.Ishii K, Shinohara M, Sawa M, Kogame M, Higami K, Sano M, Morita T, Sumino Y: Interferon alpha receptor 2 expression by peripheral blood monocytes in patients with a high viral load of hepatitis C virus genotype 1 showing substitution of amino Acid 70 in the core region. Intervirology. 2010;53(2):105-10. doi: 10.1159/000264200. Epub 2009 Dec 3.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Dhalluin C, Ross A, Huber W, Gerber P, Brugger D, Gsell B, Senn H: Structural, kinetic, and thermodynamic analysis of the binding of the 40 kDa PEG-interferon-alpha2a and its individual positional isomers to the extracellular domain of the receptor IFNAR2. Bioconjug Chem. 2005 May-Jun;16(3):518-27.Ishii K, Shinohara M, Sawa M, Kogame M, Higami K, Sano M, Morita T, Sumino Y: Interferon alpha receptor 2 expression by peripheral blood monocytes in patients with a high viral load of hepatitis C virus genotype 1 showing substitution of amino Acid 70 in the core region. Intervirology. 2010;53(2):105-10. doi: 10.1159/000264200. Epub 2009 Dec 3.Yano H, Ogasawara S, Momosaki S, Akiba J, Kojiro S, Fukahori S, Ishizaki H, Kuratomi K, Basaki Y, Oie S, Kuwano M, Kojiro M: Growth inhibitory effects of pegylated IFN alpha-2b on human liver cancer cells in vitro and in vivo. Liver Int. 2006 Oct;26(8):964-75.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. 1713928417016423158987171995581511752352171392841701642315898717199558151695383711752352 P17181P48551 Interferon alpha/beta receptor 1Interferon alpha/beta receptor 2 HumanHuman intracellularplasma membraneintegral component of plasma membranetype I interferon receptor activityregulation of type I interferon-mediated signaling pathwayresponse to virustype I interferon signaling pathwaypositive regulation of transcription, DNA-templateddefense response to viruscell surface receptor signaling pathwaypositive regulation of interleukin-1 beta secretioncytokine-mediated signaling pathwaypositive regulation of interferon-beta productionregulation of peptidyl-tyrosine phosphorylationtype I interferon biosynthetic processpositive regulation of interferon-gamma productionT cell activationJAK-STAT cascadeintracellularextracellular regionplasma membraneextracellular spaceintegral component of plasma membraneprotein kinase bindingtype I interferon bindingtype I interferon receptor activityJAK-STAT cascaderegulation of transcription from RNA polymerase II promoterregulation of type I interferon-mediated signaling pathwayresponse to interferon-alphacell proliferationresponse to virustype I interferon signaling pathwaycell surface receptor signaling pathwaycytokine-mediated signaling pathway Type i interferon receptor activityType i interferon receptor activity Associates with IFNAR2 to form the type I interferon receptor. Receptor for interferons alpha and beta. Binding to type I IFNs triggers tyrosine phosphorylation of a number of proteins including JAKs, TYK2, STAT proteins and IFNR alpha- and beta-subunits themselves. Can also transduce IFNB signals without the help of IFNAR2, and not activating the Jak-STAT pathway.Associates with IFNAR1 to form the type I interferon receptor. Receptor for interferons alpha and beta. Involved in IFN-mediated STAT1, STAT2 and STAT3 activation. Isoform 1 and isoform 2 are directly involved in signal transduction due to their association with the TYR kinase, JAK1. Isoform 3 is a potent inhibitor of type I IFN receptor activity. Interferon alfa-n3 upregulates the expression of MHC I proteins, allowing for increased presentation of peptides derived from viral antigens. This enhances the activation of CD8+ T cells that are the precursors for cytotoxic T lymphocytes (CTLs) and makes the macrophage a better target for CTL-mediated killing. Interferon alpha also induce the synthesis of several key antiviral mediators, including 2'-5' oligoadenylate synthetase (2'-5' A synthetase), beta-2 microglobulin, neopterin and protein kinase R. The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Aldesleukin.The metabolism of Ambroxol acefyllinate can be decreased when combined with Interferon alfa-n3.The metabolism of Theophylline can be decreased when combined with Interferon alfa-n3.The metabolism of Dyphylline can be decreased when combined with Interferon alfa-n3.The metabolism of Aminophylline can be decreased when combined with Interferon alfa-n3.The serum concentration of Methadone can be increased when it is combined with Interferon alfa-n3.The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Ribavirin.The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Zidovudine.The risk or severity of myelosuppression can be increased when Metamizole is combined with Interferon alfa-n3.The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Clozapine. DB00041DB13141DB00277DB00651DB01223DB00333DB00811DB00495DB04817DB00363 AldesleukinAmbroxol acefyllinateTheophyllineDyphyllineAminophyllineMethadoneRibavirinZidovudineMetamizoleClozapine Melting PointIsoelectric Point 61 °C5.99 Beldarrain, A. et al., Biochemistry 38:7865-7873 (1999) Alfa InterferonsAmino Acids, Peptides, and ProteinsBiological FactorsCytokinesIntercellular Signaling Peptides and ProteinsInterferon alphaInterferon Type IInterferonsMyelosuppressive AgentsPeptidesProteins D000602D001685D016207D036341D016898D007370D007372D010455D011506 46508902PA164746228DAP001281Interferon_alfa-n3CHEMBL2109047 PubChem SubstancePharmGKBTherapeutic Targets DatabaseWikipediaChEMBL Drugs.com http://www.drugs.com/cdi/interferon-alfa-n3-solution.html Sturgill MG, Rashidbaigi A, Liao MJ, Zhao XX, Hua J, Trout R, Knill JR, Grasing KW: Extravascular administration of interferon alfa-N3 increases serum exposure and 2-5(A) synthetase activity. J Clin Pharmacol. 2000 Jun;40(6):606-15. 10868311 approvedinvestigational Interferon Sciences Inc. AlferonAlferon LDOAlferon N Injection Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides Interferon alfa-n3 Alferon Hemispherx Biopharma Inc. http://www.hemispherx.net Alferon false Hemispherx Biopharma false Subcutaneous Injection FDA NDC 5000000 [arb'U]/mL 54746-001 BLA103158 true US 1989-10-10 ml 412.87 USD Alferon n 5 million unit vial DB00019 208265-92-3 Pegfilgrastim Granulocyte colony-stimulating factor pegfilgrastimPeg-filgrastim biotech 3A58010674 liquid PEGylated (at N terminus) form of human G-CSF (Granulocyte colony stimulating factor), 175 residues, produced from E. coli via bacterial fermentation. Humans and other mammals InjectionKitSolutionInjection, solution SubcutaneousSubcutaneousSubcutaneousSubcutaneous 6 mg/.6mL10 mg6 mg Increases leukocyte production, for treatment in non-myeloid cancer, neutropenia and bone marrow transplant. Pegfilgrastim binds to the G-CSF receptor. As a G-CSF analog, it controls proliferation of committed progenitor cells and influences their maturation into mature neutrophils. Pegfilgrastim also stimulates the release of neutrophils from bone marrow storage pools and reduces their maturation time. Pegfilgrastim acts to increase the phagocytic activity of mature neutrophils. In patients receiving cytotoxic chemotherapy, pegfilgrastim can accelerate neutrophil recovery, leading to a reduction in duration of the neutropenic phase. agonist Granulocyte colony-stimulating factor receptorNeutrophil elastase BE0000793BE0000394 HumanHuman Erkeland SJ, Aarts LH, Irandoust M, Roovers O, Klomp A, Valkhof M, Gits J, Eyckerman S, Tavernier J, Touw IP: Novel role of WD40 and SOCS box protein-2 in steady-state distribution of granulocyte colony-stimulating factor receptor and G-CSF-controlled proliferation and differentiation signaling. Oncogene. 2007 Mar 29;26(14):1985-94. Epub 2006 Sep 25.Elsasser A, Franzen M, Kohlmann A, Weisser M, Schnittger S, Schoch C, Reddy VA, Burel S, Zhang DE, Ueffing M, Tenen DG, Hiddemann W, Behre G: The fusion protein AML1-ETO in acute myeloid leukemia with translocation t(8;21) induces c-jun protein expression via the proximal AP-1 site of the c-jun promoter in an indirect, JNK-dependent manner. Oncogene. 2003 Aug 28;22(36):5646-57.Ward AC: The role of the granulocyte colony-stimulating factor receptor (G-CSF-R) in disease. Front Biosci. 2007 Jan 1;12:608-18.Zhuang D, Qiu Y, Haque SJ, Dong F: Tyrosine 729 of the G-CSF receptor controls the duration of receptor signaling: involvement of SOCS3 and SOCS1. J Leukoc Biol. 2005 Oct;78(4):1008-15. Epub 2005 Jul 20.Cao YR, Shao ZH, Liu H, Shi J, Bai J, Tu MF, Wang HQ, Xing LM, Cui ZZ, Sun J, Jia HR, Yang TY: [The response of bone marrow hematopoietic cells to G-CSF in paroxysmal nocturnal hemoglobinuria patients]. Zhonghua Xue Ye Xue Za Zhi. 2005 Apr;26(4):235-8.Kotto-Kome AC, Fox SE, Lu W, Yang BB, Christensen RD, Calhoun DA: Evidence that the granulocyte colony-stimulating factor (G-CSF) receptor plays a role in the pharmacokinetics of G-CSF and PegG-CSF using a G-CSF-R KO model. Pharmacol Res. 2004 Jul;50(1):55-8.Carter CR, Whitmore KM, Thorpe R: The significance of carbohydrates on G-CSF: differential sensitivity of G-CSFs to human neutrophil elastase degradation. J Leukoc Biol. 2004 Mar;75(3):515-22. Epub 2003 Dec 4.Jian MY, Koizumi T, Tsushima K, Fujimoto K, Kubo K: Effects of granulocyte colony-stimulating factor (G-CSF) and neutrophil elastase inhibitor (ONO-5046) on acid-induced lung injury in rats. Inflammation. 2004 Dec;28(6):327-36.Pelus LM, Bian H, King AG, Fukuda S: Neutrophil-derived MMP-9 mediates synergistic mobilization of hematopoietic stem and progenitor cells by the combination of G-CSF and the chemokines GRObeta/CXCL2 and GRObetaT/CXCL2delta4. Blood. 2004 Jan 1;103(1):110-9. Epub 2003 Sep 4.Druhan LJ, Ai J, Massullo P, Kindwall-Keller T, Ranalli MA, Avalos BR: Novel mechanism of G-CSF refractoriness in patients with severe congenital neutropenia. Blood. 2005 Jan 15;105(2):584-91. Epub 2004 Sep 7.Schepers H, Wierenga AT, van Gosliga D, Eggen BJ, Vellenga E, Schuringa JJ: Reintroduction of C/EBPalpha in leukemic CD34+ stem/progenitor cells impairs self-renewal and partially restores myelopoiesis. Blood. 2007 Aug 15;110(4):1317-25. Epub 2007 May 2. 1700130612944913171273221603381615949269150820291465721016245075129580671535348617475913 Q99062P08246 Granulocyte colony-stimulating factor receptorNeutrophil elastase 1p35-p34.319p13.3 HumanHuman extracellular regionintegral component of plasma membranereceptor activitycytokine receptor activitysignal transductioncell adhesiondefense responseneutrophil chemotaxisamelogenesisregulation of myeloid cell differentiationcytoplasmtranscriptional repressor complexextracellular regionextracellular spacecell surfaceextracellular exosomesecretory granuleprotease bindingpeptidase activityheparin bindingendopeptidase activityserine-type endopeptidase activityRNA polymerase II transcription corepressor activitycytokine bindingpositive regulation of smooth muscle cell proliferationneutrophil mediated killing of funguscollagen catabolic processpositive regulation of immune responseextracellular matrix disassemblypositive regulation of interleukin-8 biosynthetic processextracellular matrix organizationphagocytosisprotein catabolic processleukocyte migrationproteolysisresponse to UVdefense response to bacteriumresponse to yeastnegative regulation of inflammatory responseacute inflammatory response to antigenic stimulusresponse to lipopolysaccharidenegative regulation of chemokine biosynthetic processnegative regulation of transcription from RNA polymerase II promoternegative regulation of chemotaxiscellular calcium ion homeostasisnegative regulation of growth of symbiont in hostpositive regulation of MAP kinase activitynegative regulation of interleukin-8 biosynthetic process Receptor activitySerine-type endopeptidase activity Receptor for granulocyte colony-stimulating factor (CSF3), essential for granulocytic maturation. Plays a crucial role in the proliferation, differientation and survival of cells along the neutrophilic lineage. In addition it may function in some adhesion or recognition events at the cell surface.Modifies the functions of natural killer cells, monocytes and granulocytes. Inhibits C5a-dependent neutrophil enzyme release and chemotaxis. 15-80 hrs Filgrastim is primarily eliminated by the kidney and neutrophils/neutrophil precursors; the latter presumably involves binding of the growth factor to the G-CSF receptor on the cell surface, internalization of the growth factor-receptor complexes via endocytosis, and subsequent degradation inside the cells. Pegylation of filgrastim renders renal clearance insignificant, which was demonstrated in bilaterally nephrectomized rats and confirmed in subjects with renal impairment. As a result, the neutrophil-mediated clearance is the predominant elimination pathway for pegfilgrastim. During chemotherapy-induced neutropenia, the clearance of pegfilgrastim is significantly reduced and the concentration of pegfilgrastim is sustained until onset of neutrophil recovery. Used in the treatment of chemotherapy-induced neutropenia by enhancing the production of neutrophils. Pegfilgrastim acts on hematopoietic cells by binding to specific cell surface receptors thereby stimulating proliferation, differentiation, commitment, and end cell functional activation. Pegfilgrastim has reduced renal clearance and prolonged persistence in vivo as compared to Filgrastim. The therapeutic efficacy of Pegfilgrastim can be decreased when used in combination with Pegloticase. DB09208 Pegloticase Melting PointHydrophobicityIsoelectric PointMolecular WeightMolecular Formula 60 °C0.2095.6518802.8C845H1343N223O243S9 Luo, P., Protein Science 11:1218-1226 (2002) L03AA13 Colony stimulating factorsIMMUNOSTIMULANTSIMMUNOSTIMULANTSANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L03AAL03AL03L Adjuvants, ImmunologicAmino Acids, Peptides, and ProteinsAntineoplastic and Immunomodulating AgentsBiological FactorsCarbohydratesColony-Stimulating FactorsCytokinesGlycoconjugatesGlycoproteinsHematinicsHematopoietic Cell Growth FactorsIntercellular Signaling Peptides and ProteinsLeukocyte Growth FactorPeptidesProteins D000276D000602D001685D002241D003115D016207D006001D006023D006397D016298D036341D010455D011506 1231346505853D06889X03438PA164781387P09919DAP000395PegfilgrastimCHEMBL1201568 Drugs Product Database (DPD)PubChem SubstanceKEGG DrugGenBankPharmGKBUniProtKBTherapeutic Targets DatabaseWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic3/neulasta.htmhttp://www.drugs.com/cdi/pegfilgrastim.html //s3-us-west-2.amazonaws.com/drugbank/fda_labels/DB00019.pdf?1265922804 Yang BB, Kido A: Pharmacokinetics and pharmacodynamics of pegfilgrastim. Clin Pharmacokinet. 2011 May;50(5):295-306. doi: 10.2165/11586040-000000000-00000. 21456630 approved Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides 13415371339071 CanadaCanada 2007-07-311997-07-29 2024-07-312014-07-29 falsefalse PegfilgrastimPegfilgrastimPegfilgrastimPegfilgrastimPegfilgrastimPegfilgrastim NeulastaNeupopegNeupopegNeupopegNeulastaNeulasta Amgen Inc.Physicians Total Care Inc. http://www.amgen.comhttp://www.physicianstotalcare.com NeulastaNeulastaNeulastaNeupopegNeupopegNeupopeg falsefalsefalsefalsefalsefalse AmgenAmgenAmgenDompé Biotec S.P.A.Dompé Biotec S.P.A.Dompé Biotec S.P.A. falsefalsefalsefalsefalsefalse SubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneous InjectionKitSolutionInjection, solutionInjection, solutionInjection, solution FDA NDCFDA NDCDPDEMAEMAEMA 6 mg/.6mL10 mg6 mg6 mg6 mg 55513-19055513-192 BLA125031BLA125031 truetruetruefalsefalsefalse 02249790 USUSCanadaEUEUEU 2002-04-012002-04-012004-03-122002-08-222002-08-222002-08-22 2008-12-222008-12-222008-12-22 syringesyringe 4026.054102.37 USDUSD Neulasta 6 mg/0.6ml Solution 0.6ml SyringeNeulasta 6 mg/0.6 ml syringe DB00020 123774-72-1 Sargramostim GM-CSF biotech 5TAA004E22 Kaname Sugimoto, "Process for the production of human colony-stimulating factor." U.S. Patent US4621050, issued May, 1983. liquid Sargramostim is a human recombinant granulocyte macrophage colony-stimulating factor (GM-CSF) expressed in yeast. It is a glycoprotein that is 127 residues. Substitution of Leu23 leads to a difference from native protein. Humans and other mammals Injection, powder, for solutionLiquid Intravenous; SubcutaneousIntravenous; Subcutaneous 250 ug/mL500 ug/mL For the treatment of cancer and bone marrow transplant Sargramostim binds to the Granulocyte-macrophage colony stimulating factor receptor (GM-CSF-R-alpha or CSF2R) which stimulates a JAK2 STAT1/STAT3 signal transduction pathway. This leads to the production of hemopoietic cells and neutrophils agonistagonistagonistagonist Granulocyte-macrophage colony-stimulating factor receptor subunit alphaInterleukin-3 receptor subunit alphaCytokine receptor common subunit betaSyndecan-2Bone marrow proteoglycan BE0000628BE0001036BE0002115BE0002116BE0002114 HumanHumanHumanHumanHuman Wang Y, Cai D, Brendel C, Barett C, Erben P, Manley PW, Hochhaus A, Neubauer A, Burchert A: Adaptive secretion of granulocyte-macrophage colony-stimulating factor (GM-CSF) mediates imatinib and nilotinib resistance in BCR/ABL+ progenitors via JAK-2/STAT-5 pathway activation. Blood. 2007 Mar 1;109(5):2147-55. Epub 2006 Nov 7.Chen J, Carcamo JM, Golde DW: The alpha subunit of the granulocyte-macrophage colony-stimulating factor receptor interacts with c-Kit and inhibits c-Kit signaling. J Biol Chem. 2006 Aug 4;281(31):22421-6. Epub 2006 Jun 7.Lencz T, Morgan TV, Athanasiou M, Dain B, Reed CR, Kane JM, Kucherlapati R, Malhotra AK: Converging evidence for a pseudoautosomal cytokine receptor gene locus in schizophrenia. Mol Psychiatry. 2007 Jun;12(6):572-80. Epub 2007 Mar 20.Xiao R, Zhang R, Wang YL, Zhu ZL, Chen T, Yang JH: [Expression of soluble GM-CSF-Ralpha in patients with acute myeloid leukemia]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2006 Apr;14(2):225-7.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.Eksioglu EA, Mahmood SS, Chang M, Reddy V: GM-CSF promotes differentiation of human dendritic cells and T lymphocytes toward a predominantly type 1 proinflammatory response. Exp Hematol. 2007 Aug;35(8):1163-71. Epub 2007 Jun 11.Sakhno LV, Leplina OIu, Tikhonova MA, Raspai ZhM, Gileva IP, Nikonov SD, Zhdanov OA, Ostanin AA, Chernykh ER: [Characteristics of A-interferon-generated dendritic cells in patients with pulmonary tuberculosis]. Probl Tuberk Bolezn Legk. 2007;(3):42-6.Ward KA, Stewart LA, Schwarer AP: CD34+-derived CD11c+ + + BDCA-1+ + CD123+ + DC: expansion of a phenotypically undescribed myeloid DC1 population for use in adoptive immunotherapy. Cytotherapy. 2006;8(2):130-40.Lencz T, Morgan TV, Athanasiou M, Dain B, Reed CR, Kane JM, Kucherlapati R, Malhotra AK: Converging evidence for a pseudoautosomal cytokine receptor gene locus in schizophrenia. Mol Psychiatry. 2007 Jun;12(6):572-80. Epub 2007 Mar 20.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Shen Y, Baker E, Callen DF, Sutherland GR, Willson TA, Rakar S, Gough NM: Localization of the human GM-CSF receptor beta chain gene (CSF2RB) to chromosome 22q12.2-->q13.1. Cytogenet Cell Genet. 1992;61(3):175-7.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Modrowski D, Basle M, Lomri A, Marie PJ: Syndecan-2 is involved in the mitogenic activity and signaling of granulocyte-macrophage colony-stimulating factor in osteoblasts. J Biol Chem. 2000 Mar 31;275(13):9178-85.Menon K, Wu Y, Haas J, Sahu SK, Yang B, Zaheer A: Diminished degradation of myelin basic protein by anti-sulfatide antibody and interferon-gamma in myelin from glia maturation factor-deficient mice. Neurosci Res. 2007 Jun;58(2):156-63. Epub 2007 Feb 22.Letuve S, Lajoie-Kadoch S, Audusseau S, Rothenberg ME, Fiset PO, Ludwig MS, Hamid Q: IL-17E upregulates the expression of proinflammatory cytokines in lung fibroblasts. J Allergy Clin Immunol. 2006 Mar;117(3):590-6. Epub 2006 Feb 8.Kang JH, Lee da H, Seo H, Park JS, Nam KH, Shin SY, Park CS, Chung IY: Regulation of functional phenotypes of cord blood derived eosinophils by gamma-secretase inhibitor. Am J Respir Cell Mol Biol. 2007 Nov;37(5):571-7. Epub 2007 Jun 28. 17090651167604631752271116638185117523521756235517500228166986861752271117139284170164231424804171392841701642310734053173837641652245817600316 P15509P26951P32927P34741P13727 Granulocyte-macrophage colony-stimulating factor receptor subunit alphaInterleukin-3 receptor subunit alphaCytokine receptor common subunit betaSyndecan-2Bone marrow proteoglycan Xp22.32 and Yp11.3Xp22.3 or Yp11.322q13.18q22-q2311q12 HumanHumanHumanHumanHuman intracellularextracellular regionplasma membraneintegral component of plasma membranereceptor activitygranulocyte colony-stimulating factor receptor activityactivation of MAPKK activityfibroblast growth factor receptor signaling pathwayinsulin receptor signaling pathwayMAPK cascadesmall GTPase mediated signal transductionneurotrophin TRK receptor signaling pathwayaxon guidanceRas protein signal transductionepidermal growth factor receptor signaling pathwayvascular endothelial growth factor receptor signaling pathwayinnate immune responsecellular response to granulocyte macrophage colony-stimulating factor stimulusFc-epsilon receptor signaling pathwaycellular protein metabolic processintracellularplasma membraneintegral component of membraneinterleukin-3 receptor activityMAPK cascadeneurotrophin TRK receptor signaling pathwaysmall GTPase mediated signal transductionRas protein signal transductionvascular endothelial growth factor receptor signaling pathwayaxon guidancecellular response to interleukin-3epidermal growth factor receptor signaling pathwayinterleukin-3-mediated signaling pathwayinnate immune responseFc-epsilon receptor signaling pathwayactivation of MAPKK activityfibroblast growth factor receptor signaling pathwayinsulin receptor signaling pathwayintracellularplasma membraneintegral component of plasma membranegranulocyte macrophage colony-stimulating factor receptor complexreceptor activitycytokine receptor activitycellular response to interleukin-3activation of MAPKK activityinterleukin-3-mediated signaling pathwayfibroblast growth factor receptor signaling pathwayinterleukin-5-mediated signaling pathwaysignal transductioninsulin receptor signaling pathwayMAPK cascadesmall GTPase mediated signal transductionneurotrophin TRK receptor signaling pathwayaxon guidanceRas protein signal transductionepidermal growth factor receptor signaling pathwayvascular endothelial growth factor receptor signaling pathwayinnate immune responserespiratory gaseous exchangeFc-epsilon receptor signaling pathwaycellular protein metabolic processplasma membranecell surfacelysosomal lumenintegral component of membraneGolgi lumenPDZ domain bindingglycosaminoglycan biosynthetic processsmall molecule metabolic processretinoid metabolic processcarbohydrate metabolic processephrin receptor signaling pathwayaxon guidanceglycosaminoglycan metabolic processcell migrationregulation of dendrite morphogenesisextracellular matrix organizationglycosaminoglycan catabolic processchondroitin sulfate metabolic processdendrite morphogenesisbioluminescencephototransduction, visible lightextracellular regionextracellular exosometransport vesiclecarbohydrate bindingheparin bindingimmune responsedefense response to bacteriumpositive regulation of interleukin-4 productionnegative regulation of interleukin-10 productiondefense response to nematoderegulation of cytokine biosynthetic process Receptor activityInterleukin-3 receptor activityReceptor activityPdz domain bindingHeparin binding Low affinity receptor for granulocyte-macrophage colony-stimulating factor. Transduces a signal that results in the proliferation, differentiation, and functional activation of hematopoietic cells.This is a receptor for interleukin-3.High affinity receptor for interleukin-3, interleukin-5 and granulocyte-macrophage colony-stimulating factor.Cell surface proteoglycan that bears heparan sulfate. Regulates dendritic arbor morphogenesis (By similarity).Cytotoxin and helminthotoxin. Also induces non-cytolytic histamine release from human basophils. Involved in antiparasitic defense mechanisms and immune hypersensitivity reactions. The proform acts as a proteinase inhibitor, reducing the activity of PAPPA. * 420 mL/min/m2 [Normal people with liquid LEUKINE (IV)]* 431 mL/min/m2 [Normal people with lyophilized LEUKINE (IV)]* 549 mL/min/m2 [Normal people with liquid LEUKINE (SC)]* 529 mL/min/m2 [Normal people with lyophilized LEUKINE (SC)] Sargramostim is used in the treatment of bone marrow transplant recipients or those exposed to chemotherapy an recovering from acut myelogenous leukemia, Leukine or GM-CSF is a hematopoietic growth factor which stimulates the survival, clonal expansion (proliferation) and differentiation of hematopoietic progenitor cells. GM-CSF is also capable of activating mature granulocytes and macrophages. After a bone marrow transplant or chemotherapy, patients have a reduced capacity to produce red and white blood cells. Supplementing them with external sources of GM-CSF helps bring the level of neutrophils back to normal so that they can better fight infections. The risk or severity of adverse effects can be increased when Sargramostim is combined with Bleomycin.The risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Sargramostim. DB00290DB00531 BleomycinCyclophosphamide Isoelectric PointMolecular WeightMolecular Formula 5.0514434.5C639H1006N168O196S8 L03AA09 Colony stimulating factorsIMMUNOSTIMULANTSIMMUNOSTIMULANTSANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L03AAL03AL03L Adjuvants, ImmunologicAmino Acids, Peptides, and ProteinsAntineoplastic and Immunomodulating AgentsBiological FactorsCarbohydratesColony-Stimulating FactorsCytokinesGlycoconjugatesGlycoproteinsHematopoietic Cell Growth FactorsImmunologic FactorsIntercellular Signaling Peptides and ProteinsLeukocyte Growth FactorPeptidesProteins D000276D000602D001685D002241D003115D016207D006001D006023D016298D007155D036341D010455D011506 46507000M13207PA164748631P04141DAP001053SargramostimCHEMBL1201670 PubChem SubstanceGenBankPharmGKBUniProtKBTherapeutic Targets DatabaseWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic/sargramostim.htmhttp://www.drugs.com/cdi/sargramostim.html approvedinvestigational Novartis Leucomax Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides 1341150 Canada 2000-12-05 2017-12-05 false SargramostimSargramostimSargramostim LeukineLeukineLeukine Bayer HealthcareGenzyme Inc.Hospira Inc.Kramer-NovisPhysicians Total Care Inc.Wyeth Pharmaceuticals http://www.bayerhealthcare.comhttp://www.genzyme.cahttp://www.hospira.comhttp://www.kramernovis.comhttp://www.physicianstotalcare.comhttp://www.wyeth.com LeukineLeukineLeukine falsefalsefalse Sanofi AventisSanofi AventisGenzyme Corporation falsefalsefalse Intravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; Subcutaneous Injection, powder, for solutionLiquidInjection, powder, for solution FDA NDCFDA NDCFDA NDC 250 ug/mL500 ug/mL250 ug/mL 0024-58430024-584458468-0180 BLA103362BLA103362BLA103362 truetruetrue USUSUS 1991-05-011996-12-012010-03-15 2016-06-30 vialcapsule 204.790.42 USDUSD Leukine 250 mcg vialBio-immunex capsule DB00021 Secretin biotech Martin Bickel, Rolf Geiger, Richard Leeb, Walter Petri, "Secretin preparations with intensified and protracted action, process for their manufacture, their use as well as dihydroxybenzoyl-L-tyrosine." U.S. Patent US4302448, issued August, 1964. solid This drug is the synthetic form of natural secretin. It is prepared using solid phase peptide synthesis. Secretin is a peptide hormone produced in the S cells of the duodenum. Its main effect is to regulate the pH of the small intestine’s contents through the control of gastric acid secretion and buffering with bicarbonate. It was the first hormone to be discovered. Humans and other mammals Powder, for solution Intravenous 75 unit For diagnosis of pancreatic exocrine dysfunction and gastrinoma Secretin binds to the secretin receptor found on the lining of S cells in the duodenum and G cells in the stomach. Binding leads to the secrection of bicarbonate or the reduction of the secretion of gastrin. Properly functioning organs (duodenum, pancreas and stomach) should be responsive to this hormone agonist Secretin receptor BE0000318 Human Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. 171392841701642311752352 P47872 Secretin receptor 2q14.1 Human plasma membraneintegral component of plasma membranecytoplasmic microtubulesecretin receptor activitydigestionG-protein coupled receptor signaling pathwaycell surface receptor signaling pathwayexcretion Secretin receptor activity This is a receptor for secretin. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase. Used in the diagnosis of pancreatic dysfunction or gastrinoma (stomach cancer), secretin is a hormone produced in the S cells of the duodenum in response to low local pH. It stimulates the secretion of bicarbonate from bicarbonate producing organs(liver, pancreas, Brunner's glands) when the pH drops below a set value. This helps neutralize the gastric acid entering the duodenum from the stomach. It also inhibits acid secretion from the stomach by reducing gastrin release from the G cells of the stomach. The therapeutic efficacy of Secretin can be decreased when used in combination with Benzatropine.The therapeutic efficacy of Secretin can be decreased when used in combination with Ipratropium bromide.The therapeutic efficacy of Secretin can be decreased when used in combination with Trihexyphenidyl.The therapeutic efficacy of Secretin can be decreased when used in combination with Procyclidine.The therapeutic efficacy of Secretin can be decreased when used in combination with Ethopropazine.The therapeutic efficacy of Secretin can be decreased when used in combination with Atropine.The therapeutic efficacy of Secretin can be decreased when used in combination with Scopolamine.The therapeutic efficacy of Secretin can be decreased when used in combination with Tropicamide.The therapeutic efficacy of Secretin can be decreased when used in combination with Biperiden.The therapeutic efficacy of Secretin can be decreased when used in combination with Cyclopentolate.The therapeutic efficacy of Secretin can be decreased when used in combination with Tiotropium.The therapeutic efficacy of Secretin can be decreased when used in combination with Dexetimide.The therapeutic efficacy of Secretin can be decreased when used in combination with Bornaprine.The therapeutic efficacy of Secretin can be decreased when used in combination with Phenglutarimide.The therapeutic efficacy of Secretin can be decreased when used in combination with Propantheline.The therapeutic efficacy of Secretin can be decreased when used in combination with Dicyclomine.The therapeutic efficacy of Secretin can be decreased when used in combination with Aclidinium.The therapeutic efficacy of Secretin can be decreased when used in combination with Glycopyrronium.The therapeutic efficacy of Secretin can be decreased when used in combination with Umeclidinium.The therapeutic efficacy of Secretin can be decreased when used in combination with Trospium.The therapeutic efficacy of Secretin can be decreased when used in combination with Oxyphenonium.The therapeutic efficacy of Secretin can be decreased when used in combination with Hyoscyamine.The therapeutic efficacy of Secretin can be decreased when used in combination with Gallamine Triethiodide.The therapeutic efficacy of Secretin can be decreased when used in combination with Darifenacin.The therapeutic efficacy of Secretin can be decreased when used in combination with Anisotropine Methylbromide.The therapeutic efficacy of Secretin can be decreased when used in combination with Mecamylamine.The therapeutic efficacy of Secretin can be decreased when used in combination with Pirenzepine.The therapeutic efficacy of Secretin can be decreased when used in combination with Atracurium besylate.The therapeutic efficacy of Secretin can be decreased when used in combination with Quinidine.The therapeutic efficacy of Secretin can be decreased when used in combination with Methantheline.The therapeutic efficacy of Secretin can be decreased when used in combination with Desloratadine.The therapeutic efficacy of Secretin can be decreased when used in combination with Tolterodine.The therapeutic efficacy of Secretin can be decreased when used in combination with Oxybutynin.The therapeutic efficacy of Secretin can be decreased when used in combination with Pentolinium.The therapeutic efficacy of Secretin can be decreased when used in combination with Trimethaphan.The therapeutic efficacy of Secretin can be decreased when used in combination with Orphenadrine.The therapeutic efficacy of Secretin can be decreased when used in combination with Tubocurarine.The therapeutic efficacy of Secretin can be decreased when used in combination with Pancuronium.The therapeutic efficacy of Secretin can be decreased when used in combination with Pipecuronium.The therapeutic efficacy of Secretin can be decreased when used in combination with Vecuronium.The therapeutic efficacy of Secretin can be decreased when used in combination with Solifenacin.The therapeutic efficacy of Secretin can be decreased when used in combination with Fesoterodine.The therapeutic efficacy of Secretin can be decreased when used in combination with Hexamethonium.The therapeutic efficacy of Secretin can be decreased when used in combination with Chlorphenoxamine.The therapeutic efficacy of Secretin can be decreased when used in combination with Benactyzine.The therapeutic efficacy of Secretin can be decreased when used in combination with Butylscopolamine.The therapeutic efficacy of Secretin can be decreased when used in combination with Propiverine.The therapeutic efficacy of Secretin can be decreased when used in combination with Atracurium.The therapeutic efficacy of Secretin can be decreased when used in combination with Otilonium.The therapeutic efficacy of Secretin can be decreased when used in combination with Emepronium.The therapeutic efficacy of Secretin can be decreased when used in combination with Gallamine.The therapeutic efficacy of Secretin can be decreased when used in combination with Alcuronium.The therapeutic efficacy of Secretin can be decreased when used in combination with Metixene.The therapeutic efficacy of Secretin can be decreased when used in combination with Homatropine.The therapeutic efficacy of Secretin can be decreased when used in combination with Oxitropium.The therapeutic efficacy of Secretin can be decreased when used in combination with Tropatepine.The therapeutic efficacy of Secretin can be decreased when used in combination with Mazaticol.The therapeutic efficacy of Secretin can be decreased when used in combination with Etybenzatropine.The therapeutic efficacy of Secretin can be decreased when used in combination with Etanautine.The therapeutic efficacy of Secretin can be decreased when used in combination with Methylscopolamine bromide. DB00245DB00332DB00376DB00387DB00392DB00572DB00747DB00809DB00810DB00979DB01409DB08997DB13619DB13413DB00782DB00804DB08897DB00986DB09076DB00209DB00219DB00424DB00483DB00496DB00517DB00657DB00670DB00732DB00908DB00940DB00967DB01036DB01062DB01090DB01116DB01173DB01199DB01337DB01338DB01339DB01591DB06702DB08960DB09007DB09023DB09300DB12278DB13295DB13500DB13505DB13584DB13648DB00340DB11181DB12086DB13252DB13448DB13468DB13636DB00462 BenzatropineIpratropium bromideTrihexyphenidylProcyclidineEthopropazineAtropineScopolamineTropicamideBiperidenCyclopentolateTiotropiumDexetimideBornaprinePhenglutarimidePropanthelineDicyclomineAclidiniumGlycopyrroniumUmeclidiniumTrospiumOxyphenoniumHyoscyamineGallamine TriethiodideDarifenacinAnisotropine MethylbromideMecamylaminePirenzepineAtracurium besylateQuinidineMethanthelineDesloratadineTolterodineOxybutyninPentoliniumTrimethaphanOrphenadrineTubocurarinePancuroniumPipecuroniumVecuroniumSolifenacinFesoterodineHexamethoniumChlorphenoxamineBenactyzineButylscopolaminePropiverineAtracuriumOtiloniumEmeproniumGallamineAlcuroniumMetixeneHomatropineOxitropiumTropatepineMazaticolEtybenzatropineEtanautineMethylscopolamine bromide HydrophobicityIsoelectric PointMolecular WeightMolecular Formula -0.4639.453056.4C130H219N43O42 V04CK01 Tests for pancreatic functionOTHER DIAGNOSTIC AGENTSDIAGNOSTIC AGENTSVARIOUS V04CKV04CV04V Amino Acids, Peptides, and ProteinsChemical Actions and UsesDiagnostic AgentsGastrointestinal AgentsGastrointestinal HormonesHormonesHormones, Hormone Substitutes, and Hormone AntagonistsNerve Tissue ProteinsNeuropeptidesPeptide HormonesPeptidesPharmacologic ActionsPhysiological Effects of DrugsProteinsTests for Pancreatic FunctionTherapeutic Uses D000602D020164D005765D005768D006728D006730D009419D009479D036361D010455D020228D045505D011506D045506 206746508060PA164760844DAP001296SecretinCHEMBL2103754 Drugs Product Database (DPD)PubChem SubstancePharmGKBTherapeutic Targets DatabaseWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic3/secretin.htmhttp://www.drugs.com/human_secretin.html approvedinvestigational Repligen CorpRepligen Corp SecreFloSecremax Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides Ferring pharmaceuticals incChirhoclin inc falsefalse Secretin Secretin Inj 75unit/vial Professional Co. Secretin Inj 75unit/vial false Ferring Pharmaceuticals false Intravenous Powder, for solution DPD 75 unit true 00874000 Canada 1990-12-31 1999-08-04 g 1.43 USD Secretin-mannitol powder DB00022 215647-85-1 Peginterferon alfa-2b biotech G8RGG88B68 liquid Peginterferon alfa-2b is a form of recombinant interferon used as part of combination therapy to treat chronic Hepatitis C, an infectious liver disease caused by infection with Hepatitis C Virus (HCV). HCV is a single-stranded RNA virus that is categorized into nine distinct genotypes, with genotype 1 being the most common in the United States, and affecting 72% of all chronic HCV patients [L852]. Treatment options for chronic Hepatitis C have advanced significantly since 2011, with the development of Direct Acting Antivirals (DAAs) resulting in less use of Peginterferon alfa-2b. Peginterferon alfa-2b is derived from the alfa-2b moeity of recombinant human interferon and acts by binding to human type 1 interferon receptors. Activation and dimerization of this receptor induces the body's innate antiviral response by activating the janus kinase/signal transducer and activator of transcription (JAK/STAT) pathway. Use of Peginterferon alfa-2b is associated with a wide range of severe adverse effects including the aggravation and development of endocrine and autoimmune disorders, retinopathies, cardiovascular and neuropsychiatric complications, and increased risk of hepatic decompensation in patients with cirrhosis. The use of Peginterferon alfa-2b has largely declined since newer interferon-free antiviral therapies have been developed.In a joint recommendation published in 2016, the American Association for the Study of Liver Diseases (AASLD) and the Infectious Diseases Society of America (IDSA) no longer recommend Peginterferon alfa-2b for the treatment of Hepatitis C [A19593]. Peginterferon alfa-2b was used alongside [DB00811] with the intent to cure, or achieve a sustained virologic response (SVR), after 48 weeks of therapy. SVR and eradication of HCV infection is associated with significant long-term health benefits including reduced liver-related damage, improved quality of life, reduced incidence of Hepatocellular Carcinoma, and reduced all-cause mortality [A19626].Peginterferon alfa-2b is available as a variable dose injectable product (tradename Pegintron) used for the treatment of chronic Hepatitis C. Approved in 2001 by the FDA, Pegintron is indicated for the treatment of HCV with [DB00811] or other antiviral drugs [FDA Label]. When combined together, Peginterferon alfa-2b and [DB00811] have been shown to achieve a SVR between 41% for genotype 1 and 75% for genotypes 2-6 after 48 weeks of treatment. Humans and other mammals Capsule; powder, for solutionInjection, powder, lyophilized, for solutionInjection, powder, lyophilized, for solutionInjection, powder, lyophilized, for solutionInjection, powder, lyophilized, for solutionKitPowder, for solutionPowder, for solutionPowder, for solutionPowder, for solution Oral; SubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneous 120 ug/.5mL150 ug/.5mL50 ug/.5mL80 ug/.5mL118.4 mcg177.6 mcg222 mcg74 mcg Peginterferon alfa-2b is indicated for the treatment of HCV in combination with [DB00811] and a NS3/4A protease inhibitor for genotype 1 or without a NS3/4A protease inhibitor for genotypes 2-6 [FDA Label]. May be used as a monotherapy in patients with contraindications to or significant intolerance to other anti-viral therapies. Peginterferon alfa-2b is derived from recombinant human interferon's alfa-2b moeity [FDA Label]. It binds to and activates human type 1 interferon receptors causing them to dimerize. This activates the JAK/STAT pathway. Activation of the JAK/STAT pathway increases expression of multiple genes in multiple tissues involved in the innate antiviral response. Peginterferon alfa-2b may also acitvate the nuclear factor κB pathway. agonistagonist Interferon alpha/beta receptor 1Interferon alpha/beta receptor 2 BE0000661BE0000385 HumanHuman Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Dhalluin C, Ross A, Huber W, Gerber P, Brugger D, Gsell B, Senn H: Structural, kinetic, and thermodynamic analysis of the binding of the 40 kDa PEG-interferon-alpha2a and its individual positional isomers to the extracellular domain of the receptor IFNAR2. Bioconjug Chem. 2005 May-Jun;16(3):518-27.Ishii K, Shinohara M, Sawa M, Kogame M, Higami K, Sano M, Morita T, Sumino Y: Interferon alpha receptor 2 expression by peripheral blood monocytes in patients with a high viral load of hepatitis C virus genotype 1 showing substitution of amino Acid 70 in the core region. Intervirology. 2010;53(2):105-10. doi: 10.1159/000264200. Epub 2009 Dec 3.Yano H, Ogasawara S, Momosaki S, Akiba J, Kojiro S, Fukahori S, Ishizaki H, Kuratomi K, Basaki Y, Oie S, Kuwano M, Kojiro M: Growth inhibitory effects of pegylated IFN alpha-2b on human liver cancer cells in vitro and in vivo. Liver Int. 2006 Oct;26(8):964-75.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Dhalluin C, Ross A, Huber W, Gerber P, Brugger D, Gsell B, Senn H: Structural, kinetic, and thermodynamic analysis of the binding of the 40 kDa PEG-interferon-alpha2a and its individual positional isomers to the extracellular domain of the receptor IFNAR2. Bioconjug Chem. 2005 May-Jun;16(3):518-27.Ishii K, Shinohara M, Sawa M, Kogame M, Higami K, Sano M, Morita T, Sumino Y: Interferon alpha receptor 2 expression by peripheral blood monocytes in patients with a high viral load of hepatitis C virus genotype 1 showing substitution of amino Acid 70 in the core region. Intervirology. 2010;53(2):105-10. doi: 10.1159/000264200. Epub 2009 Dec 3.Yano H, Ogasawara S, Momosaki S, Akiba J, Kojiro S, Fukahori S, Ishizaki H, Kuratomi K, Basaki Y, Oie S, Kuwano M, Kojiro M: Growth inhibitory effects of pegylated IFN alpha-2b on human liver cancer cells in vitro and in vivo. Liver Int. 2006 Oct;26(8):964-75.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. 171392841701642315898717199558151695383711752352171392841701642315898717199558151695383711752352 P17181P48551 Interferon alpha/beta receptor 1Interferon alpha/beta receptor 2 HumanHuman intracellularplasma membraneintegral component of plasma membranetype I interferon receptor activityregulation of type I interferon-mediated signaling pathwayresponse to virustype I interferon signaling pathwaypositive regulation of transcription, DNA-templateddefense response to viruscell surface receptor signaling pathwaypositive regulation of interleukin-1 beta secretioncytokine-mediated signaling pathwaypositive regulation of interferon-beta productionregulation of peptidyl-tyrosine phosphorylationtype I interferon biosynthetic processpositive regulation of interferon-gamma productionT cell activationJAK-STAT cascadeintracellularextracellular regionplasma membraneextracellular spaceintegral component of plasma membraneprotein kinase bindingtype I interferon bindingtype I interferon receptor activityJAK-STAT cascaderegulation of transcription from RNA polymerase II promoterregulation of type I interferon-mediated signaling pathwayresponse to interferon-alphacell proliferationresponse to virustype I interferon signaling pathwaycell surface receptor signaling pathwaycytokine-mediated signaling pathway Type i interferon receptor activityType i interferon receptor activity Associates with IFNAR2 to form the type I interferon receptor. Receptor for interferons alpha and beta. Binding to type I IFNs triggers tyrosine phosphorylation of a number of proteins including JAKs, TYK2, STAT proteins and IFNR alpha- and beta-subunits themselves. Can also transduce IFNB signals without the help of IFNAR2, and not activating the Jak-STAT pathway.Associates with IFNAR1 to form the type I interferon receptor. Receptor for interferons alpha and beta. Involved in IFN-mediated STAT1, STAT2 and STAT3 activation. Isoform 1 and isoform 2 are directly involved in signal transduction due to their association with the TYR kinase, JAK1. Isoform 3 is a potent inhibitor of type I IFN receptor activity. Peginterferon alfa-2b may manifest neuropsychiatric complications include suicide, suicidal ideation, homicidal ideation, depression, relapse of drug addiction, and drug overdose [FDA Label]. Hypertension, supraventricular arrhythmias, chest pain, and myocardial infarction have been observed in patients using Peginterferon alfa-2b. Peginterferon alfa-2b may produce myelosuppression as well as the development or aggravation of autoimmune disorders including myositis, hepatitis, thrombotic thrombocytopenic purpura, idiopathic thrombocytopenic purpura, psoriasis, rheumatoid arthritis, interstitial nephritis, thyroiditis, and systemic lupus erythematosus. Peginterferon alfa-2b causes or aggravates hypothyroidism and hyperthyroidism. Hyperglycemia, hypoglycemia, and diabetes mellitus have been observed to develop in patients treated with Peginterferon alfa-2b. Peginterferon alfa-2b may decrease or produce loss of vision, retinopathy including macular edema, retinal artery or vein thrombosis, retinal hemorrhages and cotton wool spots, optic neuritis, papilledema and serous retinal detachment. Peginterferon mayy be related to increased ischemic and hemorrhagic cerebrovascular events. Patients with cirrhosis on Peginterferon alfa-2b are at risk of hepatic decompensation. Dyspnea, pulmonary infiltrates, pneumonia, bronchiolitis obliterans, interstitial pneumonitis, pulmonary hypertension and sarcoidosis may be induced or aggravated by Peginterferon alfa-2b. Serious and severe infections (bacterial, viral, or fungal) have been reported during treatment with Peginterferon alfa-2b. Ulcerative and hemorrhagic/ischemic colitis have been observed within 12 weeks of starting Peginterferon alfa-2b treatment. Pancreatitis and peripheral nephropathy have also been reported. Peginterferon alfa-2b is associated with growth inhibition in pediatric patients. Use of Peginterferon alfa-2b while pregant may result in delopmental abnormalities or death of the fetus. The mean half-life of elimination of Peginterferon alfa-2b is 40 hours in a range of 22-60 hours [FDA Label]. Peginterferon alfa-2b reaches peak plasma concentration 15-44 hours after subcutaneous administration [FDA Label]. The mean absorption half-life is 4.6 hours. After multiple doses the bioavailability of Peginterferon alfa-2b increases with trough concentrations at week 48 3-fold higher than those at week 4. The estimated apparent clearance of Peginterferon alfa-2b is 22 milliters per hour per kilogram [FDA Label]. Renal elimination accounts for 30% of Peginterferon alfa-2b elimination [FDA Label]. Peginterferon alfa-2b inhibits viral replication in infected cells, suppresses cell proliferation, induces apoptosis, and exerts an anti-angiogenic effect [FDA Label]. Exerts immunomodulatory effects such as enhancement of the phagocytic activity of macrophages, activation of NK cells, stimulation of cytotoxic T-lymphocytes, and the upregulation of the Th1 T-helper cell subset. Also increases concentrations of effector proteins such as serum neopterin and 2'5' oligoadenylate synthetase, raises body temperature, and causes reversible decreases in leukocyte and platelet counts. The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Aldesleukin.The serum concentration of Tizanidine can be increased when it is combined with Peginterferon alfa-2b.The therapeutic efficacy of Peginterferon alfa-2b can be decreased when used in combination with Pegloticase.The metabolism of Ambroxol acefyllinate can be decreased when combined with Peginterferon alfa-2b.The metabolism of Dyphylline can be decreased when combined with Peginterferon alfa-2b.The serum concentration of Methadone can be increased when it is combined with Peginterferon alfa-2b.The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Ribavirin.The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Zidovudine.The serum concentration of Fluoxetine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Fluvoxamine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Amphetamine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Cevimeline can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Tramadol can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Lidocaine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Venlafaxine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Atomoxetine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Morphine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Codeine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Ipratropium bromide can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Mirtazapine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Timolol can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Mexiletine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Prochlorperazine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Pethidine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Duloxetine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Chlorpromazine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Darifenacin can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Oxycodone can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Haloperidol can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Ritonavir can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Dextromethorphan can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Carteolol can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Clonidine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Bisoprolol can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Fluphenazine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Trazodone can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Galantamine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Tamoxifen can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Nicergoline can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Paroxetine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Risperidone can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Dolasetron can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Minaprine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Donepezil can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Perphenazine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Ranitidine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Alprenolol can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Ondansetron can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Phenformin can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Almotriptan can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Maprotiline can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Hydrocodone can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Pindolol can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Formoterol can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Procainamide can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Tolterodine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Promethazine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Perhexiline can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Chlorphenamine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Carvedilol can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Doxepin can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Desipramine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Flecainide can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Captopril can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Encainide can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Metoclopramide can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Clomipramine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Moclobemide can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Arformoterol can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Ethylmorphine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Tiotropium can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Diphenhydramine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Debrisoquin can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Citalopram can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Gefitinib can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Amitriptyline can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Hydromorphone can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Terfenadine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Diltiazem can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Chlorzoxazone can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Clozapine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Loratadine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Imipramine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Quinine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Mephenytoin can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Nortriptyline can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Nicardipine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Delavirdine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Trimipramine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Buprenorphine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Mesoridazine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Azelastine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Mequitazine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Sertraline can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Nifedipine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Amiodarone can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Nefazodone can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Bupropion can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Escitalopram can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Propafenone can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Dexfenfluramine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Oxymorphone can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Halofantrine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Aripiprazole can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Methotrimeprazine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Dihydrocodeine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Palonosetron can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Nebivolol can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Sertindole can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Mianserin can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Tesmilifene can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Zuclopenthixol can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Dextroamphetamine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Propranolol can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Rotigotine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Lisuride can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Fluvastatin can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Imatinib can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Olanzapine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Bortezomib can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Trabectedin can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Cinnarizine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Flunarizine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Bufuralol can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of 4-Methoxyamphetamine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Phenacetin can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Sparteine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Doxorubicin can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Ticlopidine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Amoxapine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Chloroquine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Iloperidone can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Methamphetamine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Pipotiazine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Protriptyline can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Tamsulosin can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Tetrabenazine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Tipranavir can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Dronedarone can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Aminophenazone can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Nevirapine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Eletriptan can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Zolpidem can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Etoricoxib can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Sildenafil can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Acetaminophen can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Cyclobenzaprine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Acetylcholine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Ajmaline can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Amprenavir can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Amsacrine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Aprindine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Artemether can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Astemizole can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Benzatropine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Bepridil can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Betaxolol can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Brompheniramine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Bupivacaine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Buspirone can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Caffeine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Cephalexin can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Chlordiazepoxide can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Cyclophosphamide can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Domperidone can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Dopamine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Doxazosin can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Epinastine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Granisetron can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Halothane can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Idarubicin can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Labetalol can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Levodopa can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Lomustine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Methoxyflurane can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Methylphenidate can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Methyprylon can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Nateglinide can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Nicotine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Nitrofural can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Pentamidine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Antipyrine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Piperazine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Progesterone can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Propofol can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Pseudoephedrine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Quetiapine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Remoxipride can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Ropivacaine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Saquinavir can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Simvastatin can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Tegaserod can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Theophylline can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Vinblastine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Vinorelbine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Yohimbine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Zalcitabine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Dexmethylphenidate can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Erlotinib can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Cilostazol can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Pazopanib can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Fesoterodine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Vilazodone can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Loperamide can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Repinotan can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Benzyl alcohol can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Clevidipine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Enclomiphene can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Tapentadol can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Fingolimod can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Lorcaserin can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Mirabegron can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Ponatinib can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Alogliptin can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Levomilnacipran can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Dapagliflozin can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Eliglustat can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Netupitant can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Ibrutinib can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Umeclidinium can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Vortioxetine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Cariprazine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Brexpiprazole can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Esmirtazapine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Ixazomib can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Dasabuvir can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Rucaparib can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Dexchlorpheniramine maleate can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Deutetrabenazine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Vernakalant can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Valbenazine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Perospirone can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Rupatadine can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Enasidenib can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Letermovir can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Lorpiprazole can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Opium can be decreased when it is combined with Peginterferon alfa-2b.The serum concentration of Anagrelide can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Carmustine can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Ropinirole can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Conjugated estrogens can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Zolmitriptan can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Grepafloxacin can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Tacrine can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Flutamide can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Fluorouracil can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Estrone can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Verapamil can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Warfarin can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Riluzole can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Zileuton can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Estradiol can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Diazepam can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Dacarbazine can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Lomefloxacin can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Ramelteon can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Frovatriptan can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Levobupivacaine can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Cinacalcet can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Hesperetin can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Leflunomide can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Pimozide can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Alosetron can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Rasagiline can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Pantoprazole can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Rofecoxib can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Diclofenac can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Thiabendazole can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Telithromycin can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Acenocoumarol can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Melatonin can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Thalidomide can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Carbamazepine can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Terbinafine can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Naproxen can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Omeprazole can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Aminophylline can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Asenapine can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Estrone sulfate can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Guanabenz can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Thiothixene can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Trifluoperazine can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Primaquine can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Clopidogrel can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Promazine can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Genistein can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Resveratrol can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Albendazole can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Aprepitant can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Bromazepam can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Cisapride can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Clenbuterol can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Daunorubicin can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Dinoprostone can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Ergotamine can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Ethanol can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Etoposide can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Flunitrazepam can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Hexobarbital can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Imiquimod can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Lumiracoxib can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Malathion can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Menadione can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Oxaliplatin can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Pentoxifylline can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Praziquantel can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Proguanil can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Pyrazinamide can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Rifabutin can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Selegiline can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Temafloxacin can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Theobromine can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Tolperisone can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Toremifene can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Triamterene can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Ziprasidone can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Oxtriphylline can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Dasatinib can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Eltrombopag can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Rizatriptan can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Muraglitazar can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Vadimezan can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Nabumetone can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Nitric Oxide can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Ulipristal can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Apixaban can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Axitinib can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Pomalidomide can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Bendamustine can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Icotinib can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Stiripentol can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Voxilaprevir can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Estradiol acetate can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Estradiol benzoate can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Estradiol cypionate can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Estradiol dienanthate can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Estradiol valerate can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Zotepine can be increased when it is combined with Peginterferon alfa-2b.The risk or severity of myelosuppression can be increased when Metamizole is combined with Peginterferon alfa-2b.The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Telbivudine.The serum concentration of Pitolisant can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Metoprolol can be increased when it is combined with Peginterferon alfa-2b.The serum concentration of Thioridazine can be increased when it is combined with Peginterferon alfa-2b. 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AldesleukinTizanidinePegloticaseAmbroxol acefyllinateDyphyllineMethadoneRibavirinZidovudineFluoxetineFluvoxamineAmphetamineCevimelineTramadolLidocaineVenlafaxineAtomoxetineMorphineCodeineIpratropium bromideMirtazapineTimololMexiletineProchlorperazinePethidineDuloxetineChlorpromazineDarifenacinOxycodoneHaloperidolRitonavirDextromethorphanCarteololClonidineBisoprololFluphenazineTrazodoneGalantamineTamoxifenNicergolineParoxetineRisperidoneDolasetronMinaprineDonepezilPerphenazineRanitidineAlprenololOndansetronPhenforminAlmotriptanMaprotilineHydrocodonePindololFormoterolProcainamideTolterodinePromethazinePerhexilineChlorphenamineCarvedilolDoxepinDesipramineFlecainideCaptoprilEncainideMetoclopramideClomipramineMoclobemideArformoterolEthylmorphineTiotropiumDiphenhydramineDebrisoquinCitalopramGefitinibAmitriptylineHydromorphoneTerfenadineDiltiazemChlorzoxazoneClozapineLoratadineImipramineQuinineMephenytoinNortriptylineNicardipineDelavirdineTrimipramineBuprenorphineMesoridazineAzelastineMequitazineSertralineNifedipineAmiodaroneNefazodoneBupropionEscitalopramPropafenoneDexfenfluramineOxymorphoneHalofantrineAripiprazoleMethotrimeprazineDihydrocodeinePalonosetronNebivololSertindoleMianserinTesmilifeneZuclopenthixolDextroamphetaminePropranololRotigotineLisurideFluvastatinImatinibOlanzapineBortezomibTrabectedinCinnarizineFlunarizineBufuralol4-MethoxyamphetaminePhenacetinSparteineDoxorubicinTiclopidineAmoxapineChloroquineIloperidoneMethamphetaminePipotiazineProtriptylineTamsulosinTetrabenazineTipranavirDronedaroneAminophenazoneNevirapineEletriptanZolpidemEtoricoxibSildenafilAcetaminophenCyclobenzaprineAcetylcholineAjmalineAmprenavirAmsacrineAprindineArtemetherAstemizoleBenzatropineBepridilBetaxololBrompheniramineBupivacaineBuspironeCaffeineCephalexinChlordiazepoxideCyclophosphamideDomperidoneDopamineDoxazosinEpinastineGranisetronHalothaneIdarubicinLabetalolLevodopaLomustineMethoxyfluraneMethylphenidateMethyprylonNateglinideNicotineNitrofuralPentamidineAntipyrinePiperazineProgesteronePropofolPseudoephedrineQuetiapineRemoxiprideRopivacaineSaquinavirSimvastatinTegaserodTheophyllineVinblastineVinorelbineYohimbineZalcitabineDexmethylphenidateErlotinibCilostazolPazopanibFesoterodineVilazodoneLoperamideRepinotanBenzyl alcoholClevidipineEnclomipheneTapentadolFingolimodLorcaserinMirabegronPonatinibAlogliptinLevomilnacipranDapagliflozinEliglustatNetupitantIbrutinibUmeclidiniumVortioxetineCariprazineBrexpiprazoleEsmirtazapineIxazomibDasabuvirRucaparibDexchlorpheniramine maleateDeutetrabenazineVernakalantValbenazinePerospironeRupatadineEnasidenibLetermovirLorpiprazoleOpiumAnagrelideCarmustineRopiniroleConjugated estrogensZolmitriptanGrepafloxacinTacrineFlutamideFluorouracilEstroneVerapamilWarfarinRiluzoleZileutonEstradiolDiazepamDacarbazineLomefloxacinRamelteonFrovatriptanLevobupivacaineCinacalcetHesperetinLeflunomidePimozideAlosetronRasagilinePantoprazoleRofecoxibDiclofenacThiabendazoleTelithromycinAcenocoumarolMelatoninThalidomideCarbamazepineTerbinafineNaproxenOmeprazoleAminophyllineAsenapineEstrone sulfateGuanabenzThiothixeneTrifluoperazinePrimaquineClopidogrelPromazineGenisteinResveratrolAlbendazoleAprepitantBromazepamCisaprideClenbuterolDaunorubicinDinoprostoneErgotamineEthanolEtoposideFlunitrazepamHexobarbitalImiquimodLumiracoxibMalathionMenadioneOxaliplatinPentoxifyllinePraziquantelProguanilPyrazinamideRifabutinSelegilineTemafloxacinTheobromineTolperisoneToremifeneTriamtereneZiprasidoneOxtriphyllineDasatinibEltrombopagRizatriptanMuraglitazarVadimezanNabumetoneNitric OxideUlipristalApixabanAxitinibPomalidomideBendamustineIcotinibStiripentolVoxilaprevirEstradiol acetateEstradiol benzoateEstradiol cypionateEstradiol dienanthateEstradiol valerateZotepineMetamizoleTelbivudinePitolisantMetoprololThioridazine Melting PointIsoelectric PointMolecular Weight 61 °C5.9931000.0 Beldarrain, A. et al., Biochemistry 38:7865-7873 (1999) L03AB60L03AB10 InterferonsIMMUNOSTIMULANTSIMMUNOSTIMULANTSANTINEOPLASTIC AND IMMUNOMODULATING AGENTSInterferonsIMMUNOSTIMULANTSIMMUNOSTIMULANTSANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L03ABL03AL03LL03ABL03AL03L Adjuvants, ImmunologicAlcoholsAlfa InterferonsAmino Acids, Peptides, and ProteinsAnti-Infective AgentsAntineoplastic and Immunomodulating AgentsAntiviral AgentsBiological FactorsBiomedical and Dental MaterialsChemical Actions and UsesCytochrome P-450 CYP1A2 InhibitorsCytochrome P-450 CYP1A2 Inhibitors (weak)Cytochrome P-450 CYP2D6 InhibitorsCytochrome P-450 CYP2D6 Inhibitors (weak)Cytochrome P-450 Enzyme InhibitorsCytokinesDrug CarriersEthylene GlycolsGlycolsHepatitis CIntercellular Signaling Peptides and ProteinsInterferon alphaInterferon Type IInterferonsMacromolecular SubstancesManufactured MaterialsMyelosuppressive AgentsOrganic ChemicalsPeptidesPharmacologic ActionsPolymersProteinsSpecialty Uses of ChemicalsTechnology, Industry, and AgricultureTherapeutic Uses D000276D000438D000602D000890D000998D001685D001697D020164D065609D065690D065607D016207D004337D005026D006018D006526D036341D016898D007370D007372D046911D008420D009930D010455D020228D011108D011506D020313D013676D045506 1203646506669PA164784024P01563DAP001279Peginterferon_alfa-2bCHEMBL1201561 Drugs Product Database (DPD)PubChem SubstancePharmGKBUniProtKBTherapeutic Targets DatabaseWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic2/peginterferon.htmhttp://www.drugs.com/cdi/peginterferon-alfa-2b.html //s3-us-west-2.amazonaws.com/drugbank/fda_labels/DB00022.pdf?1497629687 Myers RP, Shah H, Burak KW, Cooper C, Feld JJ: An update on the management of chronic hepatitis C: 2015 Consensus guidelines from the Canadian Association for the Study of the Liver. Can J Gastroenterol Hepatol. 2015 Jan-Feb;29(1):19-34. Epub 2015 Jan 13.Bagaglio S, Uberti-Foppa C, Morsica G: Resistance Mechanisms in Hepatitis C Virus: implications for Direct-Acting Antiviral Use. Drugs. 2017 May 12. doi: 10.1007/s40265-017-0753-x. 2558534828497432 approved Schering Corp PEG-Intron Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides 13415672329474 CanadaCanada 2008-02-190002-02-26 2025-02-192016-10-31 falsefalse Peginterferon alfa-2bPeginterferon alfa-2bPeginterferon alfa-2bPeginterferon alfa-2bPeginterferon alfa-2bPeginterferon alfa-2bPeginterferon alfa-2bPeginterferon alfa-2bPeginterferon alfa-2b + RibavirinPeginterferon alfa-2b + RibavirinPeginterferon alfa-2b + RibavirinBoceprevir + Peginterferon alfa-2b + RibavirinBoceprevir + Peginterferon alfa-2b + RibavirinBoceprevir + Peginterferon alfa-2b + RibavirinBoceprevir + Peginterferon alfa-2b + RibavirinPeginterferon alfa-2b + RibavirinPeginterferon alfa-2b + RibavirinPeginterferon alfa-2bPeginterferon alfa-2bPeginterferon alfa-2bPeginterferon alfa-2bPeginterferon alfa-2bPeginterferon alfa-2bPeginterferon alfa-2bPeginterferon alfa-2bPeginterferon alfa-2bPeginterferon alfa-2bPeginterferon alfa-2bPeginterferon alfa-2bPeginterferon alfa-2bPeginterferon alfa-2bPeginterferon alfa-2b + RibavirinPeginterferon alfa-2b + RibavirinPeginterferon alfa-2b + RibavirinPeginterferon alfa-2b + Ribavirin PegintronPegintronPegintronPegintronUnitron PegUnitron PegUnitron PegUnitron PegPegetronPegetronPegetronVictrelis TripleVictrelis TripleVictrelis TripleVictrelis TriplePegetronPegetronSylatronPegintronSylatronPegintronPegintronPegintronSylatronSylatronSylatronSylatronPegintronPegintronPegintronPegintronPegetronPegetronPegetronPegetron Physicians Total Care Inc.Schering Corp.Schering-Plough Inc.Vetter Pharma Fertigung GmbH and Co. KG http://www.physicianstotalcare.comhttp://www.schering.dehttp://www.schering-plough.cahttp://www.vetter-pharma.com PegetronPegetronPegetronPegetronPegetronPegetronPegetronPegetronPegetronPegintronPegintronPegintronPegintronPegintronPegintronPegintronPegintronPegintronPegintronPegintronPegintronSylatronSylatronSylatronSylatronSylatronSylatronUnitron PegUnitron PegUnitron PegUnitron PegVictrelis TripleVictrelis TripleVictrelis TripleVictrelis Triple falsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalse Merck Ltd.Merck Ltd.Merck Ltd.Merck Ltd.Merck Ltd.Merck Ltd.Merck Ltd.Merck Ltd.Merck Ltd.Merck Sharp & Dohme LimitedMerck Sharp & Dohme LimitedMerck Sharp & Dohme LimitedMerck Sharp & Dohme LimitedMerck Sharp & Dohme LimitedMerck Sharp & Dohme LimitedMerck Sharp & Dohme LimitedMerck Sharp & Dohme LimitedMerck Sharp & Dohme LimitedMerck Sharp & Dohme LimitedMerck Sharp & Dohme LimitedMerck Sharp & Dohme LimitedMerck Sharp & Dohme LimitedMerck Sharp & Dohme LimitedMerck Sharp & Dohme LimitedMerck Sharp & Dohme LimitedMerck Sharp & Dohme LimitedMerck Sharp & Dohme LimitedMerck Ltd.Merck Ltd.Merck Ltd.Merck Ltd.Merck Ltd.Merck Ltd.Merck Ltd.Merck Ltd. falsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalse Oral; SubcutaneousOral; SubcutaneousOral; SubcutaneousOral; SubcutaneousOral; SubcutaneousOral; SubcutaneousOral; SubcutaneousOral; SubcutaneousOral; SubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousOral; SubcutaneousOral; SubcutaneousOral; SubcutaneousOral; Subcutaneous Capsule; Powder, for solutionCapsule; Powder, for solutionCapsule; Powder, for solutionCapsule; Powder, for solutionCapsule; Powder, for solutionCapsule; Powder, for solutionCapsule; Powder, for solutionCapsule; Powder, for solutionCapsule; Powder, for solutionKitKitKitKitInjection, powder, lyophilized, for solutionInjection, powder, lyophilized, for solutionInjection, powder, lyophilized, for solutionInjection, powder, lyophilized, for solutionKitKitKitKitKitKitKitKitKitKitPowder, for solutionPowder, for solutionPowder, for solutionPowder, for solutionCapsule; Powder, for solutionCapsule; Powder, for solutionCapsule; Powder, for solutionCapsule; Powder, for solution DPDDPDDPDDPDDPDDPDDPDDPDDPDFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCDPDDPDDPDDPDDPDDPDDPDDPD 120 ug/.5mL80 ug/.5mL50 ug/.5mL150 ug/.5mL74 mcg118.4 mcg177.6 mcg222 mcg 0085-12790085-12910085-13040085-13680085-12970085-13160085-13230085-13700085-43530085-43540085-43550085-43560085-12870085-13120085-13880085-43470085-43480085-4349 BLA103949BLA103949BLA103949BLA103949BLA103949BLA103949BLA103949BLA103949BLA103949BLA103949BLA103949BLA103949BLA103949BLA103949BLA103949BLA103949BLA103949BLA103949 truetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetrue 0225458102254603022546380225464602246026022460300224602702246028022460290224296602242967022429680224296902371448023714560237146402371472 CanadaCanadaCanadaCanadaCanadaCanadaCanadaCanadaCanadaUSUSUSUSUSUSUSUSUSUSUSUSUSUSUSUSUSUSCanadaCanadaCanadaCanadaCanadaCanadaCanadaCanada 2004-09-172004-09-172004-09-172004-09-172002-08-132002-08-132002-08-132002-08-132002-08-132001-01-192001-01-192001-01-192001-01-192001-01-192001-01-192001-01-192001-01-192014-08-112014-08-112014-08-112014-08-112011-03-292011-03-292011-03-292014-08-302011-03-292011-03-292001-03-272001-03-272001-03-272001-03-272011-08-162011-08-162011-08-162011-08-16 2017-04-042017-04-042013-01-232013-01-232013-01-232017-06-212017-06-212017-06-212017-06-212017-12-222017-12-222017-12-222012-02-012012-02-012012-02-012012-02-012017-01-102017-01-102016-09-022016-09-02 kitredipenredipenkitkitredipenkitkitredipenredipenkitkitkitkit 553.4553.4581.02607.19609.26610.09637.49639.74640.6640.61669.39671.74702.872428.8 USDUSDUSDUSDUSDUSDUSDUSDUSDUSDUSDUSDUSDUSD Peg-Intron 50 mcg kitPeg-Intron redipen 50 mcgPeg-Intron redipen 80 mcgPeg-Intron 50 mcg/0.5ml KitPeg-Intron 80 mcg KitPeg-Intron redipen 120 mcgPeg-Intron Redipen 80 mcg/0.5ml KitPeg-Intron 120 mcg KitPeg-Intron redipen 150 mcg 4pkPeg-Intron redipen 150 mcgPeg-Intron Redipen 120 mcg/0.5ml KitPeg-Intron 150 mcg KitPeg-Intron Redipen 150 mcg/0.5ml KitPeg-Intron Redipen Pak 4 4 50 mcg/0.5ml Kit Box DB00023 9015-68-3 Asparaginase Escherichia coli AsparaginaseAsparaginase (E. coli)ColaspaseEscherichia coli L-asparaginaseL-asparaginaseL-asparagine amidohydrolase biotech G4FQ3CKY5R Masao Nambu, "Process for producing immobilized L-asparaginase preparations for the therapy of leukemia." U.S. Patent US4617271, issued January, 1977. liquid Asparaginase derived from _Escherichia coli_ (L-asparagine amidohydrolase, EC 3.5.1.1) is an enzyme responsible for the metabolism of L-asparagine, by catalyzing L-asparagine into L-aspartic acid and ammonia. It also facilitates the production of oxaloacetate which is needed for general cellular metabolism. Asparaginase from _E. coli_ has clinically shown to exhibit antitumor actions in models of leukaemias [A31996, A31997]. L-asparaginase of _E. coli_ is marketed under several different trade names, including Elspar, for the treatment of acute lymphoblastic leukemia (ALL) as part of a multi-agent chemotherapeutic regimen. It is available as intramuscular or intravenous injections. Therapeutic L-asparaginase from _E. coli_ works by depleting the levels of non-essential amino acid, asparagine, in lymphoblastic leukemic cells thus promoting apoptotic cell death [A31999]. For patients who develop hypersensitivity to _E. coli_-derived formulations of L-asparaginase, the use of PEGylated or non-PEGylated [DB08886] is recommended [A31999]. Humans and other mammals Powder, for solutionInjection, powder, for solution Intramuscular; IntravenousIntravenous 10000 unit10000 U Indicated as a component of a multi-agent chemotherapeutic regimen for the treatment of patients with acute lymphoblastic leukemia (ALL) [FDA Label]. Asparagine is a non-essential amino acid that maintains DNA, RNA and protein synthesis and promotes cell growth. While healthy and normal cells are capable of obtaining asparagine via dietary intake or synthesizing the asparagine from aspartate via asparagine synthetase activity, lymphoblastic leukemic cells lack the asparagine synthetase enzyme and cannot produce asparagine _de novo_ [A31999]. Thus, leukemic cells rely on exogenous source of asparagine for protein synthesis and cell survival [A31999]. L-asparagine from E. coli serves to deplete plasma levels of asparagine in leukemic cells by converting L-asparagine to L-aspartic acid and ammonia [A31999], leading to reduced reduced DNA, RNA and protein synthesis; inhibition of cell growth; and ultimately the activation of apoptotic cell-death mechanisms [A31999]. Normal cells, however, are able to synthesize asparagine and thus are affected less by the rapid depletion produced by treatment with the enzyme asparaginase [FDA Label]. other/unknown L-asparagine BE0004798 Human Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Wetzler M, Sanford BL, Kurtzberg J, DeOliveira D, Frankel SR, Powell BL, Kolitz JE, Bloomfield CD, Larson RA: Effective asparagine depletion with pegylated asparaginase results in improved outcomes in adult acute lymphoblastic leukemia: Cancer and Leukemia Group B Study 9511. Blood. 2007 May 15;109(10):4164-7. Epub 2007 Jan 30.Wenner KA, Vieira Pinheiro JP, Escherich G, Wessalowski R, Jorch N, Wolff J, Stehn M, Kohlschutter A, Boos J, Janka-Schaub GE: Asparagine concentration in plasma after 2,500 IU/m(2) PEG-asparaginase i.v. in children with acute lymphoblastic leukemia. Klin Padiatr. 2005 Nov-Dec;217(6):321-6.Appel IM, Pinheiro JP, den Boer ML, Lanvers C, Reniers NC, Boos J, Pieters R: Lack of asparagine depletion in the cerebrospinal fluid after one intravenous dose of PEG-asparaginase: a window study at initial diagnosis of childhood ALL. Leukemia. 2003 Nov;17(11):2254-6. 1713928417016423172642951630741714523472 No studies assessing the mutagenic or carcinogenic potential of _E. coli_ L-asparagine have been conducted. In the Ames assay, no mutagenic effect was demonstrated when tested against Salmonella typhimurium strains [FDA Label]. No studies have been performed on impairment of fertility [FDA Label]. Following a single, intravenous injection of 12,500 to 50,000 International Units L-asparagine/kg in rabbits, edema and necrosis of pancreatic islets were observed. The clinical relevance of this finding is unclear as it does not indicate pancreatitis [FDA Label]. Plasma half life of L-asparagine derived from _E. coli_ following intravenous injection was 8-30 hrs [FDA Label]. Plasma half-life was 34 to 49 hours after intramuscular injection [FDA Label]. Half-life (mean ± SD) of native _E. coli_ asparaginase is approximately 1.28 ± 0.35 days [A31999]. In a study in patients with metastatic cancer and leukemia, daily intravenous administration of L-asparaginase derived from _E. coli_ resulted in a cumulative increase in plasma levels. Following intramuscular injection in patients with metastatic cancer and leukemia, peak plasma levels of asparaginase was achieved 14 to 24 hours post-dosing [FDA Label].Peak asparaginase activity of native _E. coli_ asparaginase can be observed in 24 to 48 hours following administration [A31999]. Apparent volume of distribution was slightly greater than the plasma volume. Asparaginase levels in cerebrospinal fluid were less than 1% of concurrent plasma levels [A31999]. In clinical trials of patients with previously untreated, standard-risk ALL, administration of asparaginase resulted in a decrease of plasma asparagine levels from average of 41 μM to less than 3 μM [FDA Label]. The native asparaginase in whom plasma enzyme activity before treatment was greater than 0.1 International Units/mL [FDA Label]. In this study, cerebrospinal fluid asparagine levels in patients treated with asparaginase decreased from 2.8 μM (pretreatment) to 1.0 μM and 0.3 μM at day 7 and day 28 of induction, respectively [FDA Label]. Native E. coli asparaginase results in asparagine depletion in 14 to 23 days following administration [A31999]. Trastuzumab may increase the cardiotoxic activities of Asparaginase Escherichia coli.The risk or severity of cytotoxicity can be increased when Ancestim is combined with Asparaginase Escherichia coli.The risk or severity of adverse effects can be increased when Paclitaxel is combined with Asparaginase Escherichia coli.The risk or severity of adverse effects can be increased when Docetaxel is combined with Asparaginase Escherichia coli.The risk or severity of adverse effects can be increased when Cabazitaxel is combined with Asparaginase Escherichia coli.Digoxin may decrease the cardiotoxic activities of Asparaginase Escherichia coli.Acetyldigitoxin may decrease the cardiotoxic activities of Asparaginase Escherichia coli.Deslanoside may decrease the cardiotoxic activities of Asparaginase Escherichia coli.Ouabain may decrease the cardiotoxic activities of Asparaginase Escherichia coli.Digitoxin may decrease the cardiotoxic activities of Asparaginase Escherichia coli.Cymarin may decrease the cardiotoxic activities of Asparaginase Escherichia coli.Proscillaridin may decrease the cardiotoxic activities of Asparaginase Escherichia coli.Metildigoxin may decrease the cardiotoxic activities of Asparaginase Escherichia coli.Peruvoside may decrease the cardiotoxic activities of Asparaginase Escherichia coli.Lanatoside C may decrease the cardiotoxic activities of Asparaginase Escherichia coli.Gitoformate may decrease the cardiotoxic activities of Asparaginase Escherichia coli.Acetyldigoxin may decrease the cardiotoxic activities of Asparaginase Escherichia coli.Oleandrin may decrease the cardiotoxic activities of Asparaginase Escherichia coli.Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Asparaginase Escherichia coli.Bevacizumab may increase the cardiotoxic activities of Asparaginase Escherichia coli.Cyclophosphamide may increase the cardiotoxic activities of Asparaginase Escherichia coli.The serum concentration of Dexamethasone can be increased when it is combined with Asparaginase Escherichia coli. DB00072DB09103DB01229DB01248DB06772DB00390DB00511DB01078DB01092DB01396DB13240DB13307DB13401DB13756DB13467DB13537DB13691DB12843DB00076DB00112DB00531DB01234 TrastuzumabAncestimPaclitaxelDocetaxelCabazitaxelDigoxinAcetyldigitoxinDeslanosideOuabainDigitoxinCymarinProscillaridinMetildigoxinPeruvosideLanatoside CGitoformateAcetyldigoxinOleandrinDigoxin Immune Fab (Ovine)BevacizumabCyclophosphamideDexamethasone HydrophobicityIsoelectric PointMolecular WeightMolecular Formula 0.0594.6731731.9C1377H2208N382O442S17 L01XX02 Other antineoplastic agentsOTHER ANTINEOPLASTIC AGENTSANTINEOPLASTIC AGENTSANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L01XXL01XL01L AmidohydrolasesAntineoplastic AgentsAntineoplastic and Immunomodulating AgentsAsparagine-specific EnzymeChemical Actions and UsesEnzymesEnzymes and CoenzymesHydrolasesPharmacologic ActionsTherapeutic Uses D000581D000970D020164D004798D045762D006867D020228D045506 243346507633U00096PA448492P37595AsparaginaseCHEMBL2108989 Drugs Product Database (DPD)PubChem SubstanceGenBankPharmGKBUniProtKBWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic3/asparaginase.htmhttp://www.drugs.com/cdi/asparaginase.html //s3-us-west-2.amazonaws.com/drugbank/fda_labels/DB00023.pdf?1519665697 Roberts J, Prager MD, Bachynsky N: The antitumor activity of Escherichia coli L-asparaginase. Cancer Res. 1966 Oct;26(10):2213-7.Boyse EA, Old LJ, Campbell HA, Mashburn LT: Suppression of murine leukemias by L-asparaginase. Incidence of sensitivity among leukemias of various types: comparative inhibitory activities of guinea pig serum L-asparaginase and Escherichia coli L-asparaginase. J Exp Med. 1967 Jan 1;125(1):17-31.Asselin B, Rizzari C: Asparaginase pharmacokinetics and implications of therapeutic drug monitoring. Leuk Lymphoma. 2015;56(8):2273-80. doi: 10.3109/10428194.2014.1003056. Epub 2015 Mar 11. 5331901533454325586605 approvedinvestigational Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides Asparaginase Escherichia coliAsparaginase Escherichia coliAsparaginase Escherichia coli SpectrilaSpectrilaKidrolase Lundbeck Inc.Merck & Co.Prescript Pharmaceuticals http://www.lundbeckinc.comhttp://www.merck.comhttp://www.prescript.net KidrolaseSpectrilaSpectrila falsefalsefalse Jazz Pharmaceuticals France SasMedac Gesellschaft Fuer Klinische Spezialpraeparate Mb HMedac Gesellschaft Fuer Klinische Spezialpraeparate Mb H falsefalsefalse Intramuscular; IntravenousIntravenousIntravenous Powder, for solutionInjection, powder, for solutionInjection, powder, for solution DPDEMAEMA 10000 unit10000 U10000 U truetruetrue 01926438 CanadaEUEU 1974-12-312016-01-142016-01-14 vial 74.6 USD Elspar 10000 unit vial DB00024 194100-83-9 Thyrotropin Alfa rTSHThyroid stimulating hormoneThyrotrophin-alfaThyrotrophin-alphaThyrotropinThyrotropin-aThyrotropin-alphaThytrophinTSH biotech AVX3D5A4LM 19366632 liquid Thyrotropin alfa is a recombinant form of thyroid stimulating hormone used in performing certain tests in patients who have or have had thyroid cancer. It is also used along with a radioactive agent to destroy remaining thyroid tissue in certain patients who have had their thyroid gland removed because of thyroid cancer. It is a heterodimeric glycoprotein comprised of two non-covalently linked subunits, an alpha subunit of 92 amino acid residues containing two N-linked glycosylation sites and a beta subunit of 112 residues containing one N-linked glycosylation site. The alpha subunit is nearly identical to that of human chorionic gonadotropin (hCG), luteinizing hormone (LH), and follicle-stimulating hormone (FSH). The alpha subunit is thought to be the effector region responsible for stimulation of adenylate cyclase (involved the generation of cAMP). The beta subunit (TSHB) is unique to TSH, and therefore determines its receptor specificity. The amino acid sequence of thyrotropin alfa is identical to that of human pituitary thyroid stimulating hormone. Humans and other mammals Injection, powder, for solutionKitPowder, for solution IntramuscularIntramuscular .9 mg/mL0.9 mg For detection of residueal or recurrent thyroid cancer Thyrotropin Alfa binds to the thyrotropin receptors found on any residual thyroid cells or tissues. This stimulates radioactive iodine uptake for better radiodiagnostic imaging. agonist Thyrotropin receptor BE0000490 Human Szkudlinski MW: Recombinant human thyrotropins of the twenty-first century. Expert Opin Pharmacother. 2004 Dec;5(12):2435-40.Conway GS: Clinical manifestations of genetic defects affecting gonadotrophins and their receptors. Clin Endocrinol (Oxf). 1996 Dec;45(6):657-63.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. 15571461903933011752352 P16473 Thyrotropin receptor 14q31 Human plasma membranereceptor complexintegral component of plasma membranethyroid-stimulating hormone receptor activityG-protein coupled peptide receptor activitythyroid-stimulating hormone signaling pathwaycell-cell signalingactivation of adenylate cyclase activityG-protein coupled receptor signaling pathwaypositive regulation of cell proliferationG-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messengeradenylate cyclase-activating G-protein coupled receptor signaling pathwayhormone-mediated signaling pathway Thyroid-stimulating hormone receptor activity Receptor for thyrothropin. Plays a central role in controlling thyroid cell metabolism. The activity of this receptor is mediated by G proteins which activate adenylate cyclase. Also acts as a receptor for thyrostimulin (GPA2+GPB5). No difference in efficacy and toxicity between adult and geriatric patients. No studies in lactating women, pregnant women and pediatrics. Cautionary administration is advised. 25 ± 10 hours Time to peak: Median: 10 hours (range: 3-24 hours)After a single intramuscular injection of 0.9 mg of thyrotropin alfa: Cmax= 116+38mU/L, Tmax=22+8.5 hours. AUC=5088+1728 mU·hr/L. kidney and liver Binding of thyrotropin alfa to TSH receptors on normal thyroid epithelial cells or on well-differentiated thyroid cancer tissue stimulates iodine uptake and organification. Thyrogen is an exogenous source of human TSH that offers an additional diagnostic tool in the follow-up of patients with a history of well-differentiated thyroid cancer. Melting PointHydrophobicityIsoelectric PointMolecular WeightMolecular Formula 55 °C-0.3307.5022672.9C975H1513N267O304S26 H01AB01V04CJ01 ThyrotropinANTERIOR PITUITARY LOBE HORMONES AND ANALOGUESPITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUESSYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINSTests for thyreoidea functionOTHER DIAGNOSTIC AGENTSDIAGNOSTIC AGENTSVARIOUS H01ABH01AH01HV04CJV04CV04V Amino Acids, Peptides, and ProteinsChemical Actions and UsesDiagnostic AgentsHormonesHormones, Hormone Substitutes, and Hormone AntagonistsPeptide HormonesPeptidesPharmacologic ActionsPhysiological Effects of DrugsPituitary HormonesPituitary Hormones, AnteriorTests for Thyreoidea FunctionThyroid FunctionThyrotropin D000602D020164D006728D006730D036361D010455D020228D045505D010907D010908D013972 1279046505696M16647PA164746560P01225DAP001248Thyrotropin_AlfaCHEMBL1201533 Drugs Product Database (DPD)PubChem SubstanceGenBankPharmGKBUniProtKBTherapeutic Targets DatabaseWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic2/thyrotropin.htmhttp://www.drugs.com/cdi/thyrotropin-alfa.html //s3-us-west-2.amazonaws.com/drugbank/fda_labels/DB00024.pdf?1265922804 approvedvet_approved Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides 5840566 United States 1995-11-24 2015-11-24 false Sanofi aventis us llcGenzyme corp falsefalse Thyrotropin AlfaThyrotropin AlfaThyrotropin Alfa ThyrogenThyrogenThyrogen Genzyme Inc.Organon Pharmaceuticals http://www.genzyme.cahttp://www.organonshop.com ThyrogenThyrogenThyrogen falsefalsefalse Sanofi Genzyme, a Division of Sanofi Aventis Canada IncGenzyme CorporationGenzyme Corporation falsefalsefalse IntramuscularIntramuscular Powder, for solutionInjection, powder, for solutionKit DPDFDA NDCFDA NDC 0.9 mg.9 mg/mL 58468-003058468-1849 NDA020898NDA020898 truetruetrue 02246016 CanadaUSUS 2002-08-121998-11-301998-11-30 vial 1196.4 USD Thyrogen 1.1 mg vial DB00025DB13162DBSALT002413 139076-62-3 Antihemophilic factor, human recombinant Antihemophilic factor (recombinant)Antihemophilic factor recombinantAntihemophilic factor, human recombinantAntihemophilic factor, recombinantFactor VIII (rDNA)Factor VIII (Recombinant)Factor VIII recombinFactor VIII, recombinantHuman Factor VIII (Recombinant)Human factor VIII recombinantOctocog alfarAHFRecombinant antihemophilic factor VIII biotech P89DR4NY54 James W. Bloom, "Warm ethanol method for preparation of low fibrinogen antihemophilic factor." U.S. Patent US4478825, issued June, 1955. solid Human recombinant antihemophilic factor (AHF) or Factor VIII, 2332 residues, glycosylated, produced by CHO cells Humans and other mammals Injection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionPowder, for solutionPowder, for solutionKitKitPowder, for solutionPowder, for solutionPowder, for solutionPowder, for solutionKit; powder, for solutionKit; powder, for solutionKit; powder, for solutionKit; powder, for solutionKit; powder, for solutionKitPowder, for solutionKit IntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenous 1000 IU1500 IU2000 IU250 IU3000 IU500 IU1500 unit3000 unit1000 unit2000 unit250 unit500 unit1000 unit2000 unit250 unit3000 unit500 unit For the treatment of hemophilia A, von Willebrand disease and Factor XIII deficiency. Antihemophilic factor (AHF) is a protein found in normal plasma which is necessary for clot formation. The administration of AHF provides an increase in plasma levels of AHF and can temporarily correct the coagulation defect of patients with hemophilia A (classical hemophilia). activatorcofactorbinderantagonistbinderchaperonechaperonechaperonechaperonemodulatormodulator Coagulation factor XCoagulation factor IXvon Willebrand factorPhytanoyl-CoA dioxygenase, peroxisomalAsialoglycoprotein receptor 278 kDa glucose-regulated proteinCalreticulinCalnexinProtein ERGIC-53Prolow-density lipoprotein receptor-related protein 1Multiple coagulation factor deficiency protein 2 BE0000216BE0000364BE0001043BE0002117BE0002118BE0001098BE0002109BE0001011BE0002119BE0002110BE0002120 HumanHumanHumanHumanHumanHumanHumanHumanHumanHumanHuman BLATRIX C, SOULIER JP: [Preparation of a fraction rich in prothrombin, proconvertin, Stuart factor and antihemophilic factor B (P.P.B. fraction)]. Pathol Biol (Paris). 1959 Dec;7:2477-86.LUNDBLAD RL, DAVIE EW: THE ACTIVATION OF STUART FACTOR (FACTOR X) BY ACTIVATED ANTIHEMOPHILIC FACTOR (ACTIVATED FACTOR 8). Biochemistry. 1965 Jan;4:113-20.Radnoff OD, Saito H: Inhibition of Hageman factor, plasma thromboplastin antecedent, thrombin and other clotting factors by phenylglyoxal hydrate (38500). Proc Soc Exp Biol Med. 1975 Jan;148(1):177-82.Orthner CL: Characterization of proteases in AHF concentrates: effect on factor VIII:von Willebrand protein as assessed by high-pressure gel permeation chromatography. J Lab Clin Med. 1984 Nov;104(5):816-28.Freedman J, Mody M, Lazarus AH, Dewar L, Song S, Blanchette VS, Garvey MB, Ofosu FA: Platelet activation and hypercoagulability following treatment with porcine factor VIII (HYATE:C). Am J Hematol. 2002 Mar;69(3):192-9.Hule V: [Factor IX inhibitor (antihemophilic factor B, PTC) in a woman]. Vnitr Lek. 1975 Mar;21(3):274-7.Yoshitake S, Schach BG, Foster DC, Davie EW, Kurachi K: Nucleotide sequence of the gene for human factor IX (antihemophilic factor B). Biochemistry. 1985 Jul 2;24(14):3736-50.LUNDBLAD RL, DAVIE EW: THE ACTIVATION OF ANTIHEMOPHILIC FACTOR (FACTOR 8) BY ACTIVATED CHRISTMAS FACTOR (ACTIVATED FACTOR9 9). Biochemistry. 1964 Nov;3:1720-5.Hoofnagle JH, Gerety RJ, Thiel J, Barker LF: The prevalence of hepatitis B surface antigen in commercially prepared plasma products. J Lab Clin Med. 1976 Jul;88(1):102-13.Prince AM, Horowitz B, Brotman B, Huima T, Richardson L, van den Ende MC: Inactivation of hepatitis B and Hutchinson strain non-A, non-B hepatitis viruses by exposure to Tween 80 and ether. Vox Sang. 1984;46(1):36-43.Shord SS, Lindley CM: Coagulation products and their uses. Am J Health Syst Pharm. 2000 Aug 1;57(15):1403-17; quiz 1418-20.Lillicrap D, Poon MC, Walker I, Xie F, Schwartz BA: Efficacy and safety of the factor VIII/von Willebrand factor concentrate, haemate-P/humate-P: ristocetin cofactor unit dosing in patients with von Willebrand disease. Thromb Haemost. 2002 Feb;87(2):224-30.Gill JC, Ewenstein BM, Thompson AR, Mueller-Velten G, Schwartz BA: Successful treatment of urgent bleeding in von Willebrand disease with factor VIII/VWF concentrate (Humate-P): use of the ristocetin cofactor assay (VWF:RCo) to measure potency and to guide therapy. Haemophilia. 2003 Nov;9(6):688-95.Smith KJ, Lusher JM, Cohen AR, Salzman P: Initial clinical experience with a new pasteurized monoclonal antibody purified factor VIIIC. Semin Hematol. 1990 Apr;27(2 Suppl 2):25-9.Altieri DC, Capitanio AM, Mannucci PM: von Willebrand factor contaminating porcine factor VIII concentrate (Hyate:C) causes platelet aggregation. Br J Haematol. 1986 Aug;63(4):703-11.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Chen C, Wang Q, Fang X, Xu Q, Chi C, Gu J: Roles of phytanoyl-CoA alpha-hydroxylase in mediating the expression of human coagulation factor VIII. J Biol Chem. 2001 Dec 7;276(49):46340-6.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Bovenschen N, Rijken DC, Havekes LM, van Vlijmen BJ, Mertens K: The B domain of coagulation factor VIII interacts with the asialoglycoprotein receptor. J Thromb Haemost. 2005 Jun;3(6):1257-65.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Kaufman RJ, Pipe SW, Tagliavacca L, Swaroop M, Moussalli M: Biosynthesis, assembly and secretion of coagulation factor VIII. Blood Coagul Fibrinolysis. 1997 Dec;8 Suppl 2:S3-14.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Pipe SW, Morris JA, Shah J, Kaufman RJ: Differential interaction of coagulation factor VIII and factor V with protein chaperones calnexin and calreticulin. J Biol Chem. 1998 Apr 3;273(14):8537-44.Srour MA, Grupp J, Aburubaiha Z, Albert T, Brondke H, Oldenburg J, Schwaab R: Modified expression of coagulation factor VIII by addition of a glycosylation site at the N terminus of the protein. Ann Hematol. 2008 Feb;87(2):107-12. Epub 2007 Sep 26.Kaufman RJ, Pipe SW, Tagliavacca L, Swaroop M, Moussalli M: Biosynthesis, assembly and secretion of coagulation factor VIII. Blood Coagul Fibrinolysis. 1997 Dec;8 Suppl 2:S3-14.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Pipe SW, Morris JA, Shah J, Kaufman RJ: Differential interaction of coagulation factor VIII and factor V with protein chaperones calnexin and calreticulin. J Biol Chem. 1998 Apr 3;273(14):8537-44.Becker S, Simpson JC, Pepperkok R, Heinz S, Herder C, Grez M, Seifried E, Tonn T: Confocal microscopy analysis of native, full length and B-domain deleted coagulation factor VIII trafficking in mammalian cells. Thromb Haemost. 2004 Jul;92(1):23-35.Srour MA, Grupp J, Aburubaiha Z, Albert T, Brondke H, Oldenburg J, Schwaab R: Modified expression of coagulation factor VIII by addition of a glycosylation site at the N terminus of the protein. Ann Hematol. 2008 Feb;87(2):107-12. Epub 2007 Sep 26.Kaufman RJ, Pipe SW, Tagliavacca L, Swaroop M, Moussalli M: Biosynthesis, assembly and secretion of coagulation factor VIII. Blood Coagul Fibrinolysis. 1997 Dec;8 Suppl 2:S3-14.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Cunningham MA, Pipe SW, Zhang B, Hauri HP, Ginsburg D, Kaufman RJ: LMAN1 is a molecular chaperone for the secretion of coagulation factor VIII. J Thromb Haemost. 2003 Nov;1(11):2360-7.Miao HZ, Sirachainan N, Palmer L, Kucab P, Cunningham MA, Kaufman RJ, Pipe SW: Bioengineering of coagulation factor VIII for improved secretion. Blood. 2004 May 1;103(9):3412-9. Epub 2004 Jan 15.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Franchini M, Montagnana M: Low-density lipoprotein receptor-related protein 1: new functions for an old molecule. Clin Chem Lab Med. 2011 Jun;49(6):967-70. doi: 10.1515/CCLM.2011.154. Epub 2011 Mar 11.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Zhang B, Kaufman RJ, Ginsburg D: LMAN1 and MCFD2 form a cargo receptor complex and interact with coagulation factor VIII in the early secretory pathway. J Biol Chem. 2005 Jul 8;280(27):25881-6. Epub 2005 May 10. 138013711428522723656764364161189180611191072994716142406349325296422634109389811185848114750934212885529421721713928417016423115745391713928417016423159462161713928417016423960710817139284170164239525969178990809607108171392841701642395259691521384117899080960710817139284170164231462947014726380171392841701642321391865171392841701642315886209 P00742P00740P04275O14832P07307P11021P27797P27824P49257Q07954Q8NI22 Coagulation factor XCoagulation factor IXvon Willebrand factorPhytanoyl-CoA dioxygenase, peroxisomalAsialoglycoprotein receptor 278 kDa glucose-regulated proteinCalreticulinCalnexinProtein ERGIC-53Prolow-density lipoprotein receptor-related protein 1Multiple coagulation factor deficiency protein 2 13q34Xq27.1-q27.212p13.310pter-p11.217p9q33-q34.119p13.3-p13.25q3518q21.3-q2212q13-q142p21 HumanHumanHumanHumanHumanHumanHumanHumanHumanHumanHuman Golgi lumenextracellular regionintrinsic component of external side of plasma membraneplasma membraneextracellular spaceendoplasmic reticulum lumencalcium ion bindingserine-type endopeptidase activityphospholipid bindingblood coagulationcellular protein metabolic processpost-translational protein modificationproteolysisblood coagulation, intrinsic pathwayblood coagulation, extrinsic pathwaypeptidyl-glutamic acid carboxylationpositive regulation of protein kinase B signalingpositive regulation of cell migrationGolgi lumenextracellular regionplasma membraneextracellular spaceextracellular exosomeendoplasmic reticulum lumencalcium ion bindingendopeptidase activityserine-type endopeptidase activityblood coagulationcellular protein metabolic processpost-translational protein modificationblood coagulation, intrinsic pathwayproteolysisblood coagulation, extrinsic pathwayzymogen activationpeptidyl-glutamic acid carboxylationproteinaceous extracellular matrixexternal side of plasma membraneextracellular matrixplatelet alpha granule lumenextracellular regionendoplasmic reticulumplatelet alpha granuleWeibel-Palade bodyextracellular exosomecollagen bindingidentical protein bindingchaperone bindingglycoprotein bindingintegrin bindingprotein N-terminus bindingimmunoglobulin bindingprotease bindingprotein homodimerization activitycell adhesionhemostasisextracellular matrix organizationblood coagulationplatelet degranulationblood coagulation, intrinsic pathwaycell-substrate adhesionresponse to woundingplatelet activationliver developmentplacenta developmentprotein homooligomerizationmitochondrionperoxisomeperoxisomal matrixcofactor bindingmetal ion bindingL-ascorbic acid bindingphytanoyl-CoA dioxygenase activitymethyl-branched fatty acid metabolic processsmall molecule metabolic processcellular lipid metabolic processfatty acid alpha-oxidationisoprenoid metabolic processintegral component of membranecarbohydrate bindingasialoglycoprotein receptor activityreceptor-mediated endocytosiscell surface receptor signaling pathwaybone mineralizationlipid homeostasisregulation of protein stabilityglycoprotein metabolic processmitochondrionsmooth endoplasmic reticulummembranecell surfacefocal adhesionendoplasmic reticulum-Golgi intermediate compartmentextracellular exosomenucleusmyelin sheathendoplasmic reticulumendoplasmic reticulum lumenmelanosomeplasma membraneendoplasmic reticulum membranemidbodyintegral component of endoplasmic reticulum membraneendoplasmic reticulum chaperone complexprotein domain specific bindingubiquitin protein ligase bindingATP bindingchaperone bindingenzyme bindingribosome bindingcalcium ion bindingmisfolded protein bindingATPase activityglycoprotein bindingunfolded protein bindingnegative regulation of apoptotic processmaintenance of protein localization in endoplasmic reticulumsubstantia nigra developmentregulation of IRE1-mediated unfolded protein responseATF6-mediated unfolded protein responseplatelet degranulationregulation of ATF6-mediated unfolded protein responseregulation of PERK-mediated unfolded protein responseprotein folding in endoplasmic reticulumregulation of protein folding in endoplasmic reticulumplatelet activationtoxin transportblood coagulationcellular response to glucose starvationnegative regulation of protein homodimerization activitynegative regulation of transforming growth factor beta receptor signaling pathwayendoplasmic reticulum unfolded protein responsecellular response to antibioticpositive regulation of transcription from RNA polymerase II promoter in response to endoplasmic reticulum stressPERK-mediated unfolded protein responseIRE1-mediated unfolded protein responsepositive regulation of cell migrationactivation of signaling protein activity involved in unfolded protein responsecellular response to interleukin-4ER-associated ubiquitin-dependent protein catabolic processcellular protein metabolic processcerebellum structural organizationpositive regulation of protein ubiquitinationER overload responsecerebellar Purkinje cell layer developmentperinuclear region of cytoplasmextracellular spaceexternal side of plasma membraneintracellularproteinaceous extracellular matrixendoplasmic reticulum lumencytoplasmmembraneacrosomal vesiclecell surfaceintegral component of lumenal side of endoplasmic reticulum membraneextracellular regionGolgi apparatusendocytic vesicle lumenMHC class I peptide loading complexpolysomesmooth endoplasmic reticulumnucleusfocal adhesionsarcoplasmic reticulum lumencytosolendoplasmic reticulumextracellular exosomeprotein binding involved in protein foldingiron ion bindinghormone bindingchaperone bindingzinc ion bindingpoly(A) RNA bindingcarbohydrate bindingpeptide bindingglycoprotein bindingunfolded protein bindingandrogen receptor bindingcalcium ion bindingubiquitin protein ligase bindingDNA bindingmRNA bindingintegrin bindingcomplement component C1q bindingantigen processing and presentation of peptide antigen via MHC class Ichaperone-mediated protein foldingantigen processing and presentation of exogenous peptide antigen via MHC class IATF6-mediated unfolded protein responsecardiac muscle cell differentiationregulation of transcription, DNA-templatedprotein maturation by protein foldingpositive regulation of phagocytosisprotein foldingprotein folding in endoplasmic reticulumcellular senescenceresponse to testosteronecellular response to lithium ionsequestering of calcium ionglucocorticoid receptor signaling pathwaypositive regulation of cell cyclecell cycle arrestspermatogenesispositive regulation of substrate adhesion-dependent cell spreadingnegative regulation of retinoic acid receptor signaling pathwayprotein localization to nucleusnegative regulation of transcription from RNA polymerase II promoternegative regulation of intracellular steroid hormone receptor signaling pathwaypeptide antigen assembly with MHC class I protein complexreceptor-mediated endocytosispositive regulation of DNA replicationnegative regulation of transcription, DNA-templatedpositive regulation of dendritic cell chemotaxisresponse to estradiolnegative regulation of neuron differentiationprotein export from nucleuscellular protein metabolic processcellular calcium ion homeostasisnegative regulation of translationregulation of apoptotic processregulation of meiotic nuclear divisionpost-translational protein modificationprotein stabilizationprotein N-linked glycosylation via asparagineendoplasmic reticulum unfolded protein responseantigen processing and presentation of exogenous peptide antigen via MHC class I, TAP-dependentpositive regulation of cell proliferationresponse to drugpositive regulation of gene expressioncortical actin cytoskeleton organizationaxonmembraneendoplasmic reticulum lumenrough endoplasmic reticulumprotein complexsmooth endoplasmic reticulumribosomeendoplasmic reticulumdendrite cytoplasmendoplasmic reticulum membraneneuronal cell bodyER-mitochondrion membrane contact sitemelanosomeintegral component of lumenal side of endoplasmic reticulum membraneextracellular exosomedendritic spinemyelin sheathcalcium ion bindingcarbohydrate bindingpoly(A) RNA bindingcellular protein metabolic processpost-translational protein modificationantigen processing and presentation of peptide antigen via MHC class Iprotein N-linked glycosylation via asparaginechaperone-mediated protein foldingantigen processing and presentation of exogenous peptide antigen via MHC class IIprotein foldingprotein folding in endoplasmic reticulumagingprotein secretionsynaptic vesicle endocytosisclathrin-mediated endocytosissarcomeremembraneGolgi membraneendoplasmic reticulum membraneendoplasmic reticulum-Golgi intermediate compartmentintegral component of membraneER to Golgi transport vesicle membraneextracellular exosomehost cell perinuclear region of cytoplasmendoplasmic reticulum-Golgi intermediate compartment membraneunfolded protein bindingmetal ion bindingmannose bindingGolgi organizationblood coagulationCOPII vesicle coatingendoplasmic reticulum organizationprotein transportER to Golgi vesicle-mediated transportpositive regulation of organelle organizationmembrane organizationprotein foldingpost-translational protein modificationprotein N-linked glycosylation via asparaginecellular protein metabolic processfocal adhesioncytoplasmdendriteneuronal cell bodyplasma membraneendosomereceptor complexcoated pitclathrin-coated vesiclenucleolusendocytic vesicle membranelysosomal membraneintegral component of plasma membranereceptor activitycalcium ion bindinglipoprotein particle receptor bindingapolipoprotein bindinglipoprotein transporter activityprotein complex bindingpoly(A) RNA bindingpositive regulation of lipid transportreceptor-mediated endocytosisaorta morphogenesisnegative regulation of Wnt signaling pathwaynegative regulation of neuron projection developmentprotein kinase C-activating G-protein coupled receptor signaling pathwaynegative regulation of smooth muscle cell migrationregulation of cholesterol transportretinoid metabolic processpositive regulation of protein transportphototransduction, visible lightagingnegative regulation of neuron apoptotic processlipoprotein metabolic processcell proliferationbeta-amyloid clearancepositive regulation of cholesterol effluxapoptotic cell clearancenegative regulation of platelet-derived growth factor receptor-beta signaling pathwayregulation of actin cytoskeleton organizationregulation of phospholipase A2 activitylipoprotein transportER to Golgi transport vesicle membraneendoplasmic reticulum membraneendoplasmic reticulum-Golgi intermediate compartment membraneGolgi membranecalcium ion bindingprotein transportcellular protein metabolic processCOPII vesicle coatingER to Golgi vesicle-mediated transportmembrane organizationpost-translational protein modificationprotein N-linked glycosylation via asparagine Serine-type endopeptidase activitySerine-type endopeptidase activityProtein n-terminus bindingPhytanoyl-coa dioxygenase activityCarbohydrate bindingUnfolded protein bindingZinc ion bindingPoly(a) rna bindingUnfolded protein bindingReceptor activityCalcium ion binding Factor Xa is a vitamin K-dependent glycoprotein that converts prothrombin to thrombin in the presence of factor Va, calcium and phospholipid during blood clotting.Factor IX is a vitamin K-dependent plasma protein that participates in the intrinsic pathway of blood coagulation by converting factor X to its active form in the presence of Ca(2+) ions, phospholipids, and factor VIIIa.Important in the maintenance of hemostasis, it promotes adhesion of platelets to the sites of vascular injury by forming a molecular bridge between sub-endothelial collagen matrix and platelet-surface receptor complex GPIb-IX-V. Also acts as a chaperone for coagulation factor VIII, delivering it to the site of injury, stabilizing its heterodimeric structure and protecting it from premature clearance from plasma.Converts phytanoyl-CoA to 2-hydroxyphytanoyl-CoA.Mediates the endocytosis of plasma glycoproteins to which the terminal sialic acid residue on their complex carbohydrate moieties has been removed. The receptor recognizes terminal galactose and N-acetylgalactosamine units. After ligand binding to the receptor, the resulting complex is internalized and transported to a sorting organelle, where receptor and ligand are disassociated. The receptor then returns to the cell membrane surface.Probably plays a role in facilitating the assembly of multimeric protein complexes inside the endoplasmic reticulum. Involved in the correct folding of proteins and degradation of misfolded proteins via its interaction with DNAJC10, probably to facilitate the release of DNAJC10 from its substrate.Calcium-binding chaperone that promotes folding, oligomeric assembly and quality control in the endoplasmic reticulum (ER) via the calreticulin/calnexin cycle. This lectin interacts transiently with almost all of the monoglucosylated glycoproteins that are synthesized in the ER. Interacts with the DNA-binding domain of NR3C1 and mediates its nuclear export. Involved in maternal gene expression regulation. May participate in oocyte maturation via the regulation of calcium homeostasis (By similarity).Calcium-binding protein that interacts with newly synthesized glycoproteins in the endoplasmic reticulum. It may act in assisting protein assembly and/or in the retention within the ER of unassembled protein subunits. It seems to play a major role in the quality control apparatus of the ER by the retention of incorrectly folded proteins. Associated with partial T-cell antigen receptor complexes that escape the ER of immature thymocytes, it may function as a signaling complex regulating thymocyte maturation. Additionally it may play a role in receptor-mediated endocytosis at the synapse.Mannose-specific lectin. May recognize sugar residues of glycoproteins, glycolipids, or glycosylphosphatidyl inositol anchors and may be involved in the sorting or recycling of proteins, lipids, or both. The LMAN1-MCFD2 complex forms a specific cargo receptor for the ER-to-Golgi transport of selected proteins.Endocytic receptor involved in endocytosis and in phagocytosis of apoptotic cells. Required for early embryonic development. Involved in cellular lipid homeostasis. Involved in the plasma clearance of chylomicron remnants and activated LRPAP1 (alpha 2-macroglobulin), as well as the local metabolism of complexes between plasminogen activators and their endogenous inhibitors. May modulate cellular events, such as APP metabolism, kinase-dependent intracellular signaling, neuronal calcium signaling as well as neurotransmission.Functions as a receptor for Pseudomonas aeruginosa exotoxin A.The MCFD2-LMAN1 complex forms a specific cargo receptor for the ER-to-Golgi transport of selected proteins. Plays a role in the secretion of coagulation factors. 8.4-19.3 hrs * 4.1 mL/h•kg [Previously treated pediatric patients] Antihemophilic Factor binds factor IXa along with calcium and phospholipid, This complex converts factor X to factor Xa to facilitate clotting cascade. The risk or severity of hypercoagulability can be increased when Emicizumab is combined with Antihemophilic factor, human recombinant. DB13923 Emicizumab HydrophobicityIsoelectric PointMolecular WeightMolecular Formula -0.5336.97264725.5C11794H18314N3220O3553S83 B02BD02 Blood coagulation factorsVITAMIN K AND OTHER HEMOSTATICSANTIHEMORRHAGICSBLOOD AND BLOOD FORMING ORGANS B02BDB02BB02B Amino Acids, Peptides, and ProteinsBiological FactorsBlood and Blood Forming OrgansBlood Coagulation FactorsBlood ProteinsCarbohydratesDisaccharidesHemostaticsOligosaccharidesPolysaccharidesProteins D000602D001685D001779D001798D002241D004187D006490D009844D011134D011506 7459847127872282646506209M14113PA164750168P00451Antihemophilic_FactorCHEMBL2108175 Drugs Product Database (DPD)Drugs Product Database (DPD)Drugs Product Database (DPD)Drugs Product Database (DPD)PubChem SubstanceGenBankPharmGKBUniProtKBWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic2/hemofilm.htmhttp://www.drugs.com/cdi/antihemophilic-factor-human.html Titheradge MA, Coore HG: Initial rates of pyruvate transport in mitochondria determined by an "inhibitor-stop" technique. Biochem J. 1975 Sep;150(3):553-6. 2157 approvedinvestigational BioclateHelixateHyate:CKoate-HPKogenateMonarc-MReFacto Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides 21246901339477 CanadaCanada 2007-09-111997-09-23 2013-10-012014-09-23 falsefalse Antihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinant + Von Willebrand Factor HumanAntihemophilic factor, human recombinant + Von Willebrand Factor HumanAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinantAntihemophilic factor, human recombinant AdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateWilate - von Willebrand Factor/Coagulation Factor VIII Complex (Human)Wilate - von Willebrand Factor/Coagulation Factor VIII Complex (Human)XynthaXynthaXynthaXynthaXynthaXynthaXynthaXynthaXynthaNuwiqNuwiqNuwiqNuwiqNuwiqNuwiqNuwiqHelixate FSHelixate FSHelixate FSAdvateHelixate FSAdvateAdvateRecombinate Pws Inj 250I.U./vialRecombinate Pws Inj 1000I.U./vialRecombinate Pws Inj 500I.U./vialKogenate Pws 250iu/vialKogenate Pws 500iu/vialKogenate Pws 1000iu/vialKogenate - Pws IV 250I.U./vialKogenate - Pws IV 500I.U./vialKogenate - Pws IV 1000I.U./vialKogenate FSKogenate FSKogenate FSAdvateAdvateKogenate FS -(with Bio-set)Helixate FSAdvateAdvateAdvateAdvateAdvateKogenate FSKogenate FSKogenate FSKovaltryKovaltryKovaltryKovaltryKovaltryKogenate FS -(with Bio-set)Kogenate FSKogenate FSKogenate FSKogenate FSKogenate FSAntiveninKogenate FSKogenate FSKogenate FSKogenate FSKogenate FSKogenate FSKogenate FSKogenate FSKogenate FSKogenate FSHelixate FSHelixate FSHelixate FSHelixate FSHelixate FSNovoeightNovoeightNovoeightNovoeightNovoeightNovoeightRecombinateRecombinateRecombinateRecombinateRecombinateRecombinateRecombinateRecombinateAdvateAdvateAdvateAdvateKovaltryKovaltryKovaltryKovaltryKovaltryKovaltryKovaltryKovaltryKovaltryKovaltryAdynovateAdynovateAdynovateAdynovateAdynovateEloctateEloctateEloctateAdynovateAdynovateAdynovateAdynovateAdynovateAdynovateAdynovateAdynovateAdvateAdvateAdvateAdvateAdvateAdvateAdvate Baxter International Inc.Bayer HealthcareCSL Behring LLCGlaxoSmithKline Inc.Grifols SAIpsen Pharmaceuticals Inc.Octapharma USATalecris BiotherapeuticsWyeth Pharmaceuticals http://www.baxter.comhttp://www.bayerhealthcare.comhttp://www.cslbehring.comhttp://www.gsk.comhttp://www.grifols.comhttp://www.ipsen.comhttp://www.octapharma.comhttp://www.talecris.comhttp://www.wyeth.com AdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdvateAdynovateAdynovateAdynovateAdynovateAdynovateAdynovateAdynovateAdynovateAdynovateAdynovateAdynovateAdynovateAdynovateAntiveninEloctateEloctateEloctateHelixate FSHelixate FSHelixate FSHelixate FSHelixate FSHelixate FSHelixate FSHelixate FSHelixate FSHelixate FSKogenate - Pws IV 1000I.U./vialKogenate - Pws IV 250I.U./vialKogenate - Pws IV 500I.U./vialKogenate FSKogenate FSKogenate FSKogenate FSKogenate FSKogenate FSKogenate FSKogenate FSKogenate FSKogenate FSKogenate FSKogenate FSKogenate FSKogenate FSKogenate FSKogenate 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AgBaxalta Canada CorporationBaxter AgBaxter AgBaxalta Canada CorporationBaxter AgBaxalta Canada CorporationBaxter AgBaxter AgBaxter AgBaxter AgBaxter AgBaxter AgBaxter AgBaxter AgBaxter LaboratoriesBaxter LaboratoriesBaxalta Canada CorporationBaxalta Canada CorporationBaxalta Canada CorporationBaxalta Canada CorporationBaxalta Canada CorporationBaxter LaboratoriesBaxter LaboratoriesBaxter LaboratoriesBaxter LaboratoriesBaxalta Canada CorporationBaxalta Canada CorporationBaxalta Canada CorporationBaxalta Canada CorporationBaxalta Canada CorporationBaxalta Canada CorporationBaxalta Canada CorporationBaxalta Canada CorporationBaxalta Canada CorporationBaxalta Canada CorporationBaxalta Canada CorporationBaxalta Canada CorporationBaxalta Canada CorporationMerck Sharp & Dohme LimitedBiogenBiogenBiogenCsl BehringCsl BehringCsl BehringCsl BehringCsl BehringBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerMiles Inc. Pharmaceutical DivisionMiles Inc. Pharmaceutical DivisionMiles Inc. Pharmaceutical DivisionBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerBayerNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskOctapharmaOctapharmaOctapharmaOctapharmaOctapharmaOctapharmaOctapharmaBaxter LaboratoriesBaxter LaboratoriesBaxter LaboratoriesBaxalta Canada CorporationBaxalta Canada CorporationBaxalta Canada CorporationBaxalta Canada CorporationBaxalta Canada CorporationBaxter LaboratoriesBaxter LaboratoriesBaxter LaboratoriesOctapharmaOctapharma Pharmazeutika Produktionsgesellschaft M.B.H.Wyeth Bio Pharma Division Of Wyeth Pharmaceuticals Inc., A Subsidiary Of Pfizer Inc.Wyeth Bio Pharma Division Of Wyeth Pharmaceuticals Inc., A Subsidiary Of Pfizer Inc.Wyeth Bio Pharma Division Of Wyeth Pharmaceuticals Inc., A Subsidiary Of Pfizer Inc.Wyeth Bio Pharma Division Of Wyeth Pharmaceuticals Inc., A Subsidiary Of Pfizer Inc.Wyeth Bio Pharma Division Of Wyeth Pharmaceuticals Inc., A Subsidiary Of Pfizer Inc.Wyeth Bio Pharma Division Of Wyeth Pharmaceuticals Inc., A Subsidiary Of Pfizer Inc.Wyeth Bio Pharma Division Of Wyeth Pharmaceuticals Inc., A Subsidiary Of Pfizer Inc.Wyeth Bio Pharma Division Of Wyeth Pharmaceuticals Inc., A Subsidiary Of Pfizer Inc.Wyeth Bio Pharma Division Of Wyeth Pharmaceuticals Inc., A Subsidiary Of Pfizer Inc. 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powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionPowder, for solutionInjection, powder, for solutionInjection, powder, for solutionPowder, for solutionInjection, powder, for solutionPowder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionInjection, powder, for solutionPowder, for solutionPowder, for solutionPowder, for solutionPowder, for solutionPowder, for solutionPowder, for solutionPowder, for solutionKitKitKitKitKitKitKitKitKitKitKitKitKitKitKitKitKitKitKitKitKitKitKitKitKitKitPowder, for solutionPowder, for solutionPowder, for solutionPowder, for solutionPowder, for solutionPowder, for solutionPowder, for solutionPowder, for solutionPowder, for solutionPowder, for 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600 unit kitKoate-dvi 1000 unit kitKoate-dvi 250 unit kitKoate-dvi 500 unit kitRefacto 1000 unit vialRefacto 2000 unit vialRefacto 250 unit vialRefacto 500 unit vialHemofil m 1701-2000 unit vialHemofil m 220-400 unit vialHemofil m 401-800 unit vialHemofil m 801-1700 unit vialWilate 450-450 unit kitWilate 900-900 unit kitHelixate fs 1000 unit vialHelixate fs 250 unit vialHelixate fs 3000 unit vialHelixate fs 500 unit vialXyntha 1000 unit kitXyntha 2000 unit kitXyntha 250 unit kitXyntha 500 unit kitAdvate 1201-1800 unit vialAdvate 1801-2400 unit vialAdvate 200-400 unit vialAdvate 2400-3600 unit vialAdvate 401-800 unit vialAdvate 801-1200 unit vialKogenate fs 1000 unit vialKogenate fs 250 unit vialKogenate fs 3000 unit vialKogenate fs 500 unit vial DB00026 143090-92-0 Anakinra ICIL-1RAIL-1raIL-1RNIL1 inhibitorInterleukin-1 receptor antagonist protein precursorIRAP biotech 9013DUQ28K liquid Anakinra is a recombinant, nonglycosylated human interleukin-1 receptor antagonist (IL-1Ra). The difference between anakinra and the native human IL-1Ra is that anakinra has an extra methionine residue at the amino terminus. It is manufactured by using the E. coli expression system. Anakinra is composed of 153 amino acid residues. FDA approved on November 14, 2001. Humans and other mammals Injection, solutionInjection, solutionInjection, solutionSolution SubcutaneousSubcutaneousSubcutaneousSubcutaneous 100 mg100 mg/0.67ml100 mg/.67mL150 mg For the treatment of adult rheumatoid arthritis and treatment of Neonatal-Onset Multisystem Inflammatory Disease (NOMID). Anakinra binds competitively to the Interleukin-1 type I receptor (IL-1RI), thereby inhibiting the action of elevated levels IL-1 which normally can lead to cartilage degradation and bone resorption. antagonist Interleukin-1 receptor type 1 BE0000565 Human Tang YH, Zhang SP, Liang Y, Deng CQ: [Effects of Panax notoginseng saponins on mRNA expressions of interleukin-1 beta, its correlative factors and cysteinyl-aspartate specific protease after cerebral ischemia-reperfusion in rats]. Zhong Xi Yi Jie He Xue Bao. 2007 May;5(3):328-32.Dayer JM: The pivotal role of interleukin-1 in the clinical manifestations of rheumatoid arthritis. Rheumatology (Oxford). 2003 May;42 Suppl 2:ii3-10.Vamvakopoulos J, Green C, Metcalfe S: Genetic control of IL-1beta bioactivity through differential regulation of the IL-1 receptor antagonist. Eur J Immunol. 2002 Oct;32(10):2988-96.Do H, Vasilescu A, Carpentier W, Meyer L, Diop G, Hirtzig T, Coulonges C, Labib T, Spadoni JL, Therwath A, Lathrop M, Matsuda F, Zagury JF: Exhaustive genotyping of the interleukin-1 family genes and associations with AIDS progression in a French cohort. J Infect Dis. 2006 Dec 1;194(11):1492-504. Epub 2006 Oct 26.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.So A, De Smedt T, Revaz S, Tschopp J: A pilot study of IL-1 inhibition by anakinra in acute gout. Arthritis Res Ther. 2007;9(2):R28.Vannier E, Kaser A, Atkins MB, Fantuzzi G, Dinarello CA, Mier JW, Tilg H: Elevated circulating levels of soluble interleukin-1 receptor type II during interleukin-2 immunotherapy. Eur Cytokine Netw. 1999 Mar;10(1):37-42. 17498496128170891235545317083033117523521735282810210771 P14778 Interleukin-1 receptor type 1 2q12 Human membraneintegral component of plasma membraneprotein complexnucleuspostsynaptic densityplasma membraneextracellular spaceaxoncell surfacesignal transducer activityplatelet-derived growth factor receptor bindingtransmembrane signaling receptor activityinterleukin-1, Type I, activating receptor activityinterleukin-1 receptor activityresponse to epidermal growth factorinterleukin-1-mediated signaling pathwaycell surface receptor signaling pathwayresponse to nitric oxideregulation of inflammatory responseheat acclimationresponse to transforming growth factor betaimmune responseresponse to interleukin-1ovulationresponse to radiationcellular response to glucose stimulus Transmembrane signaling receptor activity Receptor for IL1A, IL1B and IL1RN. After binding to interleukin-1 associates with the corecptor IL1RAP to form the high affinity interleukin-1 receptor complex which mediates interleukin-1-dependent activation of NF-kappa-B, MAPK and other pathways. Signaling involves the recruitment of adapter molecules such as TOLLIP, MYD88, and IRAK1 or IRAK2 via the respective TIR domains of the receptor/coreceptor subunits. Binds ligands with comparable affinity and binding of antagonist IL1RN prevents association with IL1RAP to form a signaling complex. Most common adverse reactions (incidence ≥ 5%) are injection site reaction, worsening of rheumatoid arthritis, upper respiratory tract infection, headache, nausea, diarrhea, sinusitis, arthralgia, flu like-symptoms, and abdominal pain when anakinra is used in RA patients. In NOMID patients, the most common AEs during the first 6 months of treatment (incidence >10%) are injection site reaction, headache, vomiting, arthralgia, pyrexia, and nasopharyngitis. Healthy subjects = 4 - 6 hours;NOMID patients = 5.7 hours (range of 3.1 - 28.2 hours). When a 70 mg subcutaneous bolus injection is given to healthy subjects, the absolute bioavailability is 95%. Accumulation does not occur following daily subcutaneous doses. Tmax, SubQ, 1-2 mg/kg, healthy subjects = 3-7 hours;Cmax, SubQ, 3 mg/kg once daily, NOMID patients = 3628 ng/mL. Clearance is variable and increases with increasing creatinine clearance and body weight. However, gender and age were not significant factors. Used to treat rheumatoid arthritis, Anakinra blocks the biologic activity of IL-1 by competitively inhibiting IL-1 binding to the interleukin-1 type I receptor (IL-1RI), which is expressed in a wide variety of tissues and organs. IL-1 production is induced in response to inflammatory stimuli and mediates various physiologic responses including inflammatory and immunological responses. Patients with rheumatoid arthritis have elevated levels of IL-1. The levels of the naturally occurring IL-1Ra in synovium and synovial fluid from rheumatoid arthritis (RA) patients are not sufficient to compete with the elevated amount of locally produced IL-1. Increasing the levels of IL-1Ra by artificial means reduces the negative effects (cartilage degradation, bone resorption) of IL-1. Sarilumab may increase the immunosuppressive activities of Anakinra.The risk or severity of adverse effects can be increased when Anakinra is combined with Leflunomide.Anakinra may increase the immunosuppressive activities of Fingolimod.Roflumilast may increase the immunosuppressive activities of Anakinra.Ocrelizumab may increase the immunosuppressive activities of Anakinra.The therapeutic efficacy of Varicella Zoster Vaccine (Live/Attenuated) can be decreased when used in combination with Anakinra.The therapeutic efficacy of Yellow Fever Vaccine can be decreased when used in combination with Anakinra.The therapeutic efficacy of Clostridium tetani toxoid antigen (formaldehyde inactivated) can be decreased when used in combination with Anakinra.The therapeutic efficacy of Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated) can be decreased when used in combination with Anakinra.The therapeutic efficacy of Rotavirus Vaccine can be decreased when used in combination with Anakinra.The therapeutic efficacy of G17DT can be decreased when used in combination with Anakinra.The therapeutic efficacy of INGN 201 can be decreased when used in combination with Anakinra.The therapeutic efficacy of INGN 225 can be decreased when used in combination with Anakinra.The therapeutic efficacy of Rindopepimut can be decreased when used in combination with Anakinra.The therapeutic efficacy of SRP 299 can be decreased when used in combination with Anakinra.The therapeutic efficacy of GI-5005 can be decreased when used in combination with Anakinra.The therapeutic efficacy of TG4010 can be decreased when used in combination with Anakinra.The therapeutic efficacy of Rabies virus inactivated antigen, A can be decreased when used in combination with Anakinra.The therapeutic efficacy of Tecemotide can be decreased when used in combination with Anakinra.The therapeutic efficacy of Rubella virus vaccine can be decreased when used in combination with Anakinra.The therapeutic efficacy of Anthrax immune globulin human can be decreased when used in combination with Anakinra.The therapeutic efficacy of Bacillus calmette-guerin substrain tice live antigen can be decreased when used in combination with Anakinra.The therapeutic efficacy of Japanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated) can be decreased when used in combination with Anakinra.The therapeutic efficacy of Salmonella typhi ty2 vi polysaccharide antigen can be decreased when used in combination with Anakinra.The therapeutic efficacy of Bacillus calmette-guerin substrain connaught live antigen can be decreased when used in combination with Anakinra.The therapeutic efficacy of Hepatitis A Vaccine can be decreased when used in combination with Anakinra.The therapeutic efficacy of Salmonella typhi ty21a live antigen can be decreased when used in combination with Anakinra.The therapeutic efficacy of Human rabies virus immune globulin can be decreased when used in combination with Anakinra.The therapeutic efficacy of Hepatitis B Vaccine (Recombinant) can be decreased when used in combination with Anakinra.The risk or severity of adverse effects can be increased when Denosumab is combined with Anakinra.The therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Anakinra.Trastuzumab may increase the neutropenic activities of Anakinra.The risk or severity of adverse effects can be increased when Afelimomab is combined with Anakinra.The risk or severity of adverse effects can be increased when Pirfenidone is combined with Anakinra.The risk or severity of adverse effects can be increased when Etanercept is combined with Anakinra.The risk or severity of adverse effects can be increased when Adalimumab is combined with Anakinra.The risk or severity of adverse effects can be increased when Golimumab is combined with Anakinra.The risk or severity of adverse effects can be increased when Certolizumab pegol is combined with Anakinra.The risk or severity of adverse effects can be increased when Anakinra is combined with Natalizumab.The risk or severity of adverse effects can be increased when Anakinra is combined with Infliximab.The risk or severity of adverse effects can be increased when Pimecrolimus is combined with Anakinra.Tacrolimus may increase the immunosuppressive activities of Anakinra.The risk or severity of adverse effects can be increased when Anakinra is combined with Abatacept.The risk or severity of infection can be increased when Anakinra is combined with Canakinumab.The risk or severity of adverse effects can be increased when Anakinra is combined with Tofacitinib.The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Anakinra.The risk or severity of adverse effects can be increased when Anakinra is combined with Rabies virus inactivated antigen, A.The risk or severity of adverse effects can be increased when Anakinra is combined with Rituximab.The risk or severity of adverse effects can be increased when Anakinra is combined with Tocilizumab. DB11767DB01097DB08868DB01656DB11988DB10318DB10805DB10583DB10584DB10276DB04914DB05322DB05325DB05374DB05440DB05942DB06584DB10283DB12568DB10317DB09057DB10343DB10769DB10803DB10804DB10989DB11050DB11603DB11627DB06643DB06688DB00072DB04956DB04951DB00005DB00051DB06674DB08904DB00108DB00065DB00337DB00864DB01281DB06168DB08895DB12768DB10283DB00073DB06273 SarilumabLeflunomideFingolimodRoflumilastOcrelizumabVaricella Zoster Vaccine (Live/Attenuated)Yellow Fever VaccineClostridium tetani toxoid antigen (formaldehyde inactivated)Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated)Rotavirus VaccineG17DTINGN 201INGN 225RindopepimutSRP 299GI-5005TG4010Rabies virus inactivated antigen, ATecemotideRubella virus vaccineAnthrax immune globulin humanBacillus calmette-guerin substrain tice live antigenJapanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated)Salmonella typhi ty2 vi polysaccharide antigenBacillus calmette-guerin substrain connaught live antigenHepatitis A VaccineSalmonella typhi ty21a live antigenHuman rabies virus immune globulinHepatitis B Vaccine (Recombinant)DenosumabSipuleucel-TTrastuzumabAfelimomabPirfenidoneEtanerceptAdalimumabGolimumabCertolizumab pegolNatalizumabInfliximabPimecrolimusTacrolimusAbataceptCanakinumabTofacitinibBCG vaccineRabies virus inactivated antigen, ARituximabTocilizumab HydrophobicityIsoelectric PointMolecular WeightMolecular Formula -0.4125.4617257.6C759H1186N208O232S10 L04AC03 Interleukin inhibitorsIMMUNOSUPPRESSANTSIMMUNOSUPPRESSANTSANTINEOPLASTIC AND IMMUNOMODULATING AGENTS L04ACL04AL04L Amino Acids, Peptides, and ProteinsAntineoplastic and Immunomodulating AgentsAntirheumatic AgentsBiological FactorsBiologics for Rheumatoid Arthritis TreatmentChemical Actions and UsesCytokinesDisease-modifying Antirheumatic AgentsImmunosuppressive AgentsIntercellular Signaling Peptides and ProteinsInterleukin InhibitorsInterleukin-1 Receptor AntagonistPeptidesPharmacologic ActionsProteinsTherapeutic Uses D000602D018501D001685D020164D016207D007166D036341D010455D020228D011506D045506 1260446507944D02934M55646PA10799P18510DAP000095AnakinraCHEMBL1201570 Drugs Product Database (DPD)PubChem SubstanceKEGG DrugGenBankPharmGKBUniProtKBTherapeutic Targets DatabaseWikipediaChEMBL RxListDrugs.com http://www.rxlist.com/cgi/generic/anakinra.htmhttp://www.drugs.com/cdi/anakinra.html //s3-us-west-2.amazonaws.com/drugbank/fda_labels/DB00026.pdf?1265922808 Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.Lequerre T, Quartier P, Rosellini D, Alaoui F, De Bandt M, Mejjad O, Kone-Paut I, Michel M, Dernis E, Khellaf M, Limal N, Job-Deslandre C, Fautrel B, Le Loet X, Sibilia J: Interleukin-1 receptor antagonist (anakinra) treatment in patients with systemic-onset juvenile idiopathic arthritis or adult onset Still disease: preliminary experience in France. Ann Rheum Dis. 2008 Mar;67(3):302-8. Epub 2007 Oct 18. 1175235217947302 approved Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides 21419531341322 CanadaCanada 2008-04-082001-11-27 2013-09-172018-11-27 falsefalse AnakinraAnakinraAnakinraAnakinraAnakinraAnakinraAnakinraAnakinra KineretKineretKineretKineretKineretKineretKineretKineret Amgen Inc.BioVitrum AB http://www.amgen.comhttp://www.biovitrum.com KineretKineretKineretKineretKineretKineretKineretKineret falsefalsefalsefalsefalsefalsefalsefalse SWEDISH ORPHAN BIOVITRUM AB (PUBL)SWEDISH ORPHAN BIOVITRUM AB (PUBL)SWEDISH ORPHAN BIOVITRUM AB (PUBL)SWEDISH ORPHAN BIOVITRUM AB (PUBL)SWEDISH ORPHAN BIOVITRUM AB (PUBL)SWEDISH ORPHAN BIOVITRUM AB (PUBL)SWEDISH ORPHAN BIOVITRUM AB (PUBL)SWEDISH ORPHAN BIOVITRUM AB (PUBL) falsefalsefalsefalsefalsefalsefalsefalse SubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneous SolutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solution DPDEMAEMAEMAEMAEMAEMAFDA NDC 150 mg100 mg100 mg100 mg100 mg/0.67ml100 mg/0.67ml100 mg/0.67ml100 mg/.67mL 66658-234 BLA103950 truetruetruetruetruetruetruetrue 02245913 CanadaEUEUEUEUEUEUUS 2002-05-292002-03-082002-03-082002-03-082002-03-082002-03-082002-03-082009-12-15 syringebox 61.8449.9 USDUSD Kineret 100 mg/0.67 ml syrKineret 1 Box = 7 Syringes, 4.69ml Box !Bg|w_Ta}SuIH@gzMww~`IbSmwuH__zizpw@h`Bk}H`k^}lBw~`O]bGk}H@c_|R@K~`C_}erO~`Ha}cyJaOr~JbHK~os]}hB_AVR[|x\XDzizpw@`V_AQ|Aot`Bm{w~`C]}YAnpK_z@MpK~_tc|mpK~`C]}M{w~`La}_h@w_TRL[OLhbBmww~`E~YuCoKnq`S_k~gKC\By^}eGwzb@Jwo_z@M{uTn{BmhCW@ozROpw@d`Bh@wS]}hBOTcDS}Hw__z@WyeTn|n{k~gkC_|Y^e{s]}@XBw_UR{mpK~oz@Mwtw_S\BL[|w@c]}WygTn{MGMpKe{~WouKl =v;SyzvyvyEhSvyvnCjQxUiroKzIleCbnaN4zpj4TUqU31m_Bpqf4l_4jh058XG8FJ1R118V4cN4e0KV DB00027 1405-97-6 Gramicidin D Bacillus brevis gramicidin DGramicidinGramicidin AGramicidin BGramicidin CGramicidine small molecule 5IE62321P4 1811.253 U.S.Patent 2,534,541. //s3-us-west-2.amazonaws.com/drugbank/msds/DB00027.pdf?1265922740 liquid Gramcidin D is a heterogeneous mixture of three antibiotic compounds, gramicidins A, B and C, making up 80%, 6%, and 14% respectively all of which are obtained from the soil bacterial species Bacillus brevis and called collectively gramicidin D. Gramcidins are 15 residue peptides with alternating D and L amino acids. The peptides assemble inside of the hydrophobic interior of the cellular lipid bilayer to form a β-helix. The helix itself is not long enough to span the membrane but it dimerizes to form the elongated channel needed to span the whole membrane. Gramicidin D is used primarily as a topical antibiotic and is one of the three constituents of consumer antibiotic polysporin ophthalmic solution. Pseudomonas aeruginosaStreptococcus pneumoniaeStreptococcus agalactiaeNeisseria meningitidisHaemophilus influenzaeNeisseria gonorrhoeaeEscherichia coliStaphylococcus aureusKlebsiellaEnterobacter Solution / dropsSolution / dropsSolutionSolutionLiquidLiquidOintmentSolution / dropsSolution / dropsSprayCreamOintment Auricular (otic)OphthalmicOphthalmicAuricular (otic); OphthalmicOphthalmicAuricular (otic); OphthalmicAuricular (otic); OphthalmicAuricular (otic); OphthalmicTopicalNasalTopicalTopical For treatment of skin lesions, surface wounds and eye infections. Gramicidin D binds to and inserts itself into bacterial membranes (with a strong preference to gram-positive cell membranes). This results in membrane disruption and permeabilization (it acts as a channel). This leads to (i) loss of intracellular solutes (e.g., K+ and amino acids); (ii) dissipation of the transmembrane potential; (iii) inhibition of respiration; (iv) a reduction in ATP pools; and (v) inhibition of DNA, RNA, and protein synthesis, which leads to cell death. Gramicidin is particularly effective against gram-positive bacteria. Because the drug is highly hemolytic, it cannot be administered internally and so is used only on the skin as a lotion or ointment. It is used primarily in the treatment of infected surface wounds, and in eye, nose, and throat infections. It is normally given with two other antibiotics (neomycin and polymixin B) as an ophthalmic solution. The serum concentration of Doxorubicin can be increased when it is combined with Gramicidin D.The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Gramicidin D.The serum concentration of Everolimus can be increased when it is combined with Gramicidin D.The serum concentration of Afatinib can be increased when it is combined with Gramicidin D.The serum concentration of Colchicine can be increased when it is combined with Gramicidin D.The serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Gramicidin D.The serum concentration of Ledipasvir can be increased when it is combined with Gramicidin D.The serum concentration of Naloxegol can be increased when it is combined with Gramicidin D.The serum concentration of Prucalopride can be increased when it is combined with Gramicidin D.The serum concentration of Ranolazine can be increased when it is combined with Gramicidin D.The serum concentration of Rifaximin can be increased when it is combined with Gramicidin D.The excretion of Vincristine can be decreased when combined with Gramicidin D.The serum concentration of Brentuximab vedotin can be increased when it is combined with Gramicidin D.The serum concentration of Pazopanib can be increased when it is combined with Gramicidin D.The serum concentration of Silodosin can be increased when it is combined with Gramicidin D.The serum concentration of Topotecan can be increased when it is combined with Gramicidin D.The serum concentration of Bosutinib can be increased when it is combined with Gramicidin D.The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Gramicidin D.The serum concentration of Edoxaban can be increased when it is combined with Gramicidin D. DB00997DB09268DB01590DB08916DB01394DB06695DB09027DB09049DB06480DB00243DB01220DB00541DB08870DB06589DB06207DB01030DB06616DB12768DB09075 DoxorubicinPicosulfuric acidEverolimusAfatinibColchicineDabigatran etexilateLedipasvirNaloxegolPrucaloprideRanolazineRifaximinVincristineBrentuximab vedotinPazopanibSilodosinTopotecanBosutinibBCG vaccineEdoxaban Melting Point 229 °C R02AB30 AntibioticsTHROAT PREPARATIONSTHROAT PREPARATIONSRESPIRATORY SYSTEM R02ABR02AR02R Amino Acids, Peptides, and ProteinsAnti-Bacterial AgentsAnti-Infective AgentsAnti-Infective Agents, LocalChemical Actions and UsesMacrocyclic CompoundsMembrane ProteinsP-glycoprotein/ABCB1 InhibitorsPeptidesPeptides, CyclicPharmacologic ActionsPolycyclic CompoundsPore Forming Cytotoxic ProteinsProteinsRespiratory SystemTherapeutic UsesThroat PreparationsTyrothricin D000602D000900D000890D000891D020164D047028D008565D010455D010456D020228D011083D052899D011506D012137D045506D014449 85234526710346507412D0436924623445PA449808DAP001327Gramicidin_DCHEMBL557217 Drugs Product Database (DPD)PubChem CompoundPubChem SubstanceKEGG DrugChemSpiderPharmGKBTherapeutic Targets DatabaseWikipediaChEMBL Ketchem RR, Lee KC, Huo S, Cross TA: Macromolecular structural elucidation with solid-state NMR-derived orientational constraints. J Biomol NMR. 1996 Jul;8(1):1-14.Townsley LE, Tucker WA, Sham S, Hinton JF: Structures of gramicidins A, B, and C incorporated into sodium dodecyl sulfate micelles. Biochemistry. 2001 Oct 2;40(39):11676-86.Burkhart BM, Gassman RM, Langs DA, Pangborn WA, Duax WL, Pletnev V: Gramicidin D conformation, dynamics and membrane ion transport. Biopolymers. 1999;51(2):129-44. 88105221157086810397797 approved Sanofi Sofradex Organic compounds Organic Polymers Polypeptides This compound belongs to the class of organic compounds known as polypeptides. These are peptides containing ten or more amino acid residues. Polypeptides 3-alkylindolesAlanine and derivativesAlpha amino acid amidesAzacyclic compoundsBenzenoidsCarbonyl compoundsHeteroaromatic compoundsHydrocarbon derivativesLeucine and derivativesN-acyl aminesN-acyl-alpha amino acids and derivativesN-acylethanolaminesN-formyl-alpha amino acidsOrganic oxidesPeptidesPrimary alcoholsSecondary carboxylic acid amidesSubstituted pyrrolesTryptamines and derivativesValine and derivatives 3-alkylindoleAlanine or derivativesAlcoholAlkanolamineAlpha peptideAlpha-amino acid amideAlpha-amino acid or derivativesAromatic heteropolycyclic compoundAzacycleBenzenoidCarbonyl groupCarboxamide groupCarboxylic acid derivativeFatty acylFatty amideHeteroaromatic compoundHydrocarbon derivativeIndoleIndole or derivativesLeucine or derivativesN-acyl-alpha amino acid or derivativesN-acyl-amineN-acylethanolamineN-formyl-alpha amino acid or derivativesN-formyl-alpha-amino acidN-substituted-alpha-amino acidOrganic nitrogen compoundOrganic oxideOrganic oxygen compoundOrganoheterocyclic compoundOrganonitrogen compoundOrganooxygen compoundPolypeptidePrimary alcoholPyrroleSecondary carboxylic acid amideSubstituted pyrroleTriptanValine or derivatives Gramicidin D + Neomycin + Polymyxin B SulfateGramicidin D + Neomycin + Polymyxin B SulfateGramicidin D + Neomycin + Polymyxin B SulfateGramicidin D + Neomycin + Nystatin + TriamcinoloneDexamethasone + Framycetin + Gramicidin DFramycetin + Gramicidin D + PhenylephrineGramicidin D + Polymyxin B SulfateGramicidin D + Polymyxin B SulfateGramicidin D + Polymyxin B SulfateGramicidin D + Lidocaine + Polymyxin B SulfateGramicidin D + Lidocaine + Polymyxin B SulfateGramicidin D + Polymyxin B SulfateGramicidin D + Lidocaine + Polymyxin B SulfateGramicidin D + Polymyxin B SulfateGramicidin D + Lidocaine + Polymyxin B SulfateGramicidin D + Polymyxin B SulfateGramicidin D + Lidocaine + Polymyxin B SulfateGramicidin D + Lidocaine + Polymyxin B SulfateGramicidin D + Neomycin + Nystatin + TriamcinoloneGramicidin D + Neomycin + Nystatin + TriamcinoloneGramicidin D + Polymyxin B SulfateGramicidin D + Polymyxin B SulfateGramicidin D + Lidocaine + Polymyxin B SulfateGramicidin D + Lidocaine + Polymyxin B SulfateGramicidin D + Neomycin + Nystatin + TriamcinoloneDexamethasone + Framycetin + Gramicidin DFramycetin + Gramicidin D + PhenylephrineGramicidin D + Neomycin + Nystatin + TriamcinoloneDexamethasone + Framycetin + Gramicidin DGramicidin D + Neomycin + Nystatin + TriamcinoloneFramycetin + Gramicidin DGramicidin D + Neomycin + Nystatin + TriamcinoloneBacitracin + Gramicidin D + Polymyxin B SulfateGramicidin D + Neomycin + Nystatin + TriamcinoloneDexamethasone + Framycetin + Gramicidin DFramycetin + Gramicidin D + PhenylephrineGramicidin D + Neomycin + Nystatin + TriamcinoloneGramicidin D + Polymyxin B SulfateDexamethasone + Framycetin + Gramicidin DFluocinonide + Gramicidin D + Neomycin + NystatinGramicidin D + Polymyxin B SulfateGramicidin D + Lidocaine + Polymyxin B SulfateBacitracin + Gramicidin D + Polymyxin B SulfateGramicidin D + Lidocaine + Polymyxin B SulfateGramicidin D + Neomycin + Polymyxin B SulfateGramicidin D + Neomycin + Polymyxin B SulfateFramycetin + Gramicidin DGramicidin D + Lidocaine + Polymyxin B SulfateGramicidin D + Polymyxin B SulfateGramicidin D + Polymyxin B SulfateBacitracin + Gramicidin D + Polymyxin B SulfateBacitracin + Gramicidin D + Lidocaine + Polymyxin B SulfateBacitracin + Gramicidin D + Polymyxin B SulfateBacitracin + Gramicidin D + Polymyxin B SulfateBacitracin + Gramicidin D + Lidocaine + Polymyxin B SulfateBacitracin + Gramicidin D + Polymyxin B SulfateBacitracin + Gramicidin D + Lidocaine + Polymyxin B SulfateBacitracin + Gramicidin D + Lidocaine + Polymyxin B SulfateBacitracin + Gramicidin D + Polymyxin B SulfateGramicidin D + Neomycin + Polymyxin B SulfateGramicidin D + Neomycin + Polymyxin B SulfateGramicidin D + Polymyxin B SulfateGramicidin D + Neomycin + Polymyxin B SulfateFramycetin + Gramicidin DGramicidin D + Neomycin + Polymyxin B SulfateDexamethasone + Framycetin + Gramicidin DBacitracin + Gramicidin D + Polymyxin B SulfateGramicidin D + Neomycin + Polymyxin B SulfateGramicidin D + Neomycin + Polymyxin B SulfateGramicidin D + Polymyxin B SulfateGramicidin D + Polymyxin B SulfateGramicidin D + Neomycin + Polymyxin B SulfateGramicidin D + Neomycin + Nystatin + TriamcinoloneGramicidin D + Lidocaine + Polymyxin B Sulfate Neomycin and Polymyxin B Sulfates and GramicidinNeomycin and Polymyxin B Sulfates and GramicidinNeomycin and Polymyxin B Sulfates and GramicidinTheraderm CreamSofracort Sterile Ear/eye DropsSoframycin Nasal SprayPolysporin Antibiotic CreamPolytopic CreamPolysporin Eye and Ear Drops SterilePolysporin Plus Pain ReliefPolysporin for KidsAntibiotic CreamAntibiotic Cream for KidsOriginal Antibiotic CreamAntibiotic Cream Plus Pain ReliefAntibiotic CreamAntibiotic Cream Plus Pain ReliefAntibiotic Cream Plus Pain Relief for KidsViaderm Kc CrmViaderm Kc OntPolysporin Eye and Ear Drops SterilePolysporin CreamLidosporin CreamPolysporin Burn Formula CreamKenacomb OntSofracort Sterile Ear/eye DropsSoframycin Nasal SprayKenacomb Mild CreamSofracort Sterile Ear/eye OintmentKenacomb CreamSoframycin Skin OintmentKenacomb Mild OintmentPolysporin Triple Antibiotic OintmentKenacomb OintmentSofracort Ear/eye OintmentSoframycin Nasal SprayMecomb Crm 0.1%Antibiotic CreamSofracort Sterile Ear/eye OintmentLidecomb CreamPolycidin Eye, Ear DropsPolysporin Antibiotic Burn CreamPolysporin Triple Antibiotic OintmentLidosporin CreamNeosporin Antibiotic CreamNeosporin Eye-ear SolutionSoframycin OintmentAntibiotic Cream for KidsOriginal Antibiotic CreamOptimyxinPolysporin Triple Antibiotic OintmentPolysporin CompleteTriple Antibiotic OintmentTriple Antibiotic OintmentComplete Antibiotic OintmentTriple Antibiotic OintmentPolysporin for StitchesPolysporin Cold Sore OintmentTriple Antibiotic OintmentNeomycin and Polymyxin B Sulfates and GramicidinNeosporinAntibiotic DropsOdan-sporSoframycin Skin OintmentNeomycin and Polymyxin B Sulfates and GramicidinSandoz OpticortTriple Antibiotic OintmentNeocidinNeomycin and Polymyxin B Sulfates and GramicidinAntibiotic Ear DropsAntibiotic Eye DropsOptimyxin Plus Oto-opht GtteTeva-triacombAntibiotic Plus Pain Relief Cream Johnson & Johnson HealthcareMonarch PharmacyProfessional Co. http://www.jnjcanada.comhttp://www.monarch-pharmacy.co.uk Antibiotic CreamAntibiotic CreamAntibiotic CreamAntibiotic Cream for KidsAntibiotic Cream for KidsAntibiotic Cream Plus Pain ReliefAntibiotic Cream Plus Pain ReliefAntibiotic Cream Plus Pain Relief for KidsAntibiotic DropsAntibiotic Ear DropsAntibiotic Eye DropsAntibiotic Plus Pain Relief CreamComplete Antibiotic OintmentKenacomb CreamKenacomb Mild CreamKenacomb Mild OintmentKenacomb OintmentKenacomb OntLidecomb CreamLidosporin CreamLidosporin CreamMecomb Crm 0.1%NeocidinNeomycin and Polymyxin B Sulfates and GramicidinNeomycin and Polymyxin B Sulfates and GramicidinNeomycin and Polymyxin B Sulfates 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SpraySoframycin OintmentSoframycin Skin OintmentSoframycin Skin OintmentTeva-triacombTheraderm CreamTriple Antibiotic OintmentTriple Antibiotic OintmentTriple Antibiotic OintmentTriple Antibiotic OintmentTriple Antibiotic OintmentViaderm Kc CrmViaderm Kc Ont falsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsetruetruetruetruetruetruetruetruefalsefalsetruefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsetruefalsefalsefalsefalsefalsefalsefalsefalse Pharmetics (2011) Inc.Canadian Custom Packaging CompanyTechnilab Pharma Inc.Pharmetics (2011) Inc.Taro Pharmaceuticals, Inc.Pharmetics (2011) Inc.Canadian Custom Packaging CompanyCanadian Custom Packaging CompanySandoz Canada IncorporatedSandoz Canada IncorporatedSandoz Canada IncorporatedTaro Pharmaceuticals, Inc.Taro Pharmaceuticals, Inc.Westwood Squibb, Division Of Bristol Myers Squibb Canada Inc.Westwood Squibb, Division Of Bristol Myers Squibb Canada Inc.Westwood Squibb, Division Of Bristol Myers Squibb Canada Inc.Westwood Squibb, Division Of Bristol Myers Squibb Canada Inc.Squibb Canada Inc., Division Of Bristol Myers Squibb Canada Inc.Medicis Pharmaceutical CorporationGlaxo WellcomeWarner Lambert Canada Inc.Medic Laboratory LtÉeMajorRebel DistributorsPhysicians Total Care, Inc.A S Medication SolutionsDispensing Solutions, Inc.Bauch & Lomb IncorporatedA S Medication SolutionsPfizer Laboratories Div Pfizer Inc.Glaxosmithkline IncGlaxosmithkline IncOdan Laboratories LtdSandoz Canada IncorporatedSandoz Canada IncorporatedCrlsTaro Pharmaceuticals, Inc.Novartis Ophthalmics Novartis Pharmaceuticals (Canada) IncWarner Lambert Canada Inc.Johnson & JohnsonGlaxo WellcomeJohnson & JohnsonJohnson & JohnsonGlaxo WellcomeJohnson & JohnsonGlaxo WellcomeJohnson & JohnsonJohnson & JohnsonJohnson & JohnsonGlaxo WellcomeJohnson & JohnsonWarner Lambert Canada Inc.Sandoz Canada IncorporatedSandoz Canada IncorporatedRoussel Canada Inc.Sanofi AventisHoechst Roussel Canada Inc.Aventis Pharma Ltd.Hoechst Roussel Canada Inc.Erfa Canada 2012 IncRoussel Canada Inc.Hoechst Roussel Canada Inc.Roussel Canada Inc.Hoechst Roussel Canada Inc.Erfa Canada 2012 IncTevaBimeda Mtc Animal Health IncMelaleuca, Inc.Pharmetics (2011) Inc.Taro Pharmaceuticals, Inc.Jamp Pharma CorporationCanadian Custom Packaging CompanyTaro Pharmaceuticals, Inc.Taro Pharmaceuticals, Inc. truetruetruetruetruetruetruetruetruetruetruetruetruefalsefalsefalsefalsefalsefalsetruetruefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsetruefalsetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsetruetruetruetruetruefalsefalse TopicalTopicalTopicalTopicalTopicalTopicalTopicalTopicalAuricular (otic); OphthalmicAuricular (otic)OphthalmicTopicalTopicalTopicalTopicalTopicalTopicalTopicalTopicalTopicalTopicalTopicalOphthalmicOphthalmicOphthalmicOphthalmicOphthalmicOphthalmicOphthalmicOphthalmicTopicalAuricular (otic); OphthalmicOphthalmicAuricular (otic); OphthalmicAuricular (otic); OphthalmicTopicalTopicalAuricular (otic); OphthalmicTopicalTopicalTopicalTopicalTopicalTopicalAuricular (otic); OphthalmicAuricular (otic); OphthalmicTopicalTopicalTopicalTopicalTopicalTopicalTopicalAuricular (otic); OphthalmicAuricular (otic); OphthalmicAuricular (otic); OphthalmicTopicalAuricular (otic); OphthalmicTopicalNasalNasalNasalTopicalTopicalTopicalTopicalTopicalTopicalTopicalTopicalTopicalTopicalTopicalTopical CreamCreamCreamCreamCreamCreamCreamCreamSolutionSolution / dropsSolution / dropsCreamOintmentCreamCreamOintmentOintmentOintmentCreamCreamCreamCreamSolution / dropsSolution / dropsSolution / dropsSolution / dropsSolution / dropsSolution / dropsSolution / dropsSolutionCreamSolutionLiquidSolution / dropsSolution / dropsCreamCreamLiquidCreamCreamCreamOintmentOintmentCreamSolution / dropsSolution / dropsCreamOintmentCreamOintmentOintmentOintmentCreamSolutionOintmentSolution / dropsSolution / dropsOintmentOintmentSpraySpraySprayOintmentOintmentOintmentCreamCreamOintmentOintmentOintmentOintmentOintmentCreamOintment DPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPDDPD 0904-301621695-52854868-625354569-118855045-119424208-79050090-024761570-045 ANDA064047ANDA064047ANDA064047ANDA064047ANDA064047ANDA064047ANDA064047ANDA060582 truetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetruetrue 023118440237202902208288023179740231503302317834023720450237718702457512024587050245871302304457023044650199985001999842019998340199982600245267004924420196600602230842004645540066620300694371006350650070178500807435024010020231765602229903022308430223084400068535022842000224056800035335022391560003534302248189024469600223920102194104022372260223084700422908022479200017360602224623019877120222463101987720022248600017358401987690000269720198767402224879005505070202281802088339022979490224669302248818023814350071700200717029 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2009-12-232012-03-221998-11-032009-07-302009-12-232012-04-092012-07-112017-06-012017-09-012017-09-012009-07-302009-01-231965-12-311968-12-311968-12-311996-07-311965-12-311980-12-311971-12-311998-07-081979-12-312004-06-071996-01-312011-04-261996-01-311996-01-311996-01-311996-01-311955-04-111986-12-311987-12-311992-12-311989-12-311989-12-312010-10-261997-01-301998-07-081997-08-071991-12-312005-05-241971-12-312000-02-121971-12-312004-04-051999-06-181996-12-311998-08-131998-07-081997-01-272004-01-161966-12-312002-07-261966-12-311999-10-251966-12-312001-05-041959-12-311994-12-311961-12-311995-12-312001-05-041992-12-311993-12-311994-12-312009-12-232003-01-202005-01-311983-12-311983-12-31 2005-08-052004-08-052004-08-052004-08-052004-08-051997-08-141998-09-252000-08-032000-11-272003-07-172018-03-302017-06-202007-12-192006-11-212002-09-101999-06-182000-08-032000-08-032000-08-032000-08-031999-08-131996-09-092004-07-302006-07-282001-07-201996-09-091998-08-121997-08-052000-07-28 mlgg 23.12240.00.32 USDUSDUSD Neosporin gu irr 40 mg/ml ampGramicidin d powderNeosporin + pain relief cream d\EQr@`@@DB`lLcXQASTkCrbTkKj~i[V[gx@L@aXnEStwGprbgjFUj{~rJIQQJJJJVqQJJIRjZJJIZIKSJHqRiQJJYSFJIJIKSJHqRjJIUSQQJIHjKRqYQJIIEdEGPlDeHJZnZV]dx~_hEAZjjijZjjffij`ihFjJjffjfhJZAjbjjZZZBZBhijfB`HbHlL@``HbJDbaxH~B@rbLhPbDhcJhQbOZ`@@ CC(C)C[C@@H](NC(=O)CNC(=O)[C@@H](NC=O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)NCCO InChI=1S/C96H135N19O16/c1-50(2)36-71(105-79(118)48-102-93(128)80(54(9)10)103-49-117)86(121)104-58(17)84(119)113-82(56(13)14)95(130)115-83(57(15)16)96(131)114-81(55(11)12)94(129)112-78(43-62-47-101-70-33-25-21-29-66(62)70)92(127)108-74(39-53(7)8)89(124)111-77(42-61-46-100-69-32-24-20-28-65(61)69)91(126)107-73(38-52(5)6)88(123)110-76(41-60-45-99-68-31-23-19-27-64(60)68)90(125)106-72(37-51(3)4)87(122)109-75(85(120)97-34-35-116)40-59-44-98-67-30-22-18-26-63(59)67/h18-33,44-47,49-58,71-78,80-83,98-101,116H,34-43,48H2,1-17H3,(H,97,120)(H,102,128)(H,103,117)(H,104,121)(H,105,118)(H,106,125)(H,107,126)(H,108,127)(H,109,122)(H,110,123)(H,111,124)(H,112,129)(H,113,119)(H,114,131)(H,115,130)/t58-,71+,72+,73+,74+,75-,76-,77-,78-,80-,81+,82+,83-/m0/s1 NDAYQJDHGXTBJL-MWWSRJDJSA-N C96H135N19O16 11.945820150825762 11.560887729305339 519.8899999999996 492.3329000000001 DB00028 9007-83-4 Immune Globulin Human Human IGGHuman Immunoglobulin GHuman Normal ImmunoglobulinImmune globulin (human)Immune Globulin IntravenousImmune Globulin SubcutaneousImmunoglobulin G (human)Immunoglobulin G, HumanIntravenous ImmunoglobulinIVIg biotech 66Y330CJHS Wolfgang Stephan, "Production of intravenously applicable native human immune globulin having a normal half-life." U.S. Patent US4082734, issued July, 1970. liquid Intravenous immunoglobulin (IVIg) is a mixture of IgG1 and other antibodies derived from healthy human plasma via Cohn fractionation. The purification process includes cold alcohol fractionation, polyethylene glycol precipitation, and ion exchange chromatography. IVIg contains the same distribution of IgG antibody subclasses as is found in the general human population. IgG subclasses are fully represented in the following proportions: 70.3% IgG1, 24.7% IgG2, 3.1% IgG3, and 1.9% IgG4. IVIg is used in the treatment of immunodeficiencies, as well as autoimmune and inflammatory disorders. Humans and other mammalsBacteria and protozoaVarious viruses Injection, solutionInjection, solutionInjection, solutionInjection, powder, lyophilized, for solutionInjection, powder, lyophilized, for solutionInjection, powder, lyophilized, for solutionSolutionSolutionSolutionSolutionSolutionSolutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionLiquidInjectionSolutionSolutionInjection, solutionKitPowder, for solutionPowder, for solutionPowder, for solutionPowder, for solutionSolutionSolutionLiquidSolutionInjectionInjection, solutionLiquidSolutionSolutionInjection, solutionLiquidSolutionSolutionKit; liquid; powder, for solutionSolutionSolutionSolutionLiquidLiquidLiquidLiquidSolutionSolutionSolutionSolutionLiquidLiquidLiquidLiquidLiquid IntravenousIntravenousIntravenousIntravenousIntravenousIntravenousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousIntravenous; SubcutaneousIntravenousIntravenousIntravenousIntramuscularIntramuscularIntramuscularIntravenousIntravenous; SubcutaneousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntramuscularIntravenous; SubcutaneousIntravenous; SubcutaneousSubcutaneousSubcutaneousSubcutaneousIntramuscularSubcutaneousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousSubcutaneousSubcutaneousIntramuscular; IntravenousIntramuscular; IntravenousIntramuscular; IntravenousIntramuscular; IntravenousIntramuscular; Intravenous 1 g/10mL10 g/100mL5 g/50mL12 g/13 g/16 g/11 g1.65 g2 g3.3 g4 g8 g1 g/5mL.05 g/mL100 mg/ml50 mg/ml16.5 %.165 g/mL18 %50 mg100 mg/mL10 g2.5 g5 g0.5 g5 g/100mL5 g/50mL165 mg10 g10 g/100mL200 mg/ml.2 g/mL200 mg1500 unit100 mg/ml50 mg10 g5 g100 mg100 mg/mL50 mg/mL10 g/100mL20 g/200mL40 g/400mL5 g/50mL10 %120 g160 mg/mL160 mg1500 [iU]/mL15000 [iU]/mL2500 [iU]/mL5000 [iU]/mL600 [iU]/mL IVIg is used in the treatment of immunodeficiencies, as well as autoimmune and inflammatory disorders. These indications includes idiopathic thrombocytopenic purpura, Kawasaki disease, hypogammaglobulinemia, B cell chronic lymphocytic leukemia, bone marrow transplant complications, Guillain-Barré syndrome, chronic inflammatory demyelinating polyneuropathy (CIDP), multiple sclerosis, rheumatoid arthritis, myesthenia gravis, Wiskott–Aldrich syndrome and inflammatory skin diseases. IVIg interacts with a number of different components of the immune system, including cytokines, complement, Fc receptors and several cell surface immunocompetent molecules. IVIg also impacts different effector cells of the immune system (B and T lymphocytes, dendritic cells, etc.) and regulates a wide range of genes. Its main mechanism of actions are believed to be Fc-dependent and F(ab')2-dependent. IVIg competitively blocks gamma Fc receptors, preventing the binding and ingestion of phagocytes and suppressing platelet depletion. IVIg contains a number of different antobodies, which prevent infection by attaching to the surface of invading pathogens and aiding in their disposal before they can infect cells. Antibodies remove pathogens via complement activation, agglutination or precipitation, pathogen receptor blocking, macrophage “tagging” or neutralization (via binding) of pathogen toxins. Intact IVIg and F(ab′)2 fragments of IVIg can also neutralize the activity of various autoantibodies. By triggering the production of interleukin-1 receptor antagonist, IVIg modulates of the production of cytokines and cytokine antagonists. It also prevents the generation of the C5b-9 membrane attack complex and subsequent complement-mediated tissue damage by binding active complement components. antagonistantagonistantagonistantagonistantagonistantagonistantagonistbinderbinderbinderbinder High affinity immunoglobulin gamma Fc receptor IHigh affinity immunoglobulin gamma Fc receptor IBLow affinity immunoglobulin gamma Fc region receptor II-aLow affinity immunoglobulin gamma Fc region receptor II-bLow affinity immunoglobulin gamma Fc region receptor II-cLow affinity immunoglobulin gamma Fc region receptor III-ALow affinity immunoglobulin gamma Fc region receptor III-BComplement C3Complement C4-AComplement C4-BComplement C5 BE0000710BE0004684BE0002098BE0002099BE0002100BE0002097BE0000901BE0003455BE0004685BE0004686BE0000855 HumanHumanHumanHumanHumanHumanHumanHumanHumanHumanHuman Siberil S, Elluru S, Graff-Dubois S, Negi VS, Delignat S, Mouthon L, Lacroix-Desmazes S, Kazatchkine MD, Bayry J, Kaveri SV: Intravenous immunoglobulins in autoimmune and inflammatory diseases: a mechanistic perspective. Ann N Y Acad Sci. 2007 Sep;1110:497-506.Baerenwaldt A, Biburger M, Nimmerjahn F: Mechanisms of action of intravenous immunoglobulins. Expert Rev Clin Immunol. 2010 May;6(3):425-34. doi: 10.1586/eci.10.9.Negi VS, Elluru S, Siberil S, Graff-Dubois S, Mouthon L, Kazatchkine MD, Lacroix-Desmazes S, Bayry J, Kaveri SV: Intravenous immunoglobulin: an update on the clinical use and mechanisms of action. J Clin Immunol. 2007 May;27(3):233-45. Epub 2007 Mar 11.Siberil S, Elluru S, Graff-Dubois S, Negi VS, Delignat S, Mouthon L, Lacroix-Desmazes S, Kazatchkine MD, Bayry J, Kaveri SV: Intravenous immunoglobulins in autoimmune and inflammatory diseases: a mechanistic perspective. Ann N Y Acad Sci. 2007 Sep;1110:497-506.Baerenwaldt A, Biburger M, Nimmerjahn F: Mechanisms of action of intravenous immunoglobulins. Expert Rev Clin Immunol. 2010 May;6(3):425-34. doi: 10.1586/eci.10.9.Negi VS, Elluru S, Siberil S, Graff-Dubois S, Mouthon L, Kazatchkine MD, Lacroix-Desmazes S, Bayry J, Kaveri SV: Intravenous immunoglobulin: an update on the clinical use and mechanisms of action. J Clin Immunol. 2007 May;27(3):233-45. Epub 2007 Mar 11.Siberil S, Elluru S, Graff-Dubois S, Negi VS, Delignat S, Mouthon L, Lacroix-Desmazes S, Kazatchkine MD, Bayry J, Kaveri SV: Intravenous immunoglobulins in autoimmune and inflammatory diseases: a mechanistic perspective. Ann N Y Acad Sci. 2007 Sep;1110:497-506.Baerenwaldt A, Biburger M, Nimmerjahn F: Mechanisms of action of intravenous immunoglobulins. Expert Rev Clin Immunol. 2010 May;6(3):425-34. doi: 10.1586/eci.10.9.Negi VS, Elluru S, Siberil S, Graff-Dubois S, Mouthon L, Kazatchkine MD, Lacroix-Desmazes S, Bayry J, Kaveri SV: Intravenous immunoglobulin: an update on the clinical use and mechanisms of action. J Clin Immunol. 2007 May;27(3):233-45. Epub 2007 Mar 11.Siberil S, Elluru S, Graff-Dubois S, Negi VS, Delignat S, Mouthon L, Lacroix-Desmazes S, Kazatchkine MD, Bayry J, Kaveri SV: Intravenous immunoglobulins in autoimmune and inflammatory diseases: a mechanistic perspective. Ann N Y Acad Sci. 2007 Sep;1110:497-506.Baerenwaldt A, Biburger M, Nimmerjahn F: Mechanisms of action of intravenous immunoglobulins. Expert Rev Clin Immunol. 2010 May;6(3):425-34. doi: 10.1586/eci.10.9.Negi VS, Elluru S, Siberil S, Graff-Dubois S, Mouthon L, Kazatchkine MD, Lacroix-Desmazes S, Bayry J, Kaveri SV: Intravenous immunoglobulin: an update on the clinical use and mechanisms of action. J Clin Immunol. 2007 May;27(3):233-45. Epub 2007 Mar 11.Siberil S, Elluru S, Graff-Dubois S, Negi VS, Delignat S, Mouthon L, Lacroix-Desmazes S, Kazatchkine MD, Bayry J, Kaveri SV: Intravenous immunoglobulins in autoimmune and inflammatory diseases: a mechanistic perspective. Ann N Y Acad Sci. 2007 Sep;1110:497-506.Baerenwaldt A, Biburger M, Nimmerjahn F: Mechanisms of action of intravenous immunoglobulins. Expert Rev Clin Immunol. 2010 May;6(3):425-34. doi: 10.1586/eci.10.9.Negi VS, Elluru S, Siberil S, Graff-Dubois S, Mouthon L, Kazatchkine MD, Lacroix-Desmazes S, Bayry J, Kaveri SV: Intravenous immunoglobulin: an update on the clinical use and mechanisms of action. J Clin Immunol. 2007 May;27(3):233-45. Epub 2007 Mar 11.Siberil S, Elluru S, Graff-Dubois S, Negi VS, Delignat S, Mouthon L, Lacroix-Desmazes S, Kazatchkine MD, Bayry J, Kaveri SV: Intravenous immunoglobulins in autoimmune and inflammatory diseases: a mechanistic perspective. Ann N Y Acad Sci. 2007 Sep;1110:497-506.Baerenwaldt A, Biburger M, Nimmerjahn F: Mechanisms of action of intravenous immunoglobulins. Expert Rev Clin Immunol. 2010 May;6(3):425-34. doi: 10.1586/eci.10.9.Negi VS, Elluru S, Siberil S, Graff-Dubois S, Mouthon L, Kazatchkine MD, Lacroix-Desmazes S, Bayry J, Kaveri SV: Intravenous immunoglobulin: an update on the clinical use and mechanisms of action. J Clin Immunol. 2007 May;27(3):233-45. Epub 2007 Mar 11.Siberil S, Elluru S, Graff-Dubois S, Negi VS, Delignat S, Mouthon L, Lacroix-Desmazes S, Kazatchkine MD, Bayry J, Kaveri SV: Intravenous immunoglobulins in autoimmune and inflammatory diseases: a mechanistic perspective. Ann N Y Acad Sci. 2007 Sep;1110:497-506.Baerenwaldt A, Biburger M, Nimmerjahn F: Mechanisms of action of intravenous immunoglobulins. Expert Rev Clin Immunol. 2010 May;6(3):425-34. doi: 10.1586/eci.10.9.Negi VS, Elluru S, Siberil S, Graff-Dubois S, Mouthon L, Kazatchkine MD, Lacroix-Desmazes S, Bayry J, Kaveri SV: Intravenous immunoglobulin: an update on the clinical use and mechanisms of action. J Clin Immunol. 2007 May;27(3):233-45. Epub 2007 Mar 11.Baerenwaldt A, Biburger M, Nimmerjahn F: Mechanisms of action of intravenous immunoglobulins. Expert Rev Clin Immunol. 2010 May;6(3):425-34. doi: 10.1586/eci.10.9.Negi VS, Elluru S, Siberil S, Graff-Dubois S, Mouthon L, Kazatchkine MD, Lacroix-Desmazes S, Bayry J, Kaveri SV: Intravenous immunoglobulin: an update on the clinical use and mechanisms of action. J Clin Immunol. 2007 May;27(3):233-45. Epub 2007 Mar 11.Siberil S, Elluru S, Graff-Dubois S, Negi VS, Delignat S, Mouthon L, Lacroix-Desmazes S, Kazatchkine MD, Bayry J, Kaveri SV: Intravenous immunoglobulins in autoimmune and inflammatory diseases: a mechanistic perspective. Ann N Y Acad Sci. 2007 Sep;1110:497-506.Baerenwaldt A, Biburger M, Nimmerjahn F: Mechanisms of action of intravenous immunoglobulins. Expert Rev Clin Immunol. 2010 May;6(3):425-34. doi: 10.1586/eci.10.9.Negi VS, Elluru S, Siberil S, Graff-Dubois S, Mouthon L, Kazatchkine MD, Lacroix-Desmazes S, Bayry J, Kaveri SV: Intravenous immunoglobulin: an update on the clinical use and mechanisms of action. J Clin Immunol. 2007 May;27(3):233-45. Epub 2007 Mar 11.Siberil S, Elluru S, Graff-Dubois S, Negi VS, Delignat S, Mouthon L, Lacroix-Desmazes S, Kazatchkine MD, Bayry J, Kaveri SV: Intravenous immunoglobulins in autoimmune and inflammatory diseases: a mechanistic perspective. Ann N Y Acad Sci. 2007 Sep;1110:497-506.Baerenwaldt A, Biburger M, Nimmerjahn F: Mechanisms of action of intravenous immunoglobulins. Expert Rev Clin Immunol. 2010 May;6(3):425-34. doi: 10.1586/eci.10.9.Negi VS, Elluru S, Siberil S, Graff-Dubois S, Mouthon L, Kazatchkine MD, Lacroix-Desmazes S, Bayry J, Kaveri SV: Intravenous immunoglobulin: an update on the clinical use and mechanisms of action. J Clin Immunol. 2007 May;27(3):233-45. Epub 2007 Mar 11.Siberil S, Elluru S, Graff-Dubois S, Negi VS, Delignat S, Mouthon L, Lacroix-Desmazes S, Kazatchkine MD, Bayry J, Kaveri SV: Intravenous immunoglobulins in autoimmune and inflammatory diseases: a mechanistic perspective. Ann N Y Acad Sci. 2007 Sep;1110:497-506.Baerenwaldt A, Biburger M, Nimmerjahn F: Mechanisms of action of intravenous immunoglobulins. Expert Rev Clin Immunol. 2010 May;6(3):425-34. doi: 10.1586/eci.10.9.Negi VS, Elluru S, Siberil S, Graff-Dubois S, Mouthon L, Kazatchkine MD, Lacroix-Desmazes S, Bayry J, Kaveri SV: Intravenous immunoglobulin: an update on the clinical use and mechanisms of action. J Clin Immunol. 2007 May;27(3):233-45. Epub 2007 Mar 11.Siberil S, Elluru S, Graff-Dubois S, Negi VS, Delignat S, Mouthon L, Lacroix-Desmazes S, Kazatchkine MD, Bayry J, Kaveri SV: Intravenous immunoglobulins in autoimmune and inflammatory diseases: a mechanistic perspective. Ann N Y Acad Sci. 2007 Sep;1110:497-506. 179114652044142817351760179114652044142817351760179114652044142817351760179114652044142817351760179114652044142817351760179114652044142817351760179114652044142817351760204414281735176017911465204414281735176017911465204414281735176017911465204414281735176017911465 P12314Q92637P12318P31994P31995P08637O75015P01024P0C0L4P0C0L5P01031 High affinity immunoglobulin gamma Fc receptor IHigh affinity immunoglobulin gamma Fc receptor IBLow affinity immunoglobulin gamma Fc region receptor II-aLow affinity immunoglobulin gamma Fc region receptor II-bLow affinity immunoglobulin gamma Fc region receptor II-cLow affinity immunoglobulin gamma Fc region receptor III-ALow affinity immunoglobulin gamma Fc region receptor III-BComplement C3Complement C4-AComplement C4-BComplement C5 1q21.2-q21.31q231q231q23.31q231q239q33-q34 HumanHumanHumanHumanHumanHumanHumanHumanHumanHumanHuman early endosome membraneplasma membraneintegral component of membraneclathrin-coated endocytic vesicle membranereceptor signaling protein activitysignal transductioncytokine-mediated signaling pathwayimmune responseantigen processing and presentation of exogenous peptide antigen via MHC class I, TAP-dependentantigen processing and presentation of peptide antigen via MHC class Iinterferon-gamma-mediated signaling pathwayFc-gamma receptor signaling pathway involved in phagocytosisinnate immune responseregulation of immune responseantigen processing and presentation of exogenous peptide antigen via MHC class Iphagocytosis, engulfmentintracellular signal transductionplasma membraneintegral component of membraneearly endosome membraneclathrin-coated endocytic vesicle membraneimmunoglobulin receptor activityimmune responseFc receptor signaling pathwayantigen processing and presentation of exogenous peptide antigen via MHC class Icytokine-mediated signaling pathwayadaptive immune responseantigen processing and presentation of exogenous peptide antigen via MHC class I, TAP-dependentantigen processing and presentation of peptide antigen via MHC class Iinterferon-gamma-mediated signaling pathwayplasma membraneintegral component of membraneextracellular exosomeFc-gamma receptor signaling pathway involved in phagocytosisinnate immune responseplasma membraneintegral component of membranesignal transductionimmune responseregulation of immune responseviral processcytoplasmplasma membraneintegral component of membranetransmembrane signaling receptor activitysignal transductionimmune responseplasma membraneintegral component of membraneextracellular exosomeexternal side of plasma membraneimmune responseFc-gamma receptor signaling pathway involved in phagocytosisinnate immune responseregulation of immune responseplasma membraneextracellular exosomeanchored component of membraneimmune responsepositive regulation of defense response to virus by hostxenophagymitophagy in response to mitochondrial depolarizationextracellular exosomeextracellular regionplasma membraneblood microparticleextracellular spacecofactor bindingC5L2 anaphylatoxin chemotactic receptor bindingreceptor bindingendopeptidase inhibitor activitylipid bindingresponse to glucocorticoidresponse to magnesium ioninflammatory responsepositive regulation of ERK1 and ERK2 cascadesignal transductioncomplement activation, alternative pathwayregulation of complement activationpositive regulation of angiogenesisblood coagulationtolerance inductionpositive regulation of vascular endothelial growth factor productioninnate immune responsepositive regulation of lipid storagepositive regulation of activation of membrane attack complexpositive regulation of protein phosphorylationfatty acid metabolic processimmune responsepositive regulation of glucose transportregulation of immune responseresponse to progesteroneregulation of triglyceride biosynthetic processresponse to estradiolpositive regulation of apoptotic cell clearanceG-protein coupled receptor signaling pathwaypositive regulation of developmental growthcomplement activation, classical pathwaypositive regulation of type IIa hypersensitivitypositive regulation of G-protein coupled receptor protein signaling pathwaycomplement activationextracellular regionplasma membraneextracellular spaceextracellular exosomeblood microparticleendopeptidase inhibitor activitycomplement component C1q bindingcomplement activation, classical pathwaycomplement activationinflammatory responseregulation of complement activationinnate immune responsepositive regulation of apoptotic cell clearanceextracellular exosomeextracellular regiondendriteplasma membranesynapseextracellular spaceblood microparticleaxonother organism cellcell junctionserine-type endopeptidase activityendopeptidase inhibitor activitycarbohydrate bindingcomplement bindingdetection of molecule of bacterial origininnate immune responsecomplement activationinflammatory responsepositive regulation of apoptotic cell clearancecomplement activation, classical pathwayopsonizationregulation of complement activationextracellular regionextracellular exosomemembrane attack complexextracellular spacereceptor bindingendopeptidase inhibitor activitychemokine activitypositive regulation of chemokine secretioncomplement activation, classical pathwayinnate immune responsenegative regulation of macrophage chemotaxisG-protein coupled receptor signaling pathwaycomplement activation, alternative pathwaycell surface receptor signaling pathwaycell chemotaxiscomplement activationcytolysisinflammatory responsepositive regulation of angiogenesischemotaxisactivation of MAPK activityregulation of complement activationpositive regulation of vascular endothelial growth factor productionresponse to stressmitophagy in response to mitochondrial depolarizationin utero embryonic development Receptor signaling protein activityImmunoglobulin receptor activityTransmembrane signaling receptor activityReceptor bindingEndopeptidase inhibitor activityNon-enzymatic component of the C3 and C5 convertases and thus essential for the propagation of the classical complement pathway. Covalently binds to immunoglobulins and immune complexes and enhances the solubilization of immune aggregates and the clearance of IC through CR1 on erythrocytes. C4A isotype is responsible for effective binding to form amide bonds with immune aggregates or protein antigens, while C4B isotype catalyzes the transacylation of the thioester carbonyl group to form ester bonds with carbohydrate antigens.Receptor binding High affinity receptor for the Fc region of immunoglobulins gamma. Functions in both innate and adaptive immune responses.May bind to the Fc region of immunoglobulins gamma with a low affinity compared to FCGR1A. May function in the humoral immune response.Binds to the Fc region of immunoglobulins gamma. Low affinity receptor. By binding to IgG it initiates cellular responses against pathogens and soluble antigens. Promotes phagocytosis of opsonized antigens.Receptor for the Fc region of complexed or aggregated immunoglobulins gamma. Low affinity receptor. Involved in a variety of effector and regulatory functions such as phagocytosis of immune complexes and modulation of antibody production by B-cells. Binding to this receptor results in down-modulation of previous state of cell activation triggered via antigen receptors on B-cells (BCR), T-cells (TCR) or via another Fc receptor. Isoform IIB1 fails to mediate endocytosis or phagocytosis. Isoform IIB2 does not trigger phagocytosis.Receptor for the Fc region of complexed immunoglobulins gamma. Low affinity receptor. Involved in a variety of effector and regulatory functions such as phagocytosis of immune complexes and modulation of antibody production by B-cells.Receptor for the Fc region of IgG. Binds complexed or aggregated IgG and also monomeric IgG. Mediates antibody-dependent cellular cytotoxicity (ADCC) and other antibody-dependent responses, such as phagocytosis.Receptor for the Fc region of immunoglobulins gamma. Low affinity receptor. Binds complexed or aggregated IgG and also monomeric IgG. Contrary to III-A, is not capable to mediate antibody-dependent cytotoxicity and phagocytosis. May serve as a trap for immune complexes in the peripheral circulation which does not activate neutrophils.C3 plays a central role in the activation of the complement system. Its processing by C3 convertase is the central reaction in both classical and alternative complement pathways. After activation C3b can bind covalently, via its reactive thioester, to cell surface carbohydrates or immune aggregates.Derived from proteolytic degradation of complement C3, C3a anaphylatoxin is a mediator of local inflammatory process. In chronic inflammation, acts as a chemoattractant for neutrophils (By similarity). It induces the contraction of smooth muscle, increases vascular permeability and causes histamine release from mast cells and basophilic leukocytes.C3-beta-c: Acts as a chemoattractant for neutrophils in chronic inflammation.Acylation stimulating protein: adipogenic hormone that stimulates triglyceride (TG) synthesis and glucose transport in adipocytes, regulating fat storage and playing a role in postprandial TG clearance. Appears to stimulate TG synthesis via activation of the PLC, MAPK and AKT signaling pathways. Ligand for C5AR2. Promotes the phosphorylation, ARRB2-mediated internalization and recycling of C5AR2 (PubMed:8376604, PubMed:2909530, PubMed:9059512, PubMed:10432298, PubMed:15833747, PubMed:16333141, PubMed:19615750).Non-enzymatic component of C3 and C5 convertases and thus essential for the propagation of the classical complement pathway. Covalently binds to immunoglobulins and immune complexes and enhances the solubilization of immune aggregates and the clearance of IC through CR1 on erythrocytes. C4A isotype is responsible for effective binding to form amide bonds with immune aggregates or protein antigens, while C4B isotype catalyzes the transacylation of the thioester carbonyl group to form ester bonds with carbohydrate antigens.Derived from proteolytic degradation of complement C4, C4a anaphylatoxin is a mediator of local inflammatory process. It induces the contraction of smooth muscle, increases vascular permeability and causes histamine release from mast cells and basophilic leukocytes.Carbohydrate bindingActivation of C5 by a C5 convertase initiates the spontaneous assembly of the late complement components, C5-C9, into the membrane attack complex. C5b has a transient binding site for C6. The C5b-C6 complex is the foundation upon which the lytic complex is assembled.Derived from proteolytic degradation of complement C5, C5 anaphylatoxin is a mediator of local inflammatory process. Binding to the receptor C5AR1 induces a variety of responses including intracellular calcium release, contraction of smooth muscle, increased vascular permeability, and histamine release from mast cells and basophilic leukocytes (PubMed:8182049). C5a is also a potent chemokine which stimulates the locomotion of polymorphonuclear leukocytes and directs their migration toward sites of inflammation. >20 hours (mammalian reticulocytes, in vitro). Used as a replacement therapy in inherited humoral immunodeficiency disorders such as severe combined immunodeficiency syndrome, x-linked agammaglobulinemia, and Wiskott-Aldrich Syndrome. The immunoglobulins target, bind and kill bacterial cells as well as viral particles. IgG is the monomeric immunoglobulin of which there are four subclasses (IgG1, IgG2, IgG3 and IgG4) in differing abundances (66%, 23%, 7% and 4%). IgAs represent about 15% of the immunoglobulins in the blood. These target inhaled or ingested pathogens. The therapeutic efficacy of Varicella Zoster Vaccine (Live/Attenuated) can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of Yellow Fever Vaccine can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of Clostridium tetani toxoid antigen (formaldehyde inactivated) can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated) can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of Rotavirus Vaccine can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of G17DT can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of INGN 201 can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of INGN 225 can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of Rindopepimut can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of SRP 299 can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of GI-5005 can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of TG4010 can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of Rabies virus inactivated antigen, A can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of Tecemotide can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of Rubella virus vaccine can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of Anthrax immune globulin human can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of Bacillus calmette-guerin substrain tice live antigen can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of Japanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated) can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of Salmonella typhi ty2 vi polysaccharide antigen can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of Bacillus calmette-guerin substrain connaught live antigen can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of Hepatitis A Vaccine can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of Salmonella typhi ty21a live antigen can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of Human rabies virus immune globulin can be decreased when used in combination with Immune Globulin Human.The therapeutic efficacy of Hepatitis B Vaccine (Recombinant) can be decreased when used in combination with Immune Globulin Human. DB10318DB10805DB10583DB10584DB10276DB04914DB05322DB05325DB05374DB05440DB05942DB06584DB10283DB12568DB12768DB10317DB09057DB10343DB10769DB10803DB10804DB10989DB11050DB11603DB11627 Varicella Zoster Vaccine (Live/Attenuated)Yellow Fever VaccineClostridium tetani toxoid antigen (formaldehyde inactivated)Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated)Rotavirus VaccineG17DTINGN 201INGN 225RindopepimutSRP 299GI-5005TG4010Rabies virus inactivated antigen, ATecemotideBCG vaccineRubella virus vaccineAnthrax immune globulin humanBacillus calmette-guerin substrain tice live antigenJapanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated)Salmonella typhi ty2 vi polysaccharide antigenBacillus calmette-guerin substrain connaught live antigenHepatitis A VaccineSalmonella typhi ty21a live antigenHuman rabies virus immune globulinHepatitis B Vaccine (Recombinant) Melting PointHydrophobicityIsoelectric PointMolecular WeightMolecular Formula 61 °C (FAB fragment), 71 °C (whole mAb)-0.3318.13142682.3C6332H9826N1692O1980S42 Vermeer, A.W.P. & Norde, W., Biophys. J. 78:394-404 (2000) Amino Acids, Peptides, and ProteinsAntibodiesBlood ProteinsChemical Actions and UsesGlobulinsHuman Immunoglobulin GImmunoglobulin GImmunoglobulin IsotypesImmunoglobulinsImmunologic FactorsImmunoproteinsPharmacologic ActionsPhysiological Effects of DrugsProteinsSerumSerum Globulins D000602D000906D001798D020164D005916D007074D007132D007136D007155D007162D020228D045505D011506D044967D012712 77731516146508774J00221PA164754884P01877 Drugs Product Database (DPD)Drugs Product Database (DPD)PubChem SubstanceGenBankPharmGKBUniProtKB RxListDrugs.com http://www.rxlist.com/cgi/generic2/baygam.htmhttp://www.drugs.com/cdi/immune-globulin-human.html Bayry J, Fournier EM, Maddur MS, Vani J, Wootla B, Siberil S, Dimitrov JD, Lacroix-Desmazes S, Berdah M, Crabol Y, Oksenhendler E, Levy Y, Mouthon L, Sautes-Fridman C, Hermine O, Kaveri SV: Intravenous immunoglobulin induces proliferation and immunoglobulin synthesis from B cells of patients with common variable immunodeficiency: a mechanism underlying the beneficial effect of IVIg in primary immunodeficiencies. J Autoimmun. 2011 Feb;36(1):9-15. doi: 10.1016/j.jaut.2010.09.006. Epub 2010 Dec 9.Siberil S, Elluru S, Graff-Dubois S, Negi VS, Delignat S, Mouthon L, Lacroix-Desmazes S, Kazatchkine MD, Bayry J, Kaveri SV: Intravenous immunoglobulins in autoimmune and inflammatory diseases: a mechanistic perspective. Ann N Y Acad Sci. 2007 Sep;1110:497-506.Stangel M, Pul R: Basic principles of intravenous immunoglobulin (IVIg) treatment. J Neurol. 2006 Sep;253 Suppl 5:V18-24.Emmi L, Chiarini F: The role of intravenous immunoglobulin therapy in autoimmune and inflammatory disorders. Neurol Sci. 2002 Apr;23 Suppl 1:S1-8. 20970960179114651699874912032582 approvedinvestigational Instituto Grifols SA CivacirFlebogamma Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides Immune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin Human + WaterImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin HumanImmune Globulin Human Gamastan S/dGammagard S/dGamunexIgivnexPrivigenOctagam 10%Gammar Inj 165mg/mlIveegam Immuno 5000mg (iv)Immune Globulin Intravenous (human) 5%Gamimune N 5% (iv)GamastanGamimune N 10% (iv)Immune Globulin Intravenous (human), 5%Immune Globulin Intravenous (human), 10%Gammagard S/d (iv)Gammagard S/dGamimune N Inj 5% (iv)VivaglobinSandoglobulin Nf LiquidHyperrho S/d Full DoseOctagam 5%Hyperrho S/d Full DoseVivaglobinGamastan S/dCarimune NanofilteredCarimune NanofilteredCarimune NanofilteredBivigamBivigamFlebogamma DIFOctagam Immune Globulin (Human)Octagam Immune Globulin (Human)Octagam Immune Globulin (Human)Octagam Immune Globulin (Human)Gammagard S/dFlebogamma DifFlebogamma DifFlebogamma DifFlebogamma DifFlebogamma DifFlebogamma DifFlebogamma DifFlebogamma DifHyqviaHyqviaHyqviaHyqviaHyqviaKiovigKiovigKiovigKiovigKiovigKiovigHizentraHizentraHizentraHizentraHizentraHizentraHizentraHizentraHizentraHizentraHizentraWinrhoWinrhoWinrhoWinrhoWinrhoFlebogamma DifGAMMAGARD LiquidHizentraHizentraHizentraHizentraWinrhoWinrhoWinrhoWinrhoPanzygaBivigamGammaplexHizentraGammaplexPrivigenPrivigenPrivigenPrivigenFlebogamma 5%Flebogamma 10%Immune Serum Globulin (human)Gammagard S/dGammagard S/dGammagard S/dGammagard S/dGammagard S/dGammagard S/dGAMMAGARD LiquidCuvitruHizentraHizentraGamunex-CGammakedGammagard S/dCuvitruCutaquigCutaquigCutaquigCutaquigCutaquigCutaquig Alpha Therapeutic Corp.American Red CrossBaxter International Inc.Biotest PharmaceuticalsCangene Corp.CSL Behring LLCGrifols SAMassachusetts Public HealthMassbiologicsMedimmune Inc.Novartis AGOctapharma USATalecris Biotherapeutics http://www.redcross.orghttp://www.baxter.comhttp://www.biotestpharma.comhttp://www.cangene.comhttp://www.cslbehring.comhttp://www.grifols.comhttp://www.mphaweb.orghttp://www.massbio.orghttp://www.medimmune.comhttp://www.novartis.comhttp://www.octapharma.comhttp://www.talecris.com BivigamBivigamBivigamCarimune NanofilteredCarimune NanofilteredCarimune NanofilteredCutaquigCutaquigCutaquigCutaquigCutaquigCutaquigCuvitruCuvitruFlebogamma 10%Flebogamma 5%Flebogamma DIFFlebogamma DifFlebogamma DifFlebogamma DifFlebogamma DifFlebogamma DifFlebogamma DifFlebogamma DifFlebogamma DifFlebogamma DifGamastanGamastan S/dGamastan S/dGamimune N 10% (iv)Gamimune N 5% (iv)Gamimune N Inj 5% (iv)GAMMAGARD LiquidGAMMAGARD LiquidGammagard S/dGammagard S/dGammagard S/dGammagard S/dGammagard S/dGammagard S/dGammagard S/dGammagard S/dGammagard S/dGammagard S/dGammagard S/d (iv)GammakedGammaplexGammaplexGammar Inj 165mg/mlGamunexGamunex-CHizentraHizentraHizentraHizentraHizentraHizentraHizentraHizentraHizentraHizentraHizentraHizentraHizentraHizentraHizentraHizentraHizentraHizentraHyperrho S/d Full DoseHyperrho S/d Full DoseHyqviaHyqviaHyqviaHyqviaHyqviaIgivnexImmune Globulin Intravenous (human) 5%Immune Globulin Intravenous (human), 10%Immune Globulin Intravenous (human), 5%Immune Serum Globulin (human)Iveegam Immuno 5000mg (iv)KiovigKiovigKiovigKiovigKiovigKiovigOctagam 10%Octagam 5%Octagam Immune Globulin (Human)Octagam Immune Globulin (Human)Octagam Immune Globulin (Human)Octagam Immune Globulin (Human)PanzygaPrivigenPrivigenPrivigenPrivigenPrivigenSandoglobulin Nf LiquidVivaglobinVivaglobinWinrhoWinrhoWinrhoWinrhoWinrhoWinrhoWinrhoWinrhoWinrho 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Grifols, S.A.GrifolsInstituto Grifols, S.A.Instituto Grifols, S.A.Instituto Grifols, S.A.Instituto Grifols, S.A.Instituto Grifols, S.A.Instituto Grifols, S.A.Instituto Grifols, S.A.Instituto Grifols, S.A.GrifolsCutter Med & Biol, Division Of Miles Canada Ltd.Grifols Therapeutics Inc.GrifolsTalecris Biotherapeutics IncTalecris Biotherapeutics IncCutter Med & Biol, Division Of Miles Canada Ltd.Baxalta Canada CorporationBaxalta Canada CorporationBaxalta Canada CorporationBaxalta Canada CorporationBaxalta Canada CorporationBaxter LaboratoriesBaxter LaboratoriesBaxter LaboratoriesBaxter LaboratoriesBaxter LaboratoriesBaxter LaboratoriesBaxalta Canada CorporationBaxter LaboratoriesKedrion Biopharma, Inc.Bio Products Laboratory LimitedBio Products Laboratory LimitedArmour Pharmaceutical Co.Grifols Therapeutics Inc.GrifolsCsl Behring AgCsl Behring AgCsl Behring AgCsl Behring AgCsl BehringCsl BehringCsl BehringCsl BehringCsl BehringCsl BehringCsl BehringCsl BehringCsl BehringCsl BehringCsl BehringCsl BehringCsl BehringCsl BehringGrifols Therapeutics Inc.Grifols Therapeutics Inc.Baxalta Innovations Gmb HBaxalta Innovations Gmb HBaxalta Innovations Gmb HBaxalta Innovations Gmb HBaxalta Innovations Gmb HGrifols Therapeutics Inc.BayerTalecris Biotherapeutics IncTalecris Biotherapeutics IncGrifols Therapeutics Inc.Baxter AgBaxter AgBaxter AgBaxter AgBaxter AgBaxter AgBaxter AgOctapharma Pharmazeutika Produktionsges M B HOctapharma Pharmazeutika Produktionsges M B HOctapharma Pharmazeutika Produktionsgesellschaft M.B.H.Octapharma AbOctapharmaOctapharmaOctapharma Pharmazeutika Produktionsges M B HCsl Behring AgCsl Behring AgCsl Behring AgCsl Behring AgCsl BehringCsl BehringCsl BehringCsl BehringCangene Bio PharmaCangene Bio PharmaCangene Bio PharmaCangene Bio PharmaCangene Bio PharmaAptevo Bio Therapeutics LlcAptevo Bio Therapeutics LlcAptevo Bio Therapeutics LlcAptevo Bio Therapeutics Llc 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SubcutaneousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenous; SubcutaneousIntravenousIntravenousIntramuscularIntravenous; SubcutaneousIntravenous; SubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousIntramuscularIntramuscularSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousIntravenous; SubcutaneousIntravenousIntravenousIntravenousIntramuscularIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousIntravenousSubcutaneousSubcutaneousIntramuscular; IntravenousIntramuscular; IntravenousIntramuscular; IntravenousIntramuscular; IntravenousIntramuscular; IntravenousIntramuscular; IntravenousIntramuscular; IntravenousIntramuscular; IntravenousIntramuscular; Intravenous Injection, solutionInjection, solutionInjection, solutionInjection, powder, lyophilized, for solutionInjection, powder, lyophilized, for solutionInjection, powder, lyophilized, for solutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionInjection, solutionSolutionSolutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionLiquidSolutionInjectionSolutionSolutionLiquidInjection, solutionSolutionKitPowder, for solutionPowder, for solutionKitKitKitKitKitKitPowder, for solutionPowder, for solutionInjectionSolutionSolutionLiquidSolutionInjectionLiquidLiquidLiquidLiquidSolutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionSolutionSolutionSolutionSolutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionSolutionLiquidSolutionSolutionSolutionKit; Liquid; Powder, for solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, solutionSolutionSolutionSolutionSolutionSolutionSolutionSolutionLiquidLiquidLiquidLiquidSolutionSolutionSolutionSolutionLiquidLiquidLiquidLiquidLiquidLiquidLiquidLiquidLiquid FDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCDPDDPDDPDDPDDPDDPDDPDFDA NDCDPDDPDFDA NDCEMAEMAEMAEMAEMAEMAEMAEMAFDA NDCDPDDPDFDA NDCDPDDPDDPDFDA NDCDPDFDA NDCDPDDPDFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCDPDDPDFDA NDCFDA NDCFDA NDCDPDDPDFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCDPDEMAEMAEMAEMAEMAEMAEMAEMAEMAEMAEMADPDDPDDPDDPDEMAEMAEMAEMAEMADPDDPDDPDDPDDPDDPDEMAEMAEMAEMAEMAEMADPDDPDFDA NDCFDA NDCFDA NDCFDA NDCDPDFDA NDCFDA NDCFDA NDCFDA NDCDPDDPDDPDFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDCFDA NDC 1 g/10mL5 g/50mL10 g/100mL3 g/16 g/112 g/11 g1.65 g2 g3.3 g4 g8 g200 mg1 g/5mL100 mg50 mg.05 g/mL50 mg/ml50 mg/ml50 mg/ml50 mg/ml50 mg/ml100 mg/ml100 mg/ml100 mg/ml5 g/50mL16.5 %18 %.165 g/mL100 mg50 mg50 mg100 mg/mL10 %2.5 g10 g5 g0.5 g10 g/100mL5 g/50mL5 g/100mL165 mg10 g10 g/100mL.2 g/mL.2 g/mL.2 g/mL.2 g/mL200 mg200 mg/ml200 mg/ml200 mg/ml200 mg/ml200 mg/ml200 mg/ml200 mg/ml200 mg/ml200 mg/ml200 mg/ml200 mg/ml200 mg200 mg1500 unit1500 unit100 mg/ml100 mg/ml100 mg/ml100 mg/ml100 mg/ml10 g50 mg10 g5 g18 %100 mg/ml100 mg/ml100 mg/ml100 mg/ml100 mg/ml100 mg/ml100 mg50 mg50 mg/mL50 mg/mL50 mg/mL100 mg/mL100 mg5 g/50mL10 g/100mL20 g/200mL40 g/400mL10 %120 g160 mg160 mg/mL15000 [iU]/mL5000 [iU]/mL600 [iU]/mL1500 [iU]/mL2500 [iU]/mL15000 [iU]/mL5000 [iU]/mL1500 [iU]/mL2500 [iU]/mL 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USUSUSUSUSUSCanadaCanadaCanadaCanadaCanadaCanadaCanadaUSCanadaCanadaUSEUEUEUEUEUEUEUEUUSCanadaCanadaUSCanadaCanadaCanadaUSCanadaUSCanadaCanadaUSUSUSUSUSUSCanadaCanadaUSUSUSCanadaCanadaUSUSUSUSUSCanadaEUEUEUEUEUEUEUEUEUEUEUCanadaCanadaCanadaCanadaEUEUEUEUEUCanadaCanadaCanadaCanadaCanadaCanadaEUEUEUEUEUEUCanadaCanadaUSUSUSUSCanadaUSUSUSUSCanadaCanadaCanadaUSUSUSUSUSUSUSUSUSUS 2013-02-042013-02-042013-02-042009-02-102009-02-102009-02-102017-12-212016-10-182006-12-212007-07-232007-07-232007-07-232007-07-232007-07-232007-07-232007-07-232007-07-232010-07-271951-12-312004-03-041996-08-142000-05-161997-01-171986-12-312005-04-272007-08-081994-05-101997-08-221997-08-221994-05-101994-05-101994-05-101994-05-101994-05-101994-05-101997-08-221997-08-222010-10-132017-04-072010-11-011991-12-312003-10-222010-10-132011-10-032011-10-032011-10-032011-10-032011-10-132011-04-142011-04-142011-04-142011-04-142011-04-142011-04-142011-04-142011-04-142011-04-142011-04-142011-04-142017-09-212017-09-212013-05-162013-05-162013-05-162013-05-162013-05-162006-05-241996-12-312000-07-311997-11-031997-04-211992-12-312006-01-192006-01-192006-01-192006-01-192006-01-192006-01-192013-04-042004-05-212006-04-142004-05-212004-05-212016-12-212009-01-202009-01-202009-01-202009-01-202009-01-082007-06-282007-03-012006-01-092005-03-312004-03-312005-03-312005-03-312005-03-312016-07-012016-07-012016-07-012016-07-01 2016-11-221998-09-252006-08-032006-08-031998-09-252015-05-122013-11-041999-12-151998-09-282006-08-032006-08-032008-12-232010-04-202015-04-022016-10-19 mlmlmlmlmlmlmlmlmlmlmlmlsyringe 4.844.849.3411.613.7924.4430.2430.2430.24165.04176.34224.07324.23 USDUSDUSDUSDUSDUSDUSDUSDUSDUSDUSDUSDUSD Flebogamma 5% vialFlebogamma dif 5% vialImmune globulin vialGamunex 10% vialGammagard liquid 10% vialGamastan s-d vialHizentra 1 gram/5 ml vialHizentra 2 gram/10 ml vialHizentra 4 gram/20 ml vialHyperhep b s-d vialNabi-hb vialHyperrab s-d vialHypertet s-d 250 unit syringe DB00029 81669-57-0 Anistreplase Anisoylated plasminogen streptokinase activator complexAPSAC biotech 5O8V541HJ6 liquid Human tissue plasminogen activator, purified, glycosylated, 527 residues purified from CHO cells. Eminase is a lyophilized (freeze-dried) formulation of anistreplase, the p-anisoyl derivative of the primary Lys-plasminogen-streptokinase activator complex (a complex of Lys-plasminogen and streptokinase). A p-anisoyl group is chemically conjugated to a complex of bacterial-derived streptokinase and human Plasma-derived Lys-plasminogen proteins. Humans and other mammals Powder, for solution Intravenous 30 unit For lysis of acute pulmonary emboli, intracoronary emboli and management of myocardial infarction Anistreplase cleaves the Arg/Val bond in plasminogen to form plasmin. This in turn leads to the degradation of blood clots. activator PlasminogenFibrinogen alpha chainUrokinase plasminogen activator surface receptorPlasminogen activator inhibitor 1 BE0000211BE0000538BE0000717BE0000240 HumanHumanHumanHuman Longstaff C, Williams S, Thelwell C: Fibrin binding and the regulation of plasminogen activators during thrombolytic therapy. Cardiovasc Hematol Agents Med Chem. 2008 Jul;6(3):212-23.Melandri G, Vagnarelli F, Calabrese D, Semprini F, Nanni S, Branzi A: Review of tenecteplase (TNKase) in the treatment of acute myocardial infarction. Vasc Health Risk Manag. 2009;5(1):249-56. Epub 2009 Apr 8.Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST-segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70. 186732351943665617963464117523521713928417016423171392841701642317963464 P00747P02671Q03405P05121 PlasminogenFibrinogen alpha chainUrokinase plasminogen activator surface receptorPlasminogen activator inhibitor 1 6q264q2819q137q21.3-q22 HumanHumanHumanHuman extracellular exosomeextrinsic component of external side of plasma membraneextracellular regionplasma membraneplatelet alpha granule lumenextracellular spaceblood microparticlecell surfaceapolipoprotein bindingserine-type endopeptidase activityreceptor bindingserine-type peptidase activityprotein domain specific bindingnegative regulation of fibrinolysisblood coagulationextracellular matrix disassemblyproteolysisextracellular matrix organizationpositive regulation of fibrinolysisnegative regulation of cell-substrate adhesiontissue remodelingcellular protein metabolic processnegative regulation of cell-cell adhesion mediated by cadherinnegative regulation of cell proliferationplatelet degranulationfibrinolysisplatelet activationblood microparticlerough endoplasmic reticulumextracellular exosomecell cortexexternal side of plasma membraneextracellular regionplasma membraneextracellular spacecell surfaceextracellular vesicleplatelet alpha granuleplatelet alpha granule lumenfibrinogen complexstructural molecule activityplatelet degranulationsignal transductionresponse to cycloheximideprotein complex assemblycellular protein complex assemblypositive regulation of peptide hormone secretionacute-phase responseprotein polymerizationpositive regulation of substrate adhesion-dependent cell spreadinginnate immune responsefibrinolysisblood coagulationadaptive immune responseliver regenerationresponse to calcium ionpositive regulation of protein secretionresponse to genisteinextracellular matrix organizationplatelet aggregationcellular response to organic cyclic compoundresponse to estradiolinduction of bacterial agglutinationpositive regulation of vasoconstrictioncell-matrix adhesionplasminogen activationcellular protein metabolic processblood coagulation, common pathwaypositive regulation of ERK1 and ERK2 cascadecellular response to interleukin-6negative regulation of extrinsic apoptotic signaling pathway via death domain receptorscellular response to granulocyte colony-stimulating factornegative regulation of endothelial cell apoptotic processpositive regulation of exocytosisnegative regulation of blood coagulation, common pathwaypositive regulation of heterotypic cell-cell adhesionplatelet activationresponse to morphineblood coagulation, fibrin clot formationintegral component of plasma membraneendoplasmic reticulum lumenanchored component of membraneplasma membraneextrinsic component of membraneendoplasmic reticulum membraneinvadopodium membranefocal adhesionintegral component of membraneextracellular exosomereceptor activityreceptor bindingprotein domain specific bindingurokinase plasminogen activator receptor activityenzyme bindingnegative regulation of intrinsic apoptotic signaling pathwayurokinase plasminogen activator signaling pathwaypositive regulation of protein phosphorylationpositive regulation of DNA bindingsignal transductionpositive regulation of epidermal growth factor receptor signaling pathwayblood coagulationpositive regulation of release of cytochrome c from mitochondriacellular protein metabolic processnegative regulation of apoptotic processpost-translational protein modificationfibrinolysisregulation of proteolysischemotaxismovement of cell or subcellular componentattachment of GPI anchor to proteinnegative regulation of cysteine-type endopeptidase activity involved in apoptotic signaling pathwayC-terminal protein lipidationextracellular matrixextracellular regionplatelet alpha granule lumenplasma membraneextracellular spaceextracellular exosomeprotease bindingreceptor bindingserine-type endopeptidase inhibitor activityangiogenesisnegative regulation of smooth muscle cell migrationextracellular matrix organizationtransforming growth factor beta receptor signaling pathwaycellular response to lipopolysaccharideblood coagulationnegative regulation of smooth muscle cell-matrix adhesionnegative regulation of extrinsic apoptotic signaling pathway via death domain receptorsnegative regulation of endopeptidase activitynegative regulation of vascular wound healingpositive regulation of transcription from RNA polymerase II promoternegative regulation of wound healingchronological cell agingpositive regulation of angiogenesisplatelet degranulationdefense response to Gram-negative bacteriumpositive regulation of interleukin-8 productionfibrinolysisnegative regulation of blood coagulationpositive regulation of leukotriene production involved in inflammatory responsenegative regulation of fibrinolysisnegative regulation of cell adhesion mediated by integrinpositive regulation of monocyte chemotaxisplatelet activationpositive regulation of blood coagulationnegative regulation of cell migrationpositive regulation of receptor-mediated endocytosisgene expressionpositive regulation of inflammatory responsenegative regulation of endothelial cell apoptotic processtranscription initiation from RNA polymerase II promoterregulation of receptor activitycircadian rhythmnegative regulation of plasminogen activationtranscription, DNA-templated Serine-type peptidase activityStructural molecule activityUrokinase plasminogen activator receptor activitySerine-type endopeptidase inhibitor activity Plasmin dissolves the fibrin of blood clots and acts as a proteolytic factor in a variety of other processes including embryonic development, tissue remodeling, tumor invasion, and inflammation. In ovulation, weakens the walls of the Graafian follicle. It activates the urokinase-type plasminogen activator, collagenases and several complement zymogens, such as C1 and C5. Cleavage of fibronectin and laminin leads to cell detachment and apoptosis. Also cleaves fibrin, thrombospondin and von Willebrand factor. Its role in tissue remodeling and tumor invasion may be modulated by CSPG4. Binds to cells.Angiostatin is an angiogenesis inhibitor that blocks neovascularization and growth of experimental primary and metastatic tumors in vivo.Cleaved by the protease thrombin to yield monomers which, together with fibrinogen beta (FGB) and fibrinogen gamma (FGG), polymerize to form an insoluble fibrin matrix. Fibrin has a major function in hemostasis as one of the primary components of blood clots. In addition, functions during the early stages of wound repair to stabilize the lesion and guide cell migration during re-epithelialization. Was originally thought to be essential for platelet aggregation, based on in vitro studies using anticoagulated blood. However, subsequent studies have shown that it is not absolutely required for thrombus formation in vivo. Enhances expression of SELP in activated platelets via an ITGB3-dependent pathway. Maternal fibrinogen is essential for successful pregnancy. Fibrin deposition is also associated with infection, where it protects against IFNG-mediated hemorrhage. May also facilitate the immune response via both innate and T-cell mediated pathways.Acts as a receptor for urokinase plasminogen activator. Plays a role in localizing and promoting plasmin formation. Mediates the proteolysis-independent signal transduction activation effects of U-PA. It is subject to negative-feedback regulation by U-PA which cleaves it into an inactive form.Serine protease inhibitor. This inhibitor acts as 'bait' for tissue plasminogen activator, urokinase, protein C and matriptase-3/TMPRSS7. Its rapid interaction with PLAT may function as a major control point in the regulation of fibrinolysis. Anistreplase cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that cause myocardial infarction. The therapeutic efficacy of Anistreplase can be decreased when used in combination with Aprotinin.The risk or severity of adverse effects can be increased when Limaprost is combined with Anistreplase.Anistreplase may increase the anticoagulant activities of Dabigatran etexilate.Anistreplase may increase the anticoagulant activities of Lepirudin.Anistreplase may increase the anticoagulant activities of Bivalirudin.Anistreplase may increase the anticoagulant activities of Abciximab.Anistreplase may increase the anticoagulant activities of Becaplermin.Anistreplase may increase the anticoagulant activities of Dicoumarol.Anistreplase may increase the anticoagulant activities of Argatroban.Anistreplase may increase the anticoagulant activities of Ardeparin.Anistreplase may increase the anticoagulant activities of Phenindione.Anistreplase may increase the anticoagulant activities of Fondaparinux sodium.Anistreplase may increase the anticoagulant activities of Warfarin.Anistreplase may increase the anticoagulant activities of Pentosan Polysulfate.Anistreplase may increase the anticoagulant activities of Phenprocoumon.Anistreplase may increase the anticoagulant activities of Edetic Acid.Anistreplase may increase the anticoagulant activities of Heparin.Anistreplase may increase the anticoagulant activities of Enoxaparin.Anistreplase may increase the anticoagulant activities of Acenocoumarol.Anistreplase may increase the anticoagulant activities of Citric Acid.Anistreplase may increase the anticoagulant activities of Ximelagatran.Anistreplase may increase the anticoagulant activities of Ancrod.Anistreplase may increase the anticoagulant activities of Pentaerythritol Tetranitrate.Anistreplase may increase the anticoagulant activities of Rivaroxaban.Anistreplase may increase the anticoagulant activities of Sulodexide.Anistreplase may increase the anticoagulant activities of Idraparinux.Anistreplase may increase the anticoagulant activities of Apixaban.Anistreplase may increase the anticoagulant activities of Otamixaban.Anistreplase may increase the anticoagulant activities of Danaparoid.Anistreplase may increase the anticoagulant activities of Dalteparin.Anistreplase may increase the anticoagulant activities of Ferulic acid.Anistreplase may increase the anticoagulant activities of Ethyl biscoumacetate.Anistreplase may increase the anticoagulant activities of Nadroparin.Anistreplase may increase the anticoagulant activities of Edoxaban.Anistreplase may increase the anticoagulant activities of Dextran.Anistreplase may increase the anticoagulant activities of Reviparin.Anistreplase may increase the anticoagulant activities of Certoparin.Anistreplase may increase the anticoagulant activities of Dextran 70.Anistreplase may increase the anticoagulant activities of Desirudin.Anistreplase may increase the anticoagulant activities of Dextran 40.Anistreplase may increase the anticoagulant activities of Dextran 75.Anistreplase may increase the anticoagulant activities of Protocatechualdehyde.Anistreplase may increase the anticoagulant activities of Protein C.Anistreplase may increase the anticoagulant activities of Antithrombin III human.Anistreplase may increase the anticoagulant activities of Fondaparinux.Anistreplase may increase the anticoagulant activities of Letaxaban.Anistreplase may increase the anticoagulant activities of Darexaban.Anistreplase may increase the anticoagulant activities of Nafamostat.Anistreplase may increase the anticoagulant activities of Gabexate.Anistreplase may increase the anticoagulant activities of Troxerutin.Anistreplase may increase the anticoagulant activities of Fluindione.Anistreplase may increase the anticoagulant activities of Protein S human.Anistreplase may increase the anticoagulant activities of Melagatran.The risk or severity of adverse effects can be increased when Salicylic acid is combined with Anistreplase.The risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Anistreplase.The risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Anistreplase.The risk or severity of adverse effects can be increased when Mesalazine is combined with Anistreplase.The risk or severity of adverse effects can be increased when Diflunisal is combined with Anistreplase.The risk or severity of adverse effects can be increased when Balsalazide is combined with Anistreplase.The risk or severity of adverse effects can be increased when Olsalazine is combined with Anistreplase.The risk or severity of adverse effects can be increased when Dersalazine is combined with Anistreplase.The risk or severity of adverse effects can be increased when Nitroaspirin is combined with Anistreplase.The risk or severity of adverse effects can be increased when Aloxiprin is combined with Anistreplase.The risk or severity of adverse effects can be increased when Guacetisal is combined with Anistreplase.The risk or severity of adverse effects can be increased when Carbaspirin calcium is combined with Anistreplase.The risk or severity of adverse effects can be increased when Hemoglobin crosfumaril is combined with Anistreplase.The risk or severity of adverse effects can be increased when Methyl salicylate is combined with Anistreplase.The risk or severity of adverse effects can be increased when Trolamine salicylate is combined with Anistreplase.Eptifibatide may increase the anticoagulant activities of Anistreplase.Ticlopidine may increase the anticoagulant activities of Anistreplase.Tirofiban may increase the anticoagulant activities of Anistreplase.Dipyridamole may increase the anticoagulant activities of Anistreplase.Clopidogrel may increase the anticoagulant activities of Anistreplase.Prasugrel may increase the anticoagulant activities of Anistreplase.Vorapaxar may increase the anticoagulant activities of Anistreplase.Milrinone may increase the anticoagulant activities of Anistreplase.Anagrelide may increase the anticoagulant activities of Anistreplase.Epinastine may increase the anticoagulant activities of Anistreplase.Alprostadil may increase the anticoagulant activities of Anistreplase.Pentoxifylline may increase the anticoagulant activities of Anistreplase.Azelastine may increase the anticoagulant activities of Anistreplase.Iloprost may increase the anticoagulant activities of Anistreplase.Cilostazol may increase the anticoagulant activities of Anistreplase.Ridogrel may increase the anticoagulant activities of Anistreplase.Sevoflurane may increase the anticoagulant activities of Anistreplase.Epoprostenol may increase the anticoagulant activities of Anistreplase.Resveratrol may increase the anticoagulant activities of Anistreplase.Nimesulide may increase the anticoagulant activities of Anistreplase.Tesmilifene may increase the anticoagulant activities of Anistreplase.Defibrotide may increase the anticoagulant activities of Anistreplase.SRT501 may increase the anticoagulant activities of Anistreplase.Beraprost may increase the anticoagulant activities of Anistreplase.Ibudilast may increase the anticoagulant activities of Anistreplase.Andrographolide may increase the anticoagulant activities of Anistreplase.eplivanserine may increase the anticoagulant activities of Anistreplase.Cangrelor may increase the anticoagulant activities of Anistreplase.Tranilast may increase the anticoagulant activities of Anistreplase.Triflusal may increase the anticoagulant activities of Anistreplase.Icosapent ethyl may increase the anticoagulant activities of Anistreplase.Ifenprodil may increase the anticoagulant activities of Anistreplase.Trapidil may increase the anticoagulant activities of Anistreplase.Naftopidil may increase the anticoagulant activities of Anistreplase.Sarpogrelate may increase the anticoagulant activities of Anistreplase.Eplivanserin may increase the anticoagulant activities of Anistreplase.Ifetroban may increase the anticoagulant activities of Anistreplase.Ketanserin may increase the anticoagulant activities of Anistreplase.Indobufen may increase the anticoagulant activities of Anistreplase.Butylphthalide may increase the anticoagulant activities of Anistreplase.Hydroxytyrosol may increase the anticoagulant activities of Anistreplase.Ramatroban may increase the anticoagulant activities of Anistreplase.Picotamide may increase the anticoagulant activities of Anistreplase.Cloricromen may increase the anticoagulant activities of Anistreplase.Linsidomine may increase the anticoagulant activities of Anistreplase.Buflomedil may increase the anticoagulant activities of Anistreplase.Relcovaptan may increase the anticoagulant activities of Anistreplase.Ticagrelor may increase the anticoagulant activities of Anistreplase.The risk or severity of adverse effects can be increased when Anistreplase is combined with Treprostinil. DB06692DB09211DB06695DB00001DB00006DB00054DB00102DB00266DB00278DB00407DB00498DB00569DB00682DB00686DB00946DB00974DB01109DB01225DB01418DB04272DB04898DB05099DB06154DB06228DB06271DB06406DB06605DB06635DB06754DB06779DB07767DB08794DB08813DB09075DB09255DB09259DB09261DB11076DB11095DB11122DB11241DB11268DB11312DB11598DB11728DB11984DB12289DB12598DB12831DB13124DB13136DB13149DB13616DB00936DB00945DB00233DB00244DB00861DB01014DB01250DB06251DB12445DB13509DB13538DB13612DB13864DB09543DB11079DB00063DB00208DB00775DB00975DB00758DB06209DB09030DB00235DB00261DB00751DB00770DB00806DB00972DB01088DB01166DB01207DB01236DB01240DB02709DB04743DB04905DB04932DB05073DB05229DB05266DB05767DB06392DB06441DB07615DB08814DB08887DB08954DB09283DB12092DB12163DB12177DB12321DB12465DB12545DB12749DB12771DB13036DB13327DB13367DB13400DB13510DB13929DB08816DB00374 AprotininLimaprostDabigatran etexilateLepirudinBivalirudinAbciximabBecaplerminDicoumarolArgatrobanArdeparinPhenindioneFondaparinux sodiumWarfarinPentosan PolysulfatePhenprocoumonEdetic AcidHeparinEnoxaparinAcenocoumarolCitric AcidXimelagatranAncrodPentaerythritol TetranitrateRivaroxabanSulodexideIdraparinuxApixabanOtamixabanDanaparoidDalteparinFerulic acidEthyl biscoumacetateNadroparinEdoxabanDextranReviparinCertoparinDextran 70DesirudinDextran 40Dextran 75ProtocatechualdehydeProtein CAntithrombin III humanFondaparinuxLetaxabanDarexabanNafamostatGabexateTroxerutinFluindioneProtein S humanMelagatranSalicylic acidAcetylsalicylic acidAminosalicylic AcidMesalazineDiflunisalBalsalazideOlsalazineDersalazineNitroaspirinAloxiprinGuacetisalCarbaspirin calciumHemoglobin crosfumarilMethyl salicylateTrolamine salicylateEptifibatideTiclopidineTirofibanDipyridamoleClopidogrelPrasugrelVorapaxarMilrinoneAnagrelideEpinastineAlprostadilPentoxifyllineAzelastineIloprostCilostazolRidogrelSevofluraneEpoprostenolResveratrolNimesulideTesmilifeneDefibrotideSRT501BeraprostIbudilastAndrographolideeplivanserineCangrelorTranilastTriflusalIcosapent ethylIfenprodilTrapidilNaftopidilSarpogrelateEplivanserinIfetrobanKetanserinIndobufenButylphthalideHydroxytyrosolRamatrobanPicotamideCloricromenLinsidomineBuflomedilRelcovaptanTicagrelorTreprostinil Melting PointHydrophobicityIsoelectric PointMolecular WeightMolecular Formula 60 °C-0.5167.6159042.3C2569H3928N746O781S40 Novokhatny, V.V. et al., J. Biol. Chem. 266:12994-123002 (1991) B01AD03 EnzymesANTITHROMBOTIC AGENTSANTITHROMBOTIC AGENTSBLOOD AND BLOOD FORMING ORGANS B01ADB01AB01B Amino Acids, Peptides, and ProteinsBiological FactorsBlood and Blood Forming OrgansBlood Coagulation FactorsBlood ProteinsCardiovascular AgentsChemical Actions and UsesEndopeptidasesEnzymesEnzymes and CoenzymesFibrin Modulating AgentsFibrinolytic AgentsHematologic AgentsHydrolasesMolecular Mechanisms of Pharmacological ActionPeptide HydrolasesPharmacologic ActionsPlasminogen ActivatorsProteinsSerine EndopeptidasesSerine ProteasesStreptokinaseTherapeutic Uses D000602D001685D001779D001798D002317D020164D010450D004798D045762D050299D005343D006401D006867D045504D010447D020228D010960D011506D012697D057057D013300D045506 119946504487L00153PA164769075P00750DAP001197AnistreplaseCHEMBL2108250 Drugs Product Database (DPD)PubChem SubstanceGenBankPharmGKBUniProtKBTherapeutic Targets DatabaseWikipediaChEMBL approved Wulfing Pharma GmbH Eminase Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides drug_action DB00029DB01022DB01373 AnistreplasePhylloquinoneCalcium P00747P00748P02452P03952P03951P00740P00451P00734P12259P00742P02671P02675P02679P00488P05160P00750P08709P13726Q9BQB6P38435 Anistreplase Action Pathway SMP00281 Anistreplase Eminase 30 Units Haupt Pharma http://haupt-pharma.de Eminase 30 Units false Well Spring Pharmaceutical Corporation false Intravenous Powder, for solution DPD 30 unit true 02229390 Canada 1997-12-15 2009-02-23 DB00030DB01383DB05278DB05215DB05283DB08914 11061-68-0 Insulin Human High molecular weight insulin humanHuman insulinhuman insulin (rDNA)Insulin (human)Insulin human [rDNA origin]Insulin Human RegularInsulin human regular (rDNA)Insulin human, rDNA originInsulin recombinant humanInsulin recombinant purified humanInsulin regularInsulin, humanRegular Insulin, human biotech 1Y17CTI5SR Humulin is synthesized in a special non-disease-producing laboratory strain of Escherichia coli bacteria that has been genetically altered to produce human insulin. //s3-us-west-2.amazonaws.com/drugbank/msds/DB00030.pdf?1370754402 liquid Insulin human is a 51 residue peptide hormone, composed of two amino acid chains covalently linked by disulfide bonds. The structure is identical to native human insulin. Recombinant insulin is synthesized by recombinant DNA techncology. Inserting the human insulin gene into the Escherichia coli bacteria or Saccharomyces cerevisiae produces insulin for human use.Inhalable insulin is a powdered form of insulin regular, delivered with a nebulizer into the lungs where it is absorbed. Exubera, developed by Inhale Therapeutics (later named Nektar Therapeutics), became the first inhaled insulin product to be marketed in 2006 by Pfizer, but poor sales led Pfizer to withdraw it in 2007. Afrezza, a monomeric inhaled insulin developed by Mannkind, was approved by the FDA in 2014. Humans and other mammals KitPowder, meteredPowder, meteredPowder, meteredSolutionInjection, solutionInjection, solutionSolutionInjection, solutionInjection, suspensionInjection, suspensionInjection, solutionInjection, solutionInjection, solutionInjection, solutionInjection, suspensionSuspensionSuspensionSolutionInjection, suspensionLiquid Respiratory (inhalation)Respiratory (inhalation)Respiratory (inhalation)SubcutaneousParenteralSubcutaneousIntramuscular; SubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntraperitonealSubcutaneousSubcutaneousSubcutaneousIntramuscular; Intravenous; SubcutaneousSubcutaneousIntramuscular; Intravenous; Subcutaneous 12 1/14 1/18 1/1500 unit100 [iU]/mL100 [iU]/mL100 unit500 [iU]/mL100 IU/ml40 IU/ml100 IU/ml100 IU/ml40 IU/ml400 IU/ml100 [USP'U]/mL100 unit100 unit100 [iU]/mL100 unit Indicated as an adjunct to diet and exercise to improve glycemic control in adults and children with type 1 and type 2 diabetes mellitus. The primary activity of insulin is the regulation of glucose metabolism. Insulin promotes glucose and amino acid uptake into muscle and adipose tissues, and other tissues except brain and liver. It also has an anabolic role in stimulating glycogen, fatty acid, and protein synthesis. Insulin inhibits gluconeogenesis in the liver.Insulin binds to the insulin receptor (IR), a heterotetrameric protein consisting of two extracellular alpha units and two transmembrane beta units. The binding of insulin to the alpha subunit of IR stimulates the tyrosine kinase activity intrinsic to the beta subunit of the receptor. The bound receptor is able to autophosphorylate and phosphorylate numerous intracellular substrates such as insulin receptor substrates (IRS) proteins, Cbl, APS, Shc and Gab 1. These activated proteins, in turn, lead to the activation of downstream signaling molecules including PI3 kinase and Akt. Akt regulates the activity of glucose transporter 4 (GLUT4) and protein kinase C (PKC) which play a critical role in metabolism and catabolism. agonist Insulin receptorInsulin-like growth factor 1 receptorRetinoblastoma-associated proteinCathepsin DInsulin-degrading enzymeNeuroendocrine convertase 2Carboxypeptidase ENeuroendocrine convertase 1Protein NOV homologLow-density lipoprotein receptor-related protein 2Insulin-like growth factor-binding protein 7Synaptotagmin-like protein 4 BE0000033BE0000858BE0002123BE0000941BE0001183BE0002124BE0001123BE0002125BE0001147BE0000942BE0002126BE0002127 HumanHumanHumanHumanHumanHumanHumanHumanHumanHumanHumanHuman Desbuquois B, Chauvet G, Kouach M, Authier F: Cell itinerary and metabolic fate of proinsulin in rat liver: in vivo and in vitro studies. Endocrinology. 2003 Dec;144(12):5308-21. Epub 2003 Sep 11.Chen LM, Yang XW, Tang JG: Acidic residues on the N-terminus of proinsulin C-Peptide are important for the folding of insulin precursor. J Biochem. 2002 Jun;131(6):855-9.Bell DS: Insulin therapy in diabetes mellitus: how can the currently available injectable insulins be most prudently and efficaciously utilised? Drugs. 2007;67(13):1813-27.Tanti JF, Jager J: Cellular mechanisms of insulin resistance: role of stress-regulated serine kinases and insulin receptor substrates (IRS) serine phosphorylation. Curr Opin Pharmacol. 2009 Dec;9(6):753-62. doi: 10.1016/j.coph.2009.07.004. Epub 2009 Aug 13.Chiu SL, Cline HT: Insulin receptor signaling in the development of neuronal structure and function. Neural Dev. 2010 Mar 15;5:7. doi: 10.1186/1749-8104-5-7.Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. 12970169120389821772295219683471202306161175235217139284170164231713928417016423171392841701642317139284170164231713928417016423171392841701642317139284170164231713928417016423171392841701642317139284170164231713928417016423 P06213P08069P06400P07339P14735P16519P16870P29120P48745P98164Q16270Q96C24 Insulin receptorInsulin-like growth factor 1 receptorRetinoblastoma-associated proteinCathepsin DInsulin-degrading enzymeNeuroendocrine convertase 2Carboxypeptidase ENeuroendocrine convertase 1Protein NOV homologLow-density lipoprotein receptor-related protein 2Insulin-like growth factor-binding protein 7Synaptotagmin-like protein 4 19p13.3-p13.215q26.313q14.211p15.510q23-q2520p11.24q32.35q15-q218q24.12q24-q314q12- HumanHumanHumanHumanHumanHumanHumanHumanHumanHumanHumanHuman membraneinsulin receptor complexcaveolaplasma membranereceptor complexintegral component of plasma membraneendosome membraneextracellular exosomeintracellular membrane-bounded organelleinsulin bindingprotein tyrosine kinase activityinsulin-like growth factor II bindingATP bindingPTB domain bindingGTP bindinginsulin-activated receptor activityinsulin-like growth factor receptor bindingphosphatidylinositol 3-kinase bindingreceptor signaling protein tyrosine kinase activityinsulin receptor substrate bindinginsulin-like growth factor I bindingpositive regulation of respiratory burstG-protein coupled receptor signaling pathwayprotein heterotetramerizationexocrine pancreas developmentpositive regulation of cell proliferationpositive regulation of MAPK cascadepeptidyl-tyrosine autophosphorylationepidermis developmentmale sex determinationpeptidyl-tyrosine phosphorylationpositive regulation of glycolytic processpositive regulation of meiotic cell cyclepositive regulation of protein phosphorylationcellular response to insulin stimulusregulation of female gonad developmentpositive regulation of protein kinase B signalingregulation of transcription, DNA-templatedpositive regulation of glucose importpositive regulation of DNA replicationtransformation of host cell by viruscellular response to growth factor stimuluspositive regulation of glycogen biosynthetic processadrenal gland developmentregulation of embryonic developmentactivation of protein kinase B activitypositive regulation of cell migrationpositive regulation of developmental growthpositive regulation of mitotic nuclear divisionpositive regulation of transcription, DNA-templatedprotein autophosphorylationpositive regulation of nitric oxide biosynthetic processsignal transduction by protein phosphorylationactivation of MAPK activitycarbohydrate metabolic processheart morphogenesisinsulin receptor signaling pathwayactivation of protein kinase activitymale gonad developmentglucose homeostasismembraneintracellular membrane-bounded organelleplasma membranereceptor complexneuron projectioncaveolaintegral component of plasma membraneidentical protein bindinginsulin receptor substrate bindingATP bindinginsulin-like growth factor-activated receptor activityinsulin bindinginsulin-like growth factor bindinginsulin-like growth factor I bindinginsulin receptor bindingphosphatidylinositol 3-kinase bindingprotein tyrosine kinase activitypositive regulation of DNA replicationinsulin-like growth factor receptor signaling pathwayaxonogenesissignal transductionpositive regulation of protein kinase B signalingestablishment of cell polaritypositive regulation of cell migrationbrain developmentmammary gland developmentphosphatidylinositol-mediated signalingimmune responsepositive regulation of cytokinesisexocrine pancreas developmentprotein tetramerizationpositive regulation of mitotic nuclear divisionphosphatidylinositol 3-kinase signalinginactivation of MAPKK activityinsulin receptor signaling pathwayprotein autophosphorylationnegative regulation of muscle cell apoptotic processnegative regulation of apoptotic processprotein heterooligomerizationpositive regulation of cell proliferationprostate gland epithelium morphogenesisresponse to vitamin Epositive regulation of MAPK cascaderegulation of JNK cascadeepidermis developmentnegative regulation of sequence-specific DNA binding transcription factor activitypeptidyl-tyrosine autophosphorylationnegative regulation of protein kinase B signalingmale sex determinationpositive regulation of steroid hormone biosynthetic processnucleusPML bodychromatinSWI/SNF complexspindlenucleoplasmRb-E2F complextranscription factor activity, sequence-specific DNA bindingDNA bindingphosphoprotein bindingubiquitin protein ligase bindingtranscription factor bindingcore promoter bindingtranscription coactivator activityandrogen receptor bindingidentical protein bindingkinase bindingnegative regulation of transcription involved in G1/S transition of mitotic cell cyclemaintenance of mitotic sister chromatid cohesionandrogen receptor signaling pathwaypositive regulation of transcription from RNA polymerase II promoterskeletal muscle cell differentiationnegative regulation of sequence-specific DNA binding transcription factor activitycell cycle checkpointnegative regulation of transcription from RNA polymerase II promoter during mitosisRas protein signal transductionprotein localization to chromosome, centromeric regionnegative regulation of transcription, DNA-templatedregulation of centromere complex assemblyneuron maturationviral processregulation of lipid kinase activitypositive regulation of macrophage differentiationregulation of cohesin localization to chromatinmitotic cell cycleregulation of transcription involved in G1/S transition of mitotic cell cyclecell cycle arrestsister chromatid biorientationregulation of mitotic cell cycleneuron projection developmentmyoblast differentiationcell divisionmitotic cell cycle checkpointneuron apoptotic processdigestive tract developmentchromatin remodelingnegative regulation of G1/S transition of mitotic cell cycletranscription, DNA-templatednegative regulation of epithelial cell proliferationnegative regulation of protein kinase activityG1/S transition of mitotic cell cyclepositive regulation of mitotic metaphase/anaphase transitionhepatocyte apoptotic processnegative regulation of smoothened signaling pathwaycellular response to xenobiotic stimuluscell morphogenesis involved in neuron differentiationenucleate erythrocyte differentiationglial cell apoptotic processpositive regulation of transcription, DNA-templatedstriated muscle cell differentiationmembrane raftextracellular regionlysosomal lumenmelanosomeextracellular spacelysosomeextracellular exosomeaspartic-type endopeptidase activityproteolysisprotein catabolic processautophagycollagen catabolic processextracellular matrix disassemblyextracellular matrix organizationantigen processing and presentation of exogenous peptide antigen via MHC class IIperoxisomal matrixcell surfacecytoplasmcytosolic proteasome complexmitochondrionperoxisomecytosolnucleoplasmnucleusplasma membraneextracellular spacezinc ion bindingvirus receptor activitybeta-endorphin bindingATP bindinginsulin bindingprotein homodimerization activitybeta-amyloid bindingmetalloendopeptidase activityglycoprotein bindingubiquitin bindingATPase activityreceptor bindingpeptide bindinghormone catabolic processdetermination of adult lifespanprotein processingprotein heterooligomerizationbeta-amyloid metabolic processprotein homooligomerizationproteolysisinsulin catabolic processinsulin metabolic processinsulin receptor signaling pathwayubiquitin homeostasisnegative regulation of proteolysispositive regulation of protein oligomerizationprotein homotetramerizationproteolysis involved in cellular protein catabolic processbradykinin catabolic processmembraneextracellular spacedendriteperikaryonsecretory granule lumentransport vesicleserine-type endopeptidase activityinsulin processingislet amyloid polypeptide processingproteolysisprotein autoprocessingcellular protein metabolic processnervous system developmentenkephalin processingnucleusneuronal cell bodysecretory granule membraneplasma membranetransport vesicle membraneextracellular spacesynaptic membraneGolgi apparatusextracellular exosomesecretory granulezinc ion bindingserine-type carboxypeptidase activitycarboxypeptidase activitycell adhesion molecule bindingmetallocarboxypeptidase activityneurexin family protein bindingcardiac left ventricle morphogenesiscellular protein metabolic processprotein localization to membraneWnt signaling pathwayneuropeptide signaling pathwayinsulin processingcellular protein modification processmetabolic processextracellular spaceGolgi apparatussecretory granule lumentransport vesicleserine-type endopeptidase activitypeptide biosynthetic processproteolysiscell-cell signalingcellular protein metabolic processregulation of insulin secretionmetabolic processpeptide hormone processingcytoplasmneuronal cell bodyextracellular regionproteinaceous extracellular matrixgap junctionaxonintracellular membrane-bounded organelledendriteintegrin bindingheparin bindingNotch bindingsmooth muscle cell migrationbone regenerationangiogenesissignal transductionendothelial cell chemotaxisnegative regulation of myotube differentiationcell adhesionnegative regulation of monocyte chemotaxisnegative regulation of NF-kappaB import into nucleusnegative regulation of sensory perception of painnegative regulation of insulin secretioncell-cell signalingnegative regulation of SMAD protein import into nucleusfibroblast migrationsmooth muscle cell proliferationnegative regulation of chondrocyte proliferationnegative regulation of cell growthcell adhesion mediated by integrinnegative regulation of cell deathendothelial cell-cell adhesionregulation of gene expressiontype B pancreatic cell proliferationpositive regulation of Notch signaling pathwaycell chemotaxischondrocyte differentiationhematopoietic stem cell homeostasisnegative regulation of inflammatory responseendoplasmic reticulumplasma membranereceptor complexendosomelysosomecoated pitapical plasma membranebrush border membraneGolgi apparatusendocytic vesicleintegral component of membranelysosomal membraneextracellular exosomecalcium ion bindingretinoid metabolic processreceptor-mediated endocytosisforebrain developmentsteroid metabolic processendocytosislipid metabolic processvitamin D metabolic processphototransduction, visible lightcell proliferationsmall molecule metabolic processprotein glycosylationextracellular regionextracellular spaceextracellular exosomecell adhesionregulation of cell growthnegative regulation of cell proliferationexocytic vesiclecytoplasmextrinsic component of membraneplasma membranesecretory granule membranetransport vesicle membranenucleoplasmcentrosomeendosomeapical plasma membranezinc ion bindingclathrin bindingneurexin family protein bindingcalcium ion bindingphospholipid bindingcalcium-dependent phospholipid bindingsyntaxin bindingnegative regulation of insulin secretioncalcium ion-dependent exocytosis of neurotransmitterregulation of calcium ion-dependent exocytosismultivesicular body sorting pathwayintracellular protein transportsynaptic vesicle exocytosispositive regulation of protein secretionpositive regulation of exocytosisvesicle fusion Receptor signaling protein tyrosine kinase activityProtein tyrosine kinase activityUbiquitin protein ligase bindingAspartic-type endopeptidase activityZinc ion bindingSerine-type endopeptidase activityZinc ion bindingSerine-type endopeptidase activityNotch bindingCalcium ion bindingZinc ion binding Receptor tyrosine kinase which mediates the pleiotropic actions of insulin. Binding of insulin leads to phosphorylation of several intracellular substrates, including, insulin receptor substrates (IRS1, 2, 3, 4), SHC, GAB1, CBL and other signaling intermediates. Each of these phosphorylated proteins serve as docking proteins for other signaling proteins that contain Src-homology-2 domains (SH2 domain) that specifically recognize different phosphotyrosines residues, including the p85 regulatory subunit of PI3K and SHP2. Phosphorylation of IRSs proteins lead to the activation of two main signaling pathways: the PI3K-AKT/PKB pathway, which is responsible for most of the metabolic actions of insulin, and the Ras-MAPK pathway, which regulates expression of some genes and cooperates with the PI3K pathway to control cell growth and differentiation. Binding of the SH2 domains of PI3K to phosphotyrosines on IRS1 leads to the activation of PI3K and the generation of phosphatidylinositol-(3, 4, 5)-triphosphate (PIP3), a lipid second messenger, which activates several PIP3-dependent serine/threonine kinases, such as PDPK1 and subsequently AKT/PKB. The net effect of this pathway is to produce a translocation of the glucose transporter SLC2A4/GLUT4 from cytoplasmic vesicles to the cell membrane to facilitate glucose transport. Moreover, upon insulin stimulation, activated AKT/PKB is responsible for: anti-apoptotic effect of insulin by inducing phosphorylation of BAD; regulates the expression of gluconeogenic and lipogenic enzymes by controlling the activity of the winged helix or forkhead (FOX) class of transcription factors. Another pathway regulated by PI3K-AKT/PKB activation is mTORC1 signaling pathway which regulates cell growth and metabolism and integrates signals from insulin. AKT mediates insulin-stimulated protein synthesis by phosphorylating TSC2 thereby activating mTORC1 pathway. The Ras/RAF/MAP2K/MAPK pathway is mainly involved in mediating cell growth, survival and cellular differentiation of insulin. Phosphorylated IRS1 recruits GRB2/SOS complex, which triggers the activation of the Ras/RAF/MAP2K/MAPK pathway. In addition to binding insulin, the insulin receptor can bind insulin-like growth factors (IGFI and IGFII). Isoform Short has a higher affinity for IGFII binding. When present in a hybrid receptor with IGF1R, binds IGF1. PubMed:12138094 shows that hybrid receptors composed of IGF1R and INSR isoform Long are activated with a high affinity by IGF1, with low affinity by IGF2 and not significantly activated by insulin, and that hybrid receptors composed of IGF1R and INSR isoform Short are activated by IGF1, IGF2 and insulin. In contrast, PubMed:16831875 shows that hybrid receptors composed of IGF1R and INSR isoform Long and hybrid receptors composed of IGF1R and INSR isoform Short have similar binding characteristics, both bind IGF1 and have a low affinity for insulin.Receptor tyrosine kinase which mediates actions of insulin-like growth factor 1 (IGF1). Binds IGF1 with high affinity and IGF2 and insulin (INS) with a lower affinity. The activated IGF1R is involved in cell growth and survival control. IGF1R is crucial for tumor transformation and survival of malignant cell. Ligand binding activates the receptor kinase, leading to receptor autophosphorylation, and tyrosines phosphorylation of multiple substrates, that function as signaling adapter proteins including, the insulin-receptor substrates (IRS1/2), Shc and 14-3-3 proteins. Phosphorylation of IRSs proteins lead to the activation of two main signaling pathways: the PI3K-AKT/PKB pathway and the Ras-MAPK pathway. The result of activating the MAPK pathway is increased cellular proliferation, whereas activating the PI3K pathway inhibits apoptosis and stimulates protein synthesis. Phosphorylated IRS1 can activate the 85 kDa regulatory subunit of PI3K (PIK3R1), leading to activation of several downstream substrates, including protein AKT/PKB. AKT phosphorylation, in turn, enhances protein synthesis through mTOR activation and triggers the antiapoptotic effects of IGFIR through phosphorylation and inactivation of BAD. In parallel to PI3K-driven signaling, recruitment of Grb2/SOS by phosphorylated IRS1 or Shc leads to recruitment of Ras and activation of the ras-MAPK pathway. In addition to these two main signaling pathways IGF1R signals also through the Janus kinase/signal transducer and activator of transcription pathway (JAK/STAT). Phosphorylation of JAK proteins can lead to phosphorylation/activation of signal transducers and activators of transcription (STAT) proteins. In particular activation of STAT3, may be essential for the transforming activity of IGF1R. The JAK/STAT pathway activates gene transcription and may be responsible for the transforming activity. JNK kinases can also be activated by the IGF1R. IGF1 exerts inhibiting activities on JNK activation via phosphorylation and inhibition of MAP3K5/ASK1, which is able to directly associate with the IGF1R.When present in a hybrid receptor with INSR, binds IGF1. PubMed:12138094 shows that hybrid receptors composed of IGF1R and INSR isoform Long are activated with a high affinity by IGF1, with low affinity by IGF2 and not significantly activated by insulin, and that hybrid receptors composed of IGF1R and INSR isoform Short are activated by IGF1, IGF2 and insulin. In contrast, PubMed:16831875 shows that hybrid receptors composed of IGF1R and INSR isoform Long and hybrid receptors composed of IGF1R and INSR isoform Short have similar binding characteristics, both bind IGF1 and have a low affinity for insulin.Key regulator of entry into cell division that acts as a tumor suppressor. Promotes G0-G1 transition when phosphorylated by CDK3/cyclin-C. Acts as a transcription repressor of E2F1 target genes. The underphosphorylated, active form of RB1 interacts with E2F1 and represses its transcription activity, leading to cell cycle arrest. Directly involved in heterochromatin formation by maintaining overall chromatin structure and, in particular, that of constitutive heterochromatin by stabilizing histone methylation. Recruits and targets histone methyltransferases SUV39H1, SUV420H1 and SUV420H2, leading to epigenetic transcriptional repression. Controls histone H4 'Lys-20' trimethylation. Inhibits the intrinsic kinase activity of TAF1. Mediates transcriptional repression by SMARCA4/BRG1 by recruiting a histone deacetylase (HDAC) complex to the c-FOS promoter. In resting neurons, transcription of the c-FOS promoter is inhibited by BRG1-dependent recruitment of a phospho-RB1-HDAC1 repressor complex. Upon calcium influx, RB1 is dephosphorylated by calcineurin, which leads to release of the repressor complex (By similarity). In case of viral infections, interactions with SV40 large T antigen, HPV E7 protein or adenovirus E1A protein induce the disassembly of RB1-E2F1 complex thereby disrupting RB1's activity.Acid protease active in intracellular protein breakdown. Involved in the pathogenesis of several diseases such as breast cancer and possibly Alzheimer disease.Plays a role in the cellular breakdown of insulin, IAPP, glucagon, bradykinin, kallidin and other peptides, and thereby plays a role in intercellular peptide signaling. Degrades amyloid formed by APP and IAPP. May play a role in the degradation and clearance of naturally secreted amyloid beta-protein by neurons and microglia.(Microbial infection) The membrane-associated isoform acts as an entry receptor for varicella-zoster virus (VZV).Involved in the processing of hormone and other protein precursors at sites comprised of pairs of basic amino acid residues. Responsible for the release of glucagon from proglucagon in pancreatic A cells.Removes residual C-terminal Arg or Lys remaining after initial endoprotease cleavage during prohormone processing. Processes proinsulin.Involved in the processing of hormone and other protein precursors at sites comprised of pairs of basic amino acid residues. Substrates include POMC, renin, enkephalin, dynorphin, somatostatin, insulin and AGRP.Immediate-early protein playing a role in various cellular processes including proliferation, adhesion, migration, differentiation and survival (PubMed:15181016, PubMed:15611078, PubMed:12695522, PubMed:21344378, PubMed:12050162). Acts by binding to integrins or membrane receptors such as NOTCH1 (PubMed:12695522, PubMed:21344378, PubMed:15611078). Essential regulator of hematopoietic stem and progenitor cell function (PubMed:17463287). Inhibits myogenic differentiation through the activation of Notch-signaling pathway (PubMed:12050162). Inhibits vascular smooth muscle cells proliferation by increasing expression of cell-cycle regulators such as CDKN2B or CDKN1A independently of TGFB1 signaling (PubMed:20139355). Ligand of integrins ITGAV:ITGB3 and ITGA5:ITGB1, acts directly upon endothelial cells to stimulate pro-angiogenic activities and induces angiogenesis. In endothelial cells, supports cell adhesion, induces directed cell migration (chemotaxis) and promotes cell survival (PubMed:12695522). Plays also a role in cutaneous wound healing acting as integrin receptor ligand. Supports skin fibroblast adhesion through ITGA5:ITGB1 and ITGA6:ITGB1 and induces fibroblast chemotaxis through ITGAV:ITGB5. Seems to enhance bFGF-induced DNA synthesis in fibroblasts (PubMed:15611078). Involved in bone regeneration as a negative regulator (By similarity). Enhances the articular chondrocytic phenotype, whereas it repressed the one representing endochondral ossification (PubMed:21871891). Impairs pancreatic beta-cell function, inhibits beta-cell proliferation and insulin secretion (By similarity). Plays a role as negative regulator of endothelial pro-inflammatory activation reducing monocyte adhesion, its anti-inflammatory effects occur secondary to the inhibition of NF-kappaB signaling pathway (PubMed:21063504). Contributes to the control and coordination of inflammatory processes in atherosclerosis (By similarity). Attenuates inflammatory pain through regulation of IL1B- and TNF-induced MMP9, MMP2 and CCL2 expression. Inhibits MMP9 expression through ITGB1 engagement (PubMed:21871891).Acts together with cubilin to mediate HDL endocytosis (By similarity). May participate in regulation of parathyroid-hormone and para-thyroid-hormone-related protein release.Binds IGF-I and IGF-II with a relatively low affinity. Stimulates prostacyclin (PGI2) production. Stimulates cell adhesion.Modulates exocytosis of dense-core granules and secretion of hormones in the pancreas and the pituitary. Interacts with vesicles containing negatively charged phospholipids in a Ca(2+)-independent manner (By similarity). 5% protein bound Hypoglycemia is one of the most frequent adverse events experienced by insulin users. Insulin is generally well absorbed. Insulin is predominantly cleared by metabolic degradation via a receptor-mediated process. 0.15 L/kg Insulin regular is a short-acting insulin. When subcutaneously administered, the onset of action (as evidenced by a decrease in glucose level) occurs 30 minutes post-dose. Maximal effect occurs between 1.5 and 3.5 hours post-dose. The glucose-lowering effect occurs 8 hours post-dose. Compared to other rapid-acting insulin analogs, insulin regular has a slower onset of action and longer duration of action. The risk or severity of heart failure can be increased when Pregabalin is combined with Insulin Human.Sitagliptin may increase the hypoglycemic activities of Insulin Human.Vildagliptin may increase the hypoglycemic activities of Insulin Human.Alogliptin may increase the hypoglycemic activities of Insulin Human.Saxagliptin may increase the hypoglycemic activities of Insulin Human.Atorvastatin may increase the hypoglycemic activities of Insulin Human.Linagliptin may increase the hypoglycemic activities of Insulin Human.Exenatide may increase the hypoglycemic activities of Insulin Human.Albiglutide may increase the hypoglycemic activities of Insulin Human.Dulaglutide may increase the hypoglycemic activities of Insulin Human.Canagliflozin may increase the hypoglycemic activities of Insulin Human.Empagliflozin may increase the hypoglycemic activities of Insulin Human.The serum concentration of Insulin Human can be decreased when it is combined with Medrogestone.Ertugliflozin may increase the hypoglycemic activities of Insulin Human.Liraglutide may increase the hypoglycemic activities of Insulin Human.Metreleptin may increase the hypoglycemic activities of Insulin Human.The risk or severity of adverse effects can be increased when Pioglitazone is combined with Insulin Human.Pramlintide may increase the hypoglycemic activities of Insulin Human.Lipoic Acid may increase the hypoglycemic activities of Insulin Human.Edetic Acid may increase the hypoglycemic activities of Insulin Human.Insulin Human may increase the hypoglycemic activities of Insulin Lispro.Insulin Human may increase the hypoglycemic activities of Insulin Glargine.Insulin Human may increase the hypoglycemic activities of Octreotide.Insulin Human may increase the hypoglycemic activities of Glimepiride.Insulin Human may increase the hypoglycemic activities of Sulfisoxazole.Insulin Human may increase the hypoglycemic activities of Disopyramide.Insulin Human may increase the hypoglycemic activities of Sulfadiazine.Insulin Human may increase the hypoglycemic activities of Quinine.Insulin Human may increase the hypoglycemic activities of Chlorpropamide.Insulin Human may increase the hypoglycemic activities of Nateglinide.Insulin Human may increase the hypoglycemic activities of Pentamidine.Insulin Human may increase the hypoglycemic activities of Mifepristone.Insulin Human may increase the hypoglycemic activities of Tolazamide.Insulin Human may increase the hypoglycemic activities of Repaglinide.Insulin Human may increase the hypoglycemic activities of Sulfamethoxazole.Insulin Human may increase the hypoglycemic activities of Glyburide.Insulin Human may increase the hypoglycemic activities of Glipizide.Insulin Human may increase the hypoglycemic activities of Gliclazide.Insulin Human may increase the hypoglycemic activities of Tolbutamide.Insulin Human may increase the hypoglycemic activities of Sunitinib.Insulin Human may increase the hypoglycemic activities of Mecasermin.Insulin Human may increase the hypoglycemic activities of Insulin Aspart.Insulin Human may increase the hypoglycemic activities of Insulin Detemir.Insulin Human may increase the hypoglycemic activities of Insulin Glulisine.Insulin Human may increase the hypoglycemic activities of Pasireotide.Insulin Human may increase the hypoglycemic activities of Lanreotide.Tranylcypromine may increase the hypoglycemic activities of Insulin Human.Phenelzine may increase the hypoglycemic activities of Insulin Human.Selegiline may increase the hypoglycemic activities of Insulin Human.Moclobemide may increase the hypoglycemic activities of Insulin Human.Isocarboxazid may increase the hypoglycemic activities of Insulin Human.Rasagiline may increase the hypoglycemic activities of Insulin Human.Pargyline may increase the hypoglycemic activities of Insulin Human.Minaprine may increase the hypoglycemic activities of Insulin Human.Iproniazid may increase the hypoglycemic activities of Insulin Human.Nialamide may increase the hypoglycemic activities of Insulin Human.Pirlindole may increase the hypoglycemic activities of Insulin Human.Toloxatone may increase the hypoglycemic activities of Insulin Human.Hydracarbazine may increase the hypoglycemic activities of Insulin Human.Methylene blue may increase the hypoglycemic activities of Insulin Human.Benmoxin may increase the hypoglycemic activities of Insulin Human.Iproclozide may increase the hypoglycemic activities of Insulin Human.Mebanazine may increase the hypoglycemic activities of Insulin Human.Octamoxin may increase the hypoglycemic activities of Insulin Human.Pheniprazine may increase the hypoglycemic activities of Insulin Human.Phenoxypropazine may increase the hypoglycemic activities of Insulin Human.Pivhydrazine may increase the hypoglycemic activities of Insulin Human.Safrazine may increase the hypoglycemic activities of Insulin Human.Caroxazone may increase the hypoglycemic activities of Insulin Human.Furazolidone may increase the hypoglycemic activities of Insulin Human.Trans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Insulin Human.7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypoglycemic activities of Insulin Human.Harmaline may increase the hypoglycemic activities of Insulin Human.Brofaromine may increase the hypoglycemic activities of Insulin Human.Amphetamine may increase the hypoglycemic activities of Insulin Human.Procarbazine may increase the hypoglycemic activities of Insulin Human.The therapeutic efficacy of Insulin Human can be increased when used in combination with Ubidecarenone.Esmolol may increase the hypoglycemic activities of Insulin Human.Betaxolol may increase the hypoglycemic activities of Insulin Human.Metoprolol may increase the hypoglycemic activities of Insulin Human.Atenolol may increase the hypoglycemic activities of Insulin Human.Timolol may increase the hypoglycemic activities of Insulin Human.Carteolol may increase the hypoglycemic activities of Insulin Human.Propranolol may increase the hypoglycemic activities of Insulin Human.Labetalol may increase the hypoglycemic activities of Insulin Human.Bisoprolol may increase the hypoglycemic activities of Insulin Human.Pindolol may increase the hypoglycemic activities of Insulin Human.Carvedilol may increase the hypoglycemic activities of Insulin Human.Acebutolol may increase the hypoglycemic activities of Insulin Human.Nadolol may increase the hypoglycemic activities of Insulin Human.Sotalol may increase the hypoglycemic activities of Insulin Human.Nebivolol may increase the hypoglycemic activities of Insulin Human.Alprenolol may increase the hypoglycemic activities of Insulin Human.Bevantolol may increase the hypoglycemic activities of Insulin Human.Practolol may increase the hypoglycemic activities of Insulin Human.Penbutolol may increase the hypoglycemic activities of Insulin Human.Oxprenolol may increase the hypoglycemic activities of Insulin Human.Platelet Activating Factor may increase the hypoglycemic activities of Insulin Human.Celiprolol may increase the hypoglycemic activities of Insulin Human.Bufuralol may increase the hypoglycemic activities of Insulin Human.Bopindolol may increase the hypoglycemic activities of Insulin Human.Bupranolol may increase the hypoglycemic activities of Insulin Human.Indenolol may increase the hypoglycemic activities of Insulin Human.Befunolol may increase the hypoglycemic activities of Insulin Human.Arotinolol may increase the hypoglycemic activities of Insulin Human.Talinolol may increase the hypoglycemic activities of Insulin Human.Landiolol may increase the hypoglycemic activities of Insulin Human.Bucindolol may increase the hypoglycemic activities of Insulin Human.Cloranolol may increase the hypoglycemic activities of Insulin Human.Mepindolol may increase the hypoglycemic activities of Insulin Human.Epanolol may increase the hypoglycemic activities of Insulin Human.Tertatolol may increase the hypoglycemic activities of Insulin Human.Grepafloxacin may increase the hypoglycemic activities of Insulin Human.Enoxacin may increase the hypoglycemic activities of Insulin Human.Pefloxacin may increase the hypoglycemic activities of Insulin Human.Trovafloxacin may increase the hypoglycemic activities of Insulin Human.Nalidixic Acid may increase the hypoglycemic activities of Insulin Human.Rosoxacin may increase the hypoglycemic activities of Insulin Human.Cinoxacin may increase the hypoglycemic activities of Insulin Human.Gatifloxacin may increase the hypoglycemic activities of Insulin Human.Norfloxacin may increase the hypoglycemic activities of Insulin Human.Levofloxacin may increase the hypoglycemic activities of Insulin Human.Gemifloxacin may increase the hypoglycemic activities of Insulin Human.Sparfloxacin may increase the hypoglycemic activities of Insulin Human.Temafloxacin may increase the hypoglycemic activities of Insulin Human.Fleroxacin may increase the hypoglycemic activities of Insulin Human.Garenoxacin may increase the hypoglycemic activities of Insulin Human.Nemonoxacin may increase the hypoglycemic activities of Insulin Human.Flumequine may increase the hypoglycemic activities of Insulin Human.Pazufloxacin may increase the hypoglycemic activities of Insulin Human.Prulifloxacin may increase the hypoglycemic activities of Insulin Human.Sitafloxacin may increase the hypoglycemic activities of Insulin Human.Oxolinic acid may increase the hypoglycemic activities of Insulin Human.Piromidic acid may increase the hypoglycemic activities of Insulin Human.Rufloxacin may increase the hypoglycemic activities of Insulin Human.Pipemidic acid may increase the hypoglycemic activities of Insulin Human.Duloxetine may increase the hypoglycemic activities of Insulin Human.Nefazodone may increase the hypoglycemic activities of Insulin Human.Desvenlafaxine may increase the hypoglycemic activities of Insulin Human.Milnacipran may increase the hypoglycemic activities of Insulin Human.Venlafaxine may increase the hypoglycemic activities of Insulin Human.Levomilnacipran may increase the hypoglycemic activities of Insulin Human.Dapoxetine may increase the hypoglycemic activities of Insulin Human.Indalpine may increase the hypoglycemic activities of Insulin Human.Fluvoxamine may increase the hypoglycemic activities of Insulin Human.Citalopram may increase the hypoglycemic activities of Insulin Human.Fluoxetine may increase the hypoglycemic activities of Insulin Human.Paroxetine may increase the hypoglycemic activities of Insulin Human.Sertraline may increase the hypoglycemic activities of Insulin Human.Escitalopram may increase the hypoglycemic activities of Insulin Human.Zimelidine may increase the hypoglycemic activities of Insulin Human.Etoperidone may increase the hypoglycemic activities of Insulin Human.Alaproclate may increase the hypoglycemic activities of Insulin Human.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Methyclothiazide.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Chlorothiazide.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Hydrochlorothiazide.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Epitizide.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Chlorthalidone.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Bendroflumethiazide.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Metolazone.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Hydroflumethiazide.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Indapamide.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Trichlormethiazide.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Polythiazide.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Quinethazone.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Cyclopenthiazide.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Leuprolide.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Goserelin.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Torasemide.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Nelfinavir.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Indinavir.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Ziprasidone.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Etonogestrel.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Desogestrel.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Olanzapine.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Megestrol acetate.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Clozapine.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Levonorgestrel.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Progesterone.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Betamethasone.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Ritonavir.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Piperazine.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Medroxyprogesterone acetate.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Triamcinolone.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Niacin.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Prednisone.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Epinephrine.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Fludrocortisone.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Furosemide.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Norethisterone.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Risperidone.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Hydrocortisone.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Estradiol.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Ethynodiol diacetate.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Prednisolone.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Tacrolimus.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Sirolimus.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Bumetanide.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Etacrynic acid.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Tipranavir.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Norgestimate.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Methylprednisolone.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Ethinyl Estradiol.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Atazanavir.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Diazoxide.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Arsenic trioxide.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Quetiapine.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Saquinavir.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Dexamethasone.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Aripiprazole.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Darunavir.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Paliperidone.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Corticotropin.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Fosamprenavir.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Mestranol.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Cortisone acetate.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Drospirenone.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Methotrimeprazine.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Danazol.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Everolimus.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Lopinavir.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Pipotiazine.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Vorinostat.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Estrone sulfate.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Cyproterone acetate.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Nilotinib.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Iloperidone.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Asenapine.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Temsirolimus.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Buserelin.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Histrelin.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Hydroxyprogesterone caproate.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Triptorelin.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Lurasidone.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Dabrafenib.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Articaine.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Ceritinib.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Dienogest.The therapeutic efficacy of Insulin Human can be decreased when used in combination with Brexpiprazole.Testosterone may increase the hypoglycemic activities of Insulin Human.Stanolone may increase the hypoglycemic activities of Insulin Human.Fluoxymesterone may increase the hypoglycemic activities of Insulin Human.Testosterone propionate may increase the hypoglycemic activities of Insulin Human.Testosterone cypionate may increase the hypoglycemic activities of Insulin Human.Testosterone enanthate may increase the hypoglycemic activities of Insulin Human.Testosterone undecanoate may increase the hypoglycemic activities of Insulin Human.Oxandrolone may increase the hypoglycemic activities of Insulin Human.Oxymetholone may increase the hypoglycemic activities of Insulin Human.Stanozolol may increase the hypoglycemic activities of Insulin Human.GLPG-0492 may increase the hypoglycemic activities of Insulin Human.Nandrolone may increase the hypoglycemic activities of Insulin Human.Mesterolone may increase the hypoglycemic activities of Insulin Human.Methyltestosterone may increase the hypoglycemic activities of Insulin Human.Nandrolone decanoate may increase the hypoglycemic activities of Insulin Human.Pegvisomant may increase the hypoglycemic activities of Insulin Human.Insulin Pork may increase the hypoglycemic activities of Insulin Human.Troglitazone may increase the hypoglycemic activities of Insulin Human.Acarbose may increase the hypoglycemic activities of Insulin Human.Metformin may increase the hypoglycemic activities of Insulin Human.Rosiglitazone may increase the hypoglycemic activities of Insulin Human.Acetohexamide may increase the hypoglycemic activities of Insulin Human.Miglustat may increase the hypoglycemic activities of Insulin Human.Miglitol may increase the hypoglycemic activities of Insulin Human.Phenformin may increase the hypoglycemic activities of Insulin Human.Gliquidone may increase the hypoglycemic activities of Insulin Human.Mitiglinide may increase the hypoglycemic activities of Insulin Human.AICA ribonucleotide may increase the hypoglycemic activities of Insulin Human.Castanospermine may increase the hypoglycemic activities of Insulin Human.Buformin may increase the hypoglycemic activities of Insulin Human.Voglibose may increase the hypoglycemic activities of Insulin Human.Sulodexide may increase the hypoglycemic activities of Insulin Human.Glibornuride may increase the hypoglycemic activities of Insulin Human.Ciglitazone may increase the hypoglycemic activities of Insulin Human.Allicin may increase the hypoglycemic activities of Insulin Human.2,4-thiazolidinedione may increase the hypoglycemic activities of Insulin Human.Bempedoic acid may increase the hypoglycemic activities of Insulin Human.Gusperimus may increase the hypoglycemic activities of Insulin Human.Sotagliflozin may increase the hypoglycemic activities of Insulin Human.Balaglitazone may increase the hypoglycemic activities of Insulin Human.Deoxyspergualin may increase the hypoglycemic activities of Insulin Human.Carbutamide may increase the hypoglycemic activities of Insulin Human.Salicylic acid may increase the hypoglycemic activities of Insulin Human.Acetylsalicylic acid may increase the hypoglycemic activities of Insulin Human.Aminosalicylic Acid may increase the hypoglycemic activities of Insulin Human.Mesalazine may increase the hypoglycemic activities of Insulin Human.Diflunisal may increase the hypoglycemic activities of Insulin Human.Balsalazide may increase the hypoglycemic activities of Insulin Human.Olsalazine may increase the hypoglycemic activities of Insulin Human.Dersalazine may increase the hypoglycemic activities of Insulin Human.Nitroaspirin may increase the hypoglycemic activities of Insulin Human.Aloxiprin may increase the hypoglycemic activities of Insulin Human.Guacetisal may increase the hypoglycemic activities of Insulin Human.Carbaspirin calcium may increase the hypoglycemic activities of Insulin Human.Hemoglobin crosfumaril may increase the hypoglycemic activities of Insulin Human.Methyl salicylate may increase the hypoglycemic activities of Insulin Human.Trolamine salicylate may increase the hypoglycemic activities of Insulin Human.The risk or severity of myocardial ischemia can be increased when Insulin Human is combined with Rosiglitazone. DB00230DB01261DB04876DB06203DB06335DB01076DB08882DB01276DB09043DB09045DB08907DB09038DB09124DB11827DB06655DB09046DB01132DB01278DB00166DB00974DB00046DB00047DB00104DB00222DB00263DB00280DB00359DB00468DB00672DB00731DB00738DB00834DB00839DB00912DB01015DB01016DB01067DB01120DB01124DB01268DB01277DB01306DB01307DB01309DB06663DB06791DB00752DB00780DB01037DB01171DB01247DB01367DB01626DB00805DB04818DB04820DB09244DB09245DB09243DB09241DB09246DB09247DB09248DB09249DB09250DB09251DB09252DB09253DB09254DB00614DB02665DB08550DB13875DB13876DB00182DB01168DB09270DB00187DB00195DB00264DB00335DB00373DB00521DB00571DB00598DB00612DB00960DB01136DB01193DB01203DB00489DB04861DB00866DB01295DB01297DB01359DB01580DB02261DB04846DB06726DB08807DB08808DB08952DB09013DB09204DB11770DB12212DB12752DB13508DB13530DB13757DB13775DB00365DB00467DB00487DB00685DB00779DB00817DB00827DB01044DB01059DB01137DB01155DB01208DB01405DB04576DB06160DB06600DB08972DB11774DB11892DB13261DB13627DB13744DB13772DB13823DB00476DB01149DB06700DB04896DB00285DB08918DB04884DB08953DB00176DB00215DB00472DB00715DB01104DB01175DB04832DB09194DB13233DB00232DB00880DB00999DB13989DB00310DB00436DB00524DB00774DB00808DB01021DB01324DB01325DB13532DB00007DB00014DB00214DB00220DB00224DB00246DB00294DB00304DB00334DB00351DB00363DB00367DB00396DB00443DB00503DB00592DB00603DB00620DB00627DB00635DB00668DB00687DB00695DB00717DB00734DB00741DB00783DB00823DB00860DB00864DB00877DB00887DB00903DB00932DB00957DB00959DB00977DB01072DB01119DB01169DB01224DB01232DB01234DB01238DB01264DB01267DB01285DB01319DB01357DB01380DB01395DB01403DB01406DB01590DB01601DB01621DB02546DB04574DB04839DB04868DB04946DB06216DB06287DB06719DB06788DB06789DB06825DB08815DB08912DB09009DB09063DB09123DB09128DB00624DB02901DB01185DB01420DB13943DB13944DB13946DB00621DB06412DB06718DB12461DB13169DB13587DB06710DB08804DB00082DB00071DB00197DB00284DB00331DB00412DB00414DB00419DB00491DB00914DB01251DB01252DB01700DB01816DB04830DB04878DB06271DB08962DB09201DB11780DB11898DB11936DB12692DB12713DB12781DB12991DB13406DB00936DB00945DB00233DB00244DB00861DB01014DB01250DB06251DB12445DB13509DB13538DB13612DB13864DB09543DB11079DB00412 PregabalinSitagliptinVildagliptinAlogliptinSaxagliptinAtorvastatinLinagliptinExenatideAlbiglutideDulaglutideCanagliflozinEmpagliflozinMedrogestoneErtugliflozinLiraglutideMetreleptinPioglitazonePramlintideLipoic AcidEdetic AcidInsulin LisproInsulin GlargineOctreotideGlimepirideSulfisoxazoleDisopyramideSulfadiazineQuinineChlorpropamideNateglinidePentamidineMifepristoneTolazamideRepaglinideSulfamethoxazoleGlyburideGlipizideGliclazideTolbutamideSunitinibMecaserminInsulin AspartInsulin DetemirInsulin GlulisinePasireotideLanreotideTranylcyprominePhenelzineSelegilineMoclobemideIsocarboxazidRasagilinePargylineMinaprineIproniazidNialamidePirlindoleToloxatoneHydracarbazineMethylene blueBenmoxinIproclozideMebanazineOctamoxinPheniprazinePhenoxypropazinePivhydrazineSafrazineCaroxazoneFurazolidone(1R,2S)-2-Phenylcyclopropanaminium7,8-Dichloro-1,2,3,4-tetrahydroisoquinolineHarmalineBrofaromineAmphetamineProcarbazineUbidecarenoneEsmololBetaxololMetoprololAtenololTimololCarteololPropranololLabetalolBisoprololPindololCarvedilolAcebutololNadololSotalolNebivololAlprenololBevantololPractololPenbutololOxprenololPlatelet Activating FactorCeliprololBufuralolBopindololBupranololIndenololBefunololArotinololTalinololLandiololBucindololCloranololMepindololEpanololTertatololGrepafloxacinEnoxacinPefloxacinTrovafloxacinNalidixic AcidRosoxacinCinoxacinGatifloxacinNorfloxacinLevofloxacinGemifloxacinSparfloxacinTemafloxacinFleroxacinGarenoxacinNemonoxacinFlumequinePazufloxacinPrulifloxacinSitafloxacinOxolinic acidPiromidic acidRufloxacinPipemidic acidDuloxetineNefazodoneDesvenlafaxineMilnacipranVenlafaxineLevomilnacipranDapoxetineIndalpineFluvoxamineCitalopramFluoxetineParoxetineSertralineEscitalopramZimelidineEtoperidoneAlaproclateMethyclothiazideChlorothiazideHydrochlorothiazideEpitizideChlorthalidoneBendroflumethiazideMetolazoneHydroflumethiazideIndapamideTrichlormethiazidePolythiazideQuinethazoneCyclopenthiazideLeuprolideGoserelinTorasemideNelfinavirIndinavirZiprasidoneEtonogestrelDesogestrelOlanzapineMegestrol acetateClozapineLevonorgestrelProgesteroneBetamethasoneRitonavirPiperazineMedroxyprogesterone acetateTriamcinoloneNiacinPrednisoneEpinephrineFludrocortisoneFurosemideNorethisteroneRisperidoneHydrocortisoneEstradiolEthynodiol diacetatePrednisoloneTacrolimusSirolimusBumetanideEtacrynic acidTipranavirNorgestimateMethylprednisoloneEthinyl EstradiolAtazanavirDiazoxideArsenic trioxideQuetiapineSaquinavirDexamethasoneAripiprazoleDarunavirPaliperidoneCorticotropinFosamprenavirMestranolCortisone acetateDrospirenoneMethotrimeprazineDanazolEverolimusLopinavirPipotiazineVorinostatEstrone sulfateCyproterone acetateNilotinibIloperidoneAsenapineTemsirolimusBuserelinHistrelinHydroxyprogesterone caproateTriptorelinLurasidoneDabrafenibArticaineCeritinibDienogestBrexpiprazoleTestosteroneStanoloneFluoxymesteroneTestosterone propionateTestosterone cypionateTestosterone enanthateTestosterone undecanoateOxandroloneOxymetholoneStanozololGLPG-0492NandroloneMesteroloneMethyltestosteroneNandrolone decanoatePegvisomantInsulin PorkTroglitazoneAcarboseMetforminRosiglitazoneAcetohexamideMiglustatMiglitolPhenforminGliquidoneMitiglinideAICA ribonucleotideCastanospermineBuforminVogliboseSulodexideGlibornurideCiglitazoneAllicin2,4-thiazolidinedioneBempedoic acidGusperimusSotagliflozinBalaglitazoneDeoxyspergualinCarbutamideSalicylic acidAcetylsalicylic acidAminosalicylic AcidMesalazineDiflunisalBalsalazideOlsalazineDersalazineNitroaspirinAloxiprinGuacetisalCarbaspirin calciumHemoglobin crosfumarilMethyl salicylateTrolamine salicylateRosiglitazone Melting PointHydrophobicityIsoelectric PointMolecular WeightMolecular Formula 81 °C0.2185.395808.0C257H383N65O77S6 Khachidze, D.G. et al., J. Biol. Phys. Chem. 1:64-67 (2001) A10AC01A10AF01A10AB01A10AE01A10AD01 Insulins and analogues for injection, intermediate-actingINSULINS AND ANALOGUESDRUGS USED IN DIABETESALIMENTARY TRACT AND METABOLISMInsulins and analogues for inhalationINSULINS AND ANALOGUESDRUGS USED IN DIABETESALIMENTARY TRACT AND METABOLISMInsulins and analogues for injection, fast-actingINSULINS AND ANALOGUESDRUGS USED IN DIABETESALIMENTARY TRACT AND METABOLISMInsulins and analogues for injection, long-actingINSULINS AND ANALOGUESDRUGS USED IN DIABETESALIMENTARY TRACT AND METABOLISMInsulins and analogues for injection, intermediate- or long-acting combined with fast-actingINSULINS AND ANALOGUESDRUGS USED IN DIABETESALIMENTARY TRACT AND METABOLISM A10ACA10AA10AA10AFA10AA10AA10ABA10AA10AA10AEA10AA10AA10ADA10AA10A Alimentary Tract and MetabolismAmino Acids, Peptides, and ProteinsBlood Glucose Lowering AgentsChemical Actions and UsesCytochrome P-450 CYP1A2 InducersCytochrome P-450 Enzyme InducersDrugs Used in DiabetesHormonesHormones, Hormone Substitutes, and Hormone AntagonistsHypoglycemia-Associated AgentsHypoglycemic AgentsInsulinInsulin, Long-ActingInsulinsInsulins and AnaloguesInsulins and Analogues for Injection, Intermediate- or Long-Acting Combined With Fast-ActingPancreatic HormonesPeptide HormonesPeptidesPharmacologic ActionsPhysiological Effects of Drugs D000602D020164D065694D065693D006728D006730D007004D007328D049528D061385D010187D036361D010455D020228D045505 2012576727671593146506231C00723D03230AY137503PA164744571Q8HXV2DAP000802Insulin Drugs Product Database (DPD)Drugs Product Database (DPD)Drugs Product Database (DPD)ChEBIPubChem SubstanceKEGG CompoundKEGG DrugGenBankPharmGKBUniProtKBTherapeutic Targets DatabaseWikipedia RxListDrugs.com http://www.rxlist.com/cgi/generic3/novolog.htmhttp://www.drugs.com/pro/humulin-r.html //s3-us-west-2.amazonaws.com/drugbank/fda_labels/DB00030.pdf?1265922794 Herrmann BL, Kasser C, Keuthage W, Huptas M, Dette H, Klute A: Comparison of insulin aspart vs. regular human insulin with or without insulin detemir concerning adipozytokines and metabolic effects in patients with type 2 diabetes mellitus. Exp Clin Endocrinol Diabetes. 2013 Apr;121(4):210-3. doi: 10.1055/s-0033-1334905. Epub 2013 Mar 19.Lepore M, Pampanelli S, Fanelli C, Porcellati F, Bartocci L, Di Vincenzo A, Cordoni C, Costa E, Brunetti P, Bolli GB: Pharmacokinetics and pharmacodynamics of subcutaneous injection of long-acting human insulin analog glargine, NPH insulin, and ultralente human insulin and continuous subcutaneous infusion of insulin lispro. Diabetes. 2000 Dec;49(12):2142-8.Owens DR, Coates PA, Luzio SD, Tinbergen JP, Kurzhals R: Pharmacokinetics of 125I-labeled insulin glargine (HOE 901) in healthy men: comparison with NPH insulin and the influence of different subcutaneous injection sites. Diabetes Care. 2000 Jun;23(6):813-9.Danne T, Lupke K, Walte K, Von Schuetz W, Gall MA: Insulin detemir is characterized by a consistent pharmacokinetic profile across age-groups in children, adolescents, and adults with type 1 diabetes. Diabetes Care. 2003 Nov;26(11):3087-92.Owens DR, Bolli GB: Beyond the era of NPH insulin--long-acting insulin analogs: chemistry, comparative pharmacology, and clinical application. Diabetes Technol Ther. 2008 Oct;10(5):333-49. doi: 10.1089/dia.2008.0023. 2351241511118018108410021457824418715209 approvedinvestigational Pfizer (withdrawn)LillyLeoNovo NordiskNovo Nordisk ExuberaHumulin N PenlnsulatardNasulinNovolin N RelionNovolin NPH Organic Compounds Organic Acids Carboxylic Acids and Derivatives Amino Acids, Peptides, and Analogues Peptides RE378722183577225339372911326257233654692966859676582728891219376489606652885825809587784036444226794357281195937943178888909986238178389470919267582153008146588895039784851809283193863600184245188551528746470687290197305986849975781569368734845822740993933729339615951119895973749358352944613396624619717689 United StatesCanadaCanadaUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited StatesUnited States 1993-02-122007-10-302007-10-092004-08-091999-05-141999-05-141998-09-112000-06-242009-06-122000-06-292000-06-292009-08-112010-06-112000-06-292006-08-102009-08-112000-06-292000-06-292009-09-182000-06-292009-06-122002-11-242003-04-242001-07-202010-03-252006-09-142012-07-122011-10-172010-06-112003-03-022008-12-262003-01-162012-02-192003-01-162010-06-112011-03-082009-07-042009-10-202010-02-162011-10-082011-02-152009-06-122009-06-122006-09-14 2010-02-122015-02-072017-05-072024-08-092019-05-142019-05-142018-09-112020-06-242029-06-122020-06-292020-06-292029-08-112030-06-112020-06-292026-08-102029-08-112020-06-292020-06-292029-09-182020-06-292029-06-122022-11-242023-04-242021-07-202030-03-252026-09-142032-07-122031-10-172030-06-112023-03-022028-12-262023-01-162032-02-192023-01-162030-06-112031-03-082029-07-042029-10-202030-02-162031-10-082031-02-152029-06-122029-06-122026-09-14 falsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalsefalse Novo nordisk inc false Insulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin 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HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin HumanInsulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin HumanInsulin Human + Insulin HumanInsulin Human + Insulin HumanInsulin Human Humulin RHumulin RNovolin RNovolin NHumulin NNovolin RNovolin NHumulin NNovolin 70/30Novolin Ge TorontoNovolin Ge Toronto PenfillNovolinset Ge Toronto Inj Liq 100u/mlNovolinN NHumulin R CartridgeInsulin Human Winthrop RapidInsulin Human Winthrop 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CartridgeHumulin 40/60 InjHumulin 40/60 InjHumulin 40/60 CartridgeHumulin 40/60 CartridgeHumulin 50/50 InjHumulin 50/50 InjHumulin 50/50 CartridgeHumulin 50/50 CartridgeHumulin 30/70 CartridgeHumulin 30/70 CartridgeAfrezzaAfrezzaAfrezzaAfrezzaAfrezzaAfrezzaAfrezzaAfrezzaHumulin NHumulin R U-500Humulin 70/30Humulin NAfrezzaAfrezzaAfrezzaAfrezzaHumulin R U-500 KwikPenHumulin NHumulin RNovolin70/30 70/30Humulin 70/30 70/30Novolin 70/30Novolin 70/30Novolin 70/30Entuzity KwikpenHumulin 70/30Novolin 70/30Humalog 70/30Novolin 70/30Humulin RHumulin R (kwikpen)Humulin 30/70 (insulin Human Biosynth Inj)Humulin 30/70 (insulin Human Biosynth Inj)Humulin N A-S Medication Solutions LLCDispenseXpress Inc.Eli Lilly & Co.Hospira Inc.Intervet InternationalNovo Nordisk Inc.Pfizer Inc.Physicians Total Care Inc. http://orders.a-smeds.comhttp://www.lilly.comhttp://www.hospira.comhttp://www.intervet.cahttp://www.novonordisk.comhttp://www.pfizer.comhttp://www.physicianstotalcare.com Actraphane 30Actraphane 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Winthrop Comb 25Insulin Human Winthrop Comb 25Insulin Human Winthrop Comb 25Insulin Human Winthrop Comb 25Insulin Human Winthrop Comb 30Insulin Human Winthrop Comb 30Insulin Human Winthrop Comb 30Insulin Human Winthrop Comb 30Insulin Human Winthrop Comb 30Insulin Human Winthrop Comb 30Insulin Human Winthrop Comb 30Insulin Human Winthrop Comb 30Insulin Human Winthrop Comb 30Insulin Human Winthrop Comb 30Insulin Human Winthrop Comb 30Insulin Human Winthrop Comb 30Insulin Human Winthrop Comb 30Insulin Human Winthrop Comb 30Insulin Human Winthrop Comb 30Insulin Human Winthrop Comb 30Insulin Human Winthrop Comb 50Insulin Human Winthrop Comb 50Insulin Human Winthrop Comb 50Insulin Human Winthrop Comb 50Insulin Human Winthrop Comb 50Insulin Human Winthrop Comb 50Insulin Human Winthrop Comb 50Insulin Human Winthrop Comb 50Insulin Human Winthrop Comb 50Insulin Human Winthrop Comb 50Insulin Human Winthrop Comb 50Insulin Human Winthrop Comb 50Insulin Human Winthrop Comb 50Insulin Human Winthrop Comb 50Insulin Human Winthrop Comb 50Insulin Human Winthrop Comb 50Insulin Human Winthrop InfusatInsulin Human Winthrop InfusatInsulin Human Winthrop RapidInsulin Human Winthrop RapidInsulin Human Winthrop RapidInsulin Human Winthrop RapidInsulin Human Winthrop RapidInsulin Human Winthrop RapidInsulin Human Winthrop RapidInsulin Human Winthrop RapidInsulin Human Winthrop RapidInsulin Human Winthrop RapidInsulin Human Winthrop RapidInsulin Human Winthrop RapidInsulin Human Winthrop RapidInsulin Human Winthrop RapidInsulin Human Winthrop RapidInsulin Human Winthrop RapidInsulin Human Winthrop RapidInsulin Human Winthrop RapidInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman BasalInsuman 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RapidInsuman RapidInsuman RapidInsuman RapidInsuman RapidInsuman RapidInsuman RapidInsuman RapidInsuman RapidInsuman RapidInsuman RapidInsuman RapidInsuman RapidInsuman RapidNovolin 70/30Novolin 70/30Novolin 70/30Novolin 70/30Novolin 70/30Novolin 70/30Novolin Ge 10/90 Penfill Inj SusNovolin Ge 10/90 Penfill Inj SusNovolin Ge 20/80 Penfill Inj SusNovolin Ge 20/80 Penfill Inj SusNovolin Ge 30/70Novolin Ge 30/70Novolin Ge 30/70 PenfillNovolin Ge 30/70 PenfillNovolin Ge 40/60 PenfillNovolin Ge 40/60 PenfillNovolin Ge 50/50 PenfillNovolin Ge 50/50 PenfillNovolin Ge NphNovolin Ge Nph PenfillNovolin Ge TorontoNovolin Ge Toronto PenfillNovolin NNovolin NNovolin NNovolin RNovolin RNovolin RNovolin70/30 70/30NovolinN NNovolinset Ge 30/70 Inj SusNovolinset Ge 30/70 Inj SusNovolinset Ge Nph Inj Sus 100u/mlNovolinset Ge Toronto Inj Liq 100u/mlVelosulinVelosulinVelosulin 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Novo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskSanofi AventisSanofi AventisSanofi AventisSanofi AventisMannkind CorporationMannkind CorporationMannkind CorporationMannkind CorporationMannkind CorporationMannkind CorporationMannkind CorporationMannkind CorporationEli Lilly & Co. Ltd.Physicians Total Care, Inc.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.A S Medication SolutionsEli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Remedy RepackEli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Physicians Total Care, Inc.A S Medication SolutionsEli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Physicians Total Care, Inc.Eli Lilly & Co. Ltd.A S Medication SolutionsEli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Eli Lilly & Co. Ltd.Novo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HSanofi Aventis Deutschland Gmb HRemedy RepackNovo NordiskA S Medication SolutionsTYA PharmaceuticalsPhysicians Total Care, Inc.A S Medication SolutionsNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskTYA PharmaceuticalsNovo NordiskA S Medication SolutionsTYA PharmaceuticalsNovo NordiskA S Medication SolutionsRemedy RepackRemedy RepackNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo NordiskNovo Nordisk 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SubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousIntravenous; SubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousRespiratory (inhalation)Respiratory (inhalation)Respiratory (inhalation)Respiratory (inhalation)SubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousSubcutaneousParenteralSubcutaneousIntramuscular; Intravenous; SubcutaneousParenteralIntramuscular; SubcutaneousIntramuscular; Intravenous; Subcutane