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Identification
NameEptifibatide
Accession NumberDB00063  (BTD00063, BIOD00063)
TypeBiotech
GroupsApproved, Investigational
Description

Synthetic cyclic hexapeptide that binds to platelet receptor glycoprotein and inhibits platelet aggregation.

Protein structureNo structure small
Related Articles
Protein chemical formulaC35H49N11O9S2
Protein average weight831.962 Da
SequencesNot Available
Synonyms
Integrelin
Intrifiban
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Eptifibatide Injectionsolution0.75 mgintravenousMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Eptifibatide Injectionsolution2 mgintravenousOmega Laboratories LtdNot applicableNot applicableCanada
Eptifibatide Injectionsolution0.75 mgintravenousOmega Laboratories LtdNot applicableNot applicableCanada
Eptifibatide Injectionsolution0.75 mgintravenousTeva Canada Limited2013-04-29Not applicableCanada
Eptifibatide Injectionsolution2 mgintravenousTeva Canada Limited2013-04-29Not applicableCanada
Eptifibatide Injectionsolution2 mgintravenousMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Integrilininjection, solution.75 mg/mLintravenousMerck Sharp & Dohme Corp.1998-05-18Not applicableUs
Integrilinsolution2 mgintravenousMerck Canada Inc1999-06-23Not applicableCanada
Integrilinsolution0.75 mgintravenousMerck Canada Inc1999-06-23Not applicableCanada
Integrilininjection, solution2 mg/mLintravenousMerck Sharp & Dohme Corp.1998-05-18Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Eptifibatideinjection, solution.75 mg/mLintravenousTeva Parenteral Medicines, Inc.2015-12-14Not applicableUs
Eptifibatideinjection200 mg/100mLintravenousAurobindo Pharma Limited2015-12-08Not applicableUs
Eptifibatideinjection20 mg/10mLintravenousAurobindo Pharma Limited2015-12-08Not applicableUs
Eptifibatideinjection75 mg/100mLintravenousAurobindo Pharma Limited2015-12-08Not applicableUs
Eptifibatideinjection200 mg/100mLintravenousAuro Medics Pharma Llc2015-12-08Not applicableUs
Eptifibatideinjection20 mg/10mLintravenousAuro Medics Pharma Llc2015-12-08Not applicableUs
Eptifibatideinjection75 mg/100mLintravenousAuro Medics Pharma Llc2015-12-08Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIINA8320J834
CAS number188627-80-7
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationFor treatment of myocardial infarction and acute coronary syndrome.
PharmacodynamicsEptifibatide is an anti-coagulant that selectively blocks the platelet glycoprotein IIb/IIIa receptor. Eptifibatide is a cyclic heptapeptide derived from a protein found in the venom of the southeastern pygmy rattlesnake (Sistrurus miliarus barbouri). It belongs to the class of the so called arginin-glycin-aspartat-mimetics and reversibly binds to platelets.
Mechanism of actionEptifibatide inhibits platelet aggregation by reversibly binding to the platelet receptor glycoprotein (GP) IIb/IIIa of human platelets, thus preventing the binding of fibrinogen, von Willebrand factor, and other adhesive ligands. Inhibition of platelet aggregation occurs in a dose- and concentration-dependent manner.
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AbsorptionNot Available
Volume of distributionNot Available
Protein bindingApproximately 25%
Metabolism

No major metabolites have been detected in human plasma. Deamidated eptifibatide and other, more polar metabolites have been detected in urine.

Route of eliminationNot Available
Half lifeApproximately 2.5 hours
Clearance
  • 55 mL/kg/h [patients with coronary artery disease]
ToxicityEptifibatide was not lethal to rats, rabbits, or monkeys when administered by continuous intravenous infusion for 90 minutes at a total dose of 45 mg/kg (about 2 to 5 times the recommended maximum daily human dose on a body surface area basis)
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Eptifibatide Action PathwayDrug actionSMP00266
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
Manufacturers
  • Schering corp
Packagers
Dosage forms
FormRouteStrength
Injectionintravenous20 mg/10mL
Injectionintravenous200 mg/100mL
Injectionintravenous75 mg/100mL
Injection, solutionintravenous.75 mg/mL
Injection, solutionintravenous2 mg/mL
Solutionintravenous0.75 mg
Solutionintravenous2 mg
Prices
Unit descriptionCostUnit
Integrilin 20 mg/10 ml vial12.41USD ml
Integrilin 200 mg/100 ml vial10.74USD ml
Integrilin 75 mg/100 ml vial3.88USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2133205 No2007-04-172013-04-27Canada
US5686570 No1994-11-112014-11-11Us
US5807825 No1995-09-152015-09-15Us
Properties
StateLiquid
Experimental Properties
PropertyValueSource
hydrophobicity-2.3Not Available
References
Synthesis Reference

Guojie Ho, Antoinette Paone, Luciano Forni, Catherine De Tollenaere, Brice Bonnet, Christine Devijver, “Processes for preparing eptifibatide.” U.S. Patent US20060036071, issued February 16, 2006.

US20060036071
General References
  1. Nguyen CM, Harrington RA: Glycoprotein IIb/IIIa receptor antagonists: a comparative review of their use in percutaneous coronary intervention. Am J Cardiovasc Drugs. 2003;3(6):423-36. [PubMed:14728062 ]
External Links
ATC CodesB01AC16
AHFS Codes
  • 20:12.18
PDB EntriesNot Available
FDA labelDownload (87.5 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AbciximabEptifibatide may increase the anticoagulant activities of Abciximab.
AcenocoumarolEptifibatide may increase the anticoagulant activities of Acenocoumarol.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Acetylsalicylic acid.
AlteplaseEptifibatide may increase the anticoagulant activities of Alteplase.
AnistreplaseEptifibatide may increase the anticoagulant activities of Anistreplase.
ApixabanThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Apixaban.
Citric AcidEptifibatide may increase the anticoagulant activities of Citric Acid.
CollagenaseThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Collagenase.
Dabigatran etexilateEptifibatide may increase the anticoagulant activities of Dabigatran etexilate.
DalteparinEptifibatide may increase the anticoagulant activities of Dalteparin.
DasatinibDasatinib may increase the anticoagulant activities of Eptifibatide.
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Deoxycholic Acid.
DicoumarolEptifibatide may increase the anticoagulant activities of Dicoumarol.
Edetic AcidEptifibatide may increase the anticoagulant activities of Edetic Acid.
EnoxaparinEptifibatide may increase the anticoagulant activities of Enoxaparin.
Ethyl biscoumacetateEptifibatide may increase the anticoagulant activities of Ethyl biscoumacetate.
Fondaparinux sodiumEptifibatide may increase the anticoagulant activities of Fondaparinux sodium.
GlucosamineGlucosamine may increase the antiplatelet activities of Eptifibatide.
HeparinEptifibatide may increase the anticoagulant activities of Heparin.
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Ibritumomab.
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Eptifibatide.
LimaprostLimaprost may increase the antiplatelet activities of Eptifibatide.
ObinutuzumabThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Obinutuzumab.
Omega-3 fatty acidsOmega-3 fatty acids may increase the antiplatelet activities of Eptifibatide.
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Eptifibatide.
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Eptifibatide.
PhenindioneEptifibatide may increase the anticoagulant activities of Phenindione.
PhenprocoumonEptifibatide may increase the anticoagulant activities of Phenprocoumon.
ReteplaseEptifibatide may increase the anticoagulant activities of Reteplase.
RidogrelEptifibatide may increase the anticoagulant activities of Ridogrel.
RivaroxabanEptifibatide may increase the anticoagulant activities of Rivaroxaban.
StreptokinaseEptifibatide may increase the anticoagulant activities of Streptokinase.
SulodexideEptifibatide may increase the anticoagulant activities of Sulodexide.
TenecteplaseEptifibatide may increase the anticoagulant activities of Tenecteplase.
TipranavirTipranavir may increase the antiplatelet activities of Eptifibatide.
TositumomabThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Tositumomab.
TreprostinilEptifibatide may increase the anticoagulant activities of Treprostinil.
UrokinaseEptifibatide may increase the anticoagulant activities of Urokinase.
Vitamin EVitamin E may increase the antiplatelet activities of Eptifibatide.
WarfarinEptifibatide may increase the anticoagulant activities of Warfarin.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
General Function:
Virus receptor activity
Specific Function:
Integrin alpha-V/beta-3 (ITGAV:ITGB3) is a receptor for cytotactin, fibronectin, laminin, matrix metalloproteinase-2, osteopontin, osteomodulin, prothrombin, thrombospondin, vitronectin and von Willebrand factor. Integrin alpha-IIb/beta-3 (ITGA2B:ITGB3) is a receptor for fibronectin, fibrinogen, plasminogen, prothrombin, thrombospondin and vitronectin. Integrins alpha-IIb/beta-3 and alpha-V/bet...
Gene Name:
ITGB3
Uniprot ID:
P05106
Molecular Weight:
87056.975 Da
References
  1. Amoroso G, van Boven AJ, van Veldhuisen DJ, Tio RA, Balje-Volkers CP, Petronio AS, van Oeveren W: Eptifibatide and abciximab exhibit equivalent antiplatelet efficacy in an experimental model of stenting in both healthy volunteers and patients with coronary artery disease. J Cardiovasc Pharmacol. 2001 Oct;38(4):633-41. [PubMed:11588534 ]
  2. Schror K, Weber AA: Comparative pharmacology of GP IIb/IIIa antagonists. J Thromb Thrombolysis. 2003 Apr;15(2):71-80. [PubMed:14618072 ]
  3. Fischer TH, Thatte HS, Nichols TC, Bender-Neal DE, Bellinger AD, Vournakis JN: Synergistic platelet integrin signaling and factor XII activation in poly-N-acetyl glucosamine fiber-mediated hemostasis. Biomaterials. 2005 Sep;26(27):5433-43. [PubMed:15860200 ]
  4. Weber AA, Jacobs C, Meila D, Weber S, Zotz RB, Scharf RE, Kelm M, Strauer BE, Schror K: No evidence for an influence of the human platelet antigen-1 polymorphism on the antiplatelet effects of glycoprotein IIb/IIIa inhibitors. Pharmacogenetics. 2002 Oct;12(7):581-3. [PubMed:12360110 ]
  5. Schwarz M, Katagiri Y, Kotani M, Bassler N, Loeffler C, Bode C, Peter K: Reversibility versus persistence of GPIIb/IIIa blocker-induced conformational change of GPIIb/IIIa (alphaIIbbeta3, CD41/CD61). J Pharmacol Exp Ther. 2004 Mar;308(3):1002-11. Epub 2003 Nov 14. [PubMed:14617694 ]
  6. Auer J, Berent R, Lassnig E, Weber T, Maurer E, Eber B: [Platelet glycoprotein IIb/IIIa inhibitors in coronary artery disease]. Herz. 2003 Aug;28(5):393-403. [PubMed:12928738 ]
  7. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
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Drug created on June 13, 2005 07:24 / Updated on May 24, 2016 02:06