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Identification
NameEptifibatide
Accession NumberDB00063  (BTD00063, BIOD00063)
TypeBiotech
GroupsApproved, Investigational
DescriptionSynthetic 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 Injectionsolution2 mgintravenousOmega Laboratories LtdNot applicableNot applicableCanada
Eptifibatide Injectionsolution2 mgintravenousAccord Healthcare IncNot applicableNot applicableCanada
Eptifibatide Injectionsolution2 mgintravenousTeva Canada Limited2013-04-29Not applicableCanada
Eptifibatide Injectionsolution0.75 mgintravenousMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Eptifibatide Injectionsolution0.75 mgintravenousTeva Canada Limited2013-04-29Not applicableCanada
Eptifibatide Injectionsolution2 mgintravenousMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Eptifibatide Injectionsolution0.75 mgintravenousOmega Laboratories LtdNot applicableNot applicableCanada
Eptifibatide Injectionsolution0.75 mgintravenousAccord Healthcare IncNot applicableNot applicableCanada
Integrilininjection, solution.75 mg/mLintravenousMerck Sharp & Dohme Corp.1998-05-18Not applicableUs
Integrilininjection, solution2 mg/mLintravenousMerck Sharp & Dohme Corp.1998-05-18Not applicableUs
Integrilinsolution0.75 mgintravenousMerck Canada Inc1999-06-23Not applicableCanada
Integrilinsolution2 mgintravenousMerck Canada Inc1999-06-23Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Eptifibatideinjection, solution.75 mg/mLintravenousTeva Parenteral Medicines, Inc.2015-12-14Not applicableUs
Eptifibatideinjection75 mg/100mLintravenousAurobindo Pharma Limited2015-12-08Not applicableUs
Eptifibatideinjection75 mg/100mLintravenousAuro Medics Pharma Llc2015-12-08Not applicableUs
Eptifibatideinjection20 mg/10mLintravenousAurobindo Pharma Limited2015-12-08Not applicableUs
Eptifibatideinjection20 mg/10mLintravenousAuro Medics Pharma Llc2015-12-08Not applicableUs
Eptifibatideinjection200 mg/100mLintravenousAurobindo Pharma Limited2015-12-08Not applicableUs
Eptifibatideinjection200 mg/100mLintravenousAuro Medics Pharma Llc2015-12-08Not applicableUs
Eptifibatide AccordSolution for infusion0.75 mg/mlIntravenous useAccord Healthcare Limited2016-01-11Not applicableEu
Eptifibatide AccordSolution for injection2 mg/mlIntravenous useAccord Healthcare Limited2016-01-11Not applicableEu
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.
Related Articles
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
Solution for infusionIntravenous use0.75 mg/ml
Solution for injectionIntravenous use2 mg/ml
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 Acetylsalicylic acid is combined with Eptifibatide.
AlprostadilAlprostadil may increase the anticoagulant activities of Eptifibatide.
AlprostadilEptifibatide may increase the antiplatelet activities of Alprostadil.
AlteplaseEptifibatide may increase the anticoagulant activities of Alteplase.
ALX-0081Eptifibatide may increase the anticoagulant activities of ALX-0081.
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Eptifibatide.
AnagrelideEptifibatide may increase the anticoagulant activities of Anagrelide.
AncrodEptifibatide may increase the anticoagulant activities of Ancrod.
AnistreplaseEptifibatide may increase the anticoagulant activities of Anistreplase.
Antithrombin III humanEptifibatide may increase the anticoagulant activities of Antithrombin III human.
ApixabanEptifibatide may increase the anticoagulant activities of Apixaban.
AprotininThe therapeutic efficacy of Eptifibatide can be decreased when used in combination with Aprotinin.
ArdeparinEptifibatide may increase the anticoagulant activities of Ardeparin.
ArgatrobanEptifibatide may increase the anticoagulant activities of Argatroban.
AstaxanthinEptifibatide may increase the anticoagulant activities of Astaxanthin.
AzelastineAzelastine may increase the anticoagulant activities of Eptifibatide.
AzelastineEptifibatide may increase the antiplatelet activities of Azelastine.
BatroxobinEptifibatide may increase the anticoagulant activities of Batroxobin.
BecaplerminEptifibatide may increase the anticoagulant activities of Becaplermin.
BemiparinEptifibatide may increase the anticoagulant activities of Bemiparin.
BeraprostEptifibatide may increase the anticoagulant activities of Beraprost.
BivalirudinEptifibatide may increase the anticoagulant activities of Bivalirudin.
CangrelorEptifibatide may increase the anticoagulant activities of Cangrelor.
CertoparinEptifibatide may increase the anticoagulant activities of Certoparin.
CilostazolEptifibatide may increase the anticoagulant activities of Cilostazol.
Citric AcidEptifibatide may increase the anticoagulant activities of Citric Acid.
ClopidogrelEptifibatide may increase the anticoagulant activities of Clopidogrel.
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.
DanaparoidEptifibatide may increase the anticoagulant activities of Danaparoid.
DasatinibDasatinib may increase the anticoagulant activities of Eptifibatide.
DefibrotideEptifibatide may increase the anticoagulant activities of Defibrotide.
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Deoxycholic Acid.
DesirudinEptifibatide may increase the anticoagulant activities of Desirudin.
DesmoteplaseEptifibatide may increase the anticoagulant activities of Desmoteplase.
DextranEptifibatide may increase the anticoagulant activities of Dextran.
Dextran 40Eptifibatide may increase the anticoagulant activities of Dextran 40.
Dextran 70Eptifibatide may increase the anticoagulant activities of Dextran 70.
Dextran 75Eptifibatide may increase the anticoagulant activities of Dextran 75.
DicoumarolEptifibatide may increase the anticoagulant activities of Dicoumarol.
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Eptifibatide.
DipyridamoleEptifibatide may increase the anticoagulant activities of Dipyridamole.
DitazoleEptifibatide may increase the anticoagulant activities of Ditazole.
Drotrecogin alfaEptifibatide may increase the anticoagulant activities of Drotrecogin alfa.
Edetic AcidEptifibatide may increase the anticoagulant activities of Edetic Acid.
EdoxabanEptifibatide may increase the anticoagulant activities of Edoxaban.
EnoxaparinEptifibatide may increase the anticoagulant activities of Enoxaparin.
EpinastineEpinastine may increase the anticoagulant activities of Eptifibatide.
EpinastineEptifibatide may increase the antiplatelet activities of Epinastine.
EpoprostenolEptifibatide may increase the anticoagulant activities of Epoprostenol.
Ethyl biscoumacetateEptifibatide may increase the anticoagulant activities of Ethyl biscoumacetate.
FibrinolysinEptifibatide may increase the anticoagulant activities of Fibrinolysin.
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.
HirulogEptifibatide may increase the anticoagulant activities of Hirulog.
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Ibritumomab tiuxetan.
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Eptifibatide.
IbudilastIbudilast may increase the anticoagulant activities of Eptifibatide.
IbudilastEptifibatide may increase the antiplatelet activities of Ibudilast.
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Eptifibatide.
Icosapent ethylEptifibatide may increase the antiplatelet activities of Icosapent ethyl.
IfenprodilIfenprodil may increase the anticoagulant activities of Eptifibatide.
IfenprodilEptifibatide may increase the antiplatelet activities of Ifenprodil.
IloprostEptifibatide may increase the anticoagulant activities of Iloprost.
LepirudinEptifibatide may increase the anticoagulant activities of Lepirudin.
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Eptifibatide.
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Eptifibatide.
MilrinoneMilrinone may increase the anticoagulant activities of Eptifibatide.
MilrinoneEptifibatide may increase the antiplatelet activities of Milrinone.
NadroparinEptifibatide may increase the anticoagulant activities of Nadroparin.
NCX 4016Eptifibatide may increase the anticoagulant activities of NCX 4016.
NimesulideNimesulide may increase the anticoagulant activities of Eptifibatide.
NimesulideEptifibatide may increase the antiplatelet activities of Nimesulide.
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.
OtamixabanEptifibatide may increase the anticoagulant activities of Otamixaban.
ParnaparinEptifibatide may increase the anticoagulant activities of Parnaparin.
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Eptifibatide.
Pentosan PolysulfateEptifibatide may increase the anticoagulant activities of Pentosan Polysulfate.
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Eptifibatide.
PhenindioneEptifibatide may increase the anticoagulant activities of Phenindione.
PhenprocoumonEptifibatide may increase the anticoagulant activities of Phenprocoumon.
PlasminEptifibatide may increase the anticoagulant activities of Plasmin.
PrasugrelEptifibatide may increase the anticoagulant activities of Prasugrel.
Protein CEptifibatide may increase the anticoagulant activities of Protein C.
ProtocatechualdehydeEptifibatide may increase the anticoagulant activities of Protocatechualdehyde.
ResveratrolResveratrol may increase the anticoagulant activities of Eptifibatide.
ResveratrolEptifibatide may increase the antiplatelet activities of Resveratrol.
ReteplaseEptifibatide may increase the anticoagulant activities of Reteplase.
ReviparinEptifibatide may increase the anticoagulant activities of Reviparin.
RidogrelRidogrel may increase the anticoagulant activities of Eptifibatide.
RidogrelEptifibatide may increase the antiplatelet activities of Ridogrel.
RivaroxabanEptifibatide may increase the anticoagulant activities of Rivaroxaban.
RosiglitazoneEptifibatide may increase the anticoagulant activities of Rosiglitazone.
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Eptifibatide.
SCH-530348SCH-530348 may increase the anticoagulant activities of Eptifibatide.
SCH-530348Eptifibatide may increase the antiplatelet activities of SCH-530348.
SelexipagEptifibatide may increase the anticoagulant activities of Selexipag.
SevofluraneSevoflurane may increase the anticoagulant activities of Eptifibatide.
SevofluraneEptifibatide may increase the antiplatelet activities of Sevoflurane.
SRT501SRT501 may increase the anticoagulant activities of Eptifibatide.
SRT501Eptifibatide may increase the antiplatelet activities of SRT501.
StreptokinaseEptifibatide may increase the anticoagulant activities of Streptokinase.
SulodexideEptifibatide may increase the anticoagulant activities of Sulodexide.
TenecteplaseEptifibatide may increase the anticoagulant activities of Tenecteplase.
TesmilifeneTesmilifene may increase the anticoagulant activities of Eptifibatide.
TesmilifeneEptifibatide may increase the antiplatelet activities of Tesmilifene.
TicagrelorEptifibatide may increase the anticoagulant activities of Ticagrelor.
TiclopidineEptifibatide may increase the anticoagulant activities of Ticlopidine.
TinzaparinEptifibatide may increase the anticoagulant activities of Tinzaparin.
TipranavirTipranavir may increase the antiplatelet activities of Eptifibatide.
TirofibanEptifibatide may increase the anticoagulant activities of Tirofiban.
TositumomabThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Tositumomab.
TranilastTranilast may increase the anticoagulant activities of Eptifibatide.
TranilastEptifibatide may increase the antiplatelet activities of Tranilast.
TrapidilTrapidil may increase the anticoagulant activities of Eptifibatide.
TrapidilEptifibatide may increase the antiplatelet activities of Trapidil.
TreprostinilEptifibatide may increase the anticoagulant activities of Treprostinil.
TreprostinilTreprostinil may increase the antiplatelet activities of Eptifibatide.
TriflusalEptifibatide may increase the anticoagulant activities of Triflusal.
UrokinaseEptifibatide may increase the anticoagulant activities of Urokinase.
Vitamin EVitamin E may increase the antiplatelet activities of Eptifibatide.
VorapaxarEptifibatide may increase the anticoagulant activities of Vorapaxar.
WarfarinEptifibatide may increase the anticoagulant activities of Warfarin.
XimelagatranEptifibatide may increase the anticoagulant activities of Ximelagatran.
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 September 26, 2016 02:12