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 IDs Not Available
Product Ingredients Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Eptifibatide InjectionSolution0.75 mgIntravenousMylan PharmaceuticalsNot applicableNot applicableCanada
Eptifibatide InjectionSolution0.75 mgIntravenousAccord Healthcare LimitedNot applicableNot applicableCanada
Eptifibatide InjectionSolution2 mgIntravenousFresenius KabiNot applicableNot applicableCanada
Eptifibatide InjectionSolution0.75 mgIntravenousOmega Laboratories LtdNot applicableNot applicableCanada
Eptifibatide InjectionSolution2 mgIntravenousAccord Healthcare LimitedNot applicableNot applicableCanada
Eptifibatide InjectionSolution2 mgIntravenousMylan PharmaceuticalsNot applicableNot applicableCanada
Eptifibatide InjectionSolution2 mgIntravenousTeva2013-04-29Not applicableCanada
Eptifibatide InjectionSolution2 mgIntravenousOmega Laboratories LtdNot applicableNot applicableCanada
Eptifibatide InjectionSolution0.75 mgIntravenousFresenius KabiNot applicableNot applicableCanada
Eptifibatide InjectionSolution0.75 mgIntravenousTeva2013-04-29Not applicableCanada
IntegrilinInjection, solution.75 mg/mLIntravenousMerck Sharp & Dohme Limited1998-05-18Not applicableUs
IntegrilinSolution2 mgIntravenousMerck Ltd.1999-06-23Not applicableCanada
IntegrilinInjection, solution2 mg/mLIntravenousMerck Sharp & Dohme Limited1998-05-18Not applicableUs
IntegrilinSolution0.75 mgIntravenousMerck Ltd.1999-06-23Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
EptifibatideInjection, solution.75 mg/mLIntravenousTeva Parenteral Medicines, Inc.2015-12-14Not applicableUs
EptifibatideInjection.75 mg/mLIntravenousAmneal Biosciences2016-12-08Not applicableUs
EptifibatideInjection20 mg/10mLIntravenousAuro Medics Pharma Llc2015-12-08Not applicableUs
EptifibatideInjection75 mg/100mLIntravenousAuro Medics Pharma Llc2015-12-08Not applicableUs
EptifibatideInjection200 mg/100mLIntravenousAurobindo Pharma2015-12-08Not applicableUs
EptifibatideInjection, solution2 mg/mLIntravenousTeva Parenteral Medicines, Inc.2016-07-06Not applicableUs
EptifibatideInjection200 mg/100mLIntravenousAuro Medics Pharma Llc2015-12-08Not applicableUs
EptifibatideInjection75 mg/100mLIntravenousAurobindo Pharma2015-12-08Not applicableUs
EptifibatideInjection, solution2 mg/mLIntravenousAkorn2017-04-18Not applicableUs
EptifibatideInjection2 mg/mLIntravenousAmneal Biosciences2016-12-08Not applicableUs
EptifibatideInjection, solution.75 mg/mLIntravenousAkorn2017-04-18Not applicableUs
EptifibatideInjection20 mg/10mLIntravenousAurobindo Pharma2015-12-08Not applicableUs
Eptifibatide AccordInjection, solution0.75 mg/mlIntravenousAccord Healthcare Limited2016-01-11Not applicableEu
Eptifibatide AccordInjection, solution2 mg/mlIntravenousAccord Healthcare Limited2016-01-11Not applicableEu
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Categories
UNIINA8320J834
CAS number188627-80-7
Pharmacology
Indication

For treatment of myocardial infarction and acute coronary syndrome.

Structured Indications
Pharmacodynamics

Eptifibatide 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 action

Eptifibatide 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.

TargetKindPharmacological actionActionsOrganismUniProt ID
Integrin beta-3ProteinyesNot AvailableHumanP05106 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein binding

Approximately 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 life

Approximately 2.5 hours

Clearance
  • 55 mL/kg/h [patients with coronary artery disease]
Toxicity

Eptifibatide 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
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
AbciximabEptifibatide may increase the anticoagulant activities of Abciximab.Approved
AcenocoumarolEptifibatide may increase the anticoagulant activities of Acenocoumarol.Approved
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Acetylsalicylic acid.Approved, Vet Approved
AlprostadilAlprostadil may increase the anticoagulant activities of Eptifibatide.Approved, Investigational
AlteplaseEptifibatide may increase the anticoagulant activities of Alteplase.Approved
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Aminosalicylic Acid.Approved
AnagrelideEptifibatide may increase the anticoagulant activities of Anagrelide.Approved
AncrodEptifibatide may increase the anticoagulant activities of Ancrod.Investigational
AnistreplaseEptifibatide may increase the anticoagulant activities of Anistreplase.Approved
Antithrombin III humanEptifibatide may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Apixaban.Approved
AprotininThe therapeutic efficacy of Eptifibatide can be decreased when used in combination with Aprotinin.Approved, Withdrawn
ArdeparinEptifibatide may increase the anticoagulant activities of Ardeparin.Approved, Withdrawn
ArgatrobanEptifibatide may increase the anticoagulant activities of Argatroban.Approved, Investigational
AzelastineAzelastine may increase the anticoagulant activities of Eptifibatide.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Balsalazide.Approved, Investigational
BecaplerminEptifibatide may increase the anticoagulant activities of Becaplermin.Approved, Investigational
BemiparinEptifibatide may increase the anticoagulant activities of Bemiparin.Approved
BeraprostEptifibatide may increase the anticoagulant activities of Beraprost.Investigational
BivalirudinEptifibatide may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
CangrelorEptifibatide may increase the anticoagulant activities of Cangrelor.Approved
CertoparinEptifibatide may increase the anticoagulant activities of Certoparin.Approved
CilostazolEptifibatide may increase the anticoagulant activities of Cilostazol.Approved
Citric AcidEptifibatide may increase the anticoagulant activities of Citric Acid.Nutraceutical, Vet Approved
ClopidogrelEptifibatide may increase the anticoagulant activities of Clopidogrel.Approved, Nutraceutical
Dabigatran etexilateEptifibatide may increase the anticoagulant activities of Dabigatran etexilate.Approved
DalteparinEptifibatide may increase the anticoagulant activities of Dalteparin.Approved
DasatinibDasatinib may increase the anticoagulant activities of Eptifibatide.Approved, Investigational
DefibrotideEptifibatide may increase the anticoagulant activities of Defibrotide.Approved, Investigational
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Deoxycholic Acid.Approved
DesirudinEptifibatide may increase the anticoagulant activities of Desirudin.Approved
DesmoteplaseEptifibatide may increase the anticoagulant activities of Desmoteplase.Investigational
DextranEptifibatide may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Eptifibatide may increase the anticoagulant activities of Dextran 40.Approved
DicoumarolEptifibatide may increase the anticoagulant activities of Dicoumarol.Approved
DiflunisalThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Diflunisal.Approved
DipyridamoleEptifibatide may increase the anticoagulant activities of Dipyridamole.Approved
DitazoleEptifibatide may increase the anticoagulant activities of Ditazole.Approved, Withdrawn
Drotrecogin alfaEptifibatide may increase the anticoagulant activities of Drotrecogin alfa.Approved, Investigational, Withdrawn
Edetic AcidEptifibatide may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanEptifibatide may increase the anticoagulant activities of Edoxaban.Approved
EnoxaparinEptifibatide may increase the anticoagulant activities of Enoxaparin.Approved
EpinastineEpinastine may increase the anticoagulant activities of Eptifibatide.Approved, Investigational
EpoprostenolEpoprostenol may increase the antiplatelet activities of Eptifibatide.Approved
Ethyl biscoumacetateEptifibatide may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
FibrinolysinEptifibatide may increase the anticoagulant activities of Plasmin.Investigational
Fondaparinux sodiumEptifibatide may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
GabexateEptifibatide may increase the anticoagulant activities of Gabexate.Investigational
GlucosamineGlucosamine may increase the antiplatelet activities of Eptifibatide.Approved
HeparinEptifibatide may increase the anticoagulant activities of Heparin.Approved, Investigational
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Ibritumomab tiuxetan.Approved
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Eptifibatide.Approved
IbudilastIbudilast may increase the anticoagulant activities of Eptifibatide.Approved, Investigational
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Eptifibatide.Approved, Nutraceutical
IfenprodilIfenprodil may increase the anticoagulant activities of Eptifibatide.Approved, Withdrawn
IloprostIloprost may increase the antiplatelet activities of Eptifibatide.Approved, Investigational
LepirudinEptifibatide may increase the anticoagulant activities of Lepirudin.Approved
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Eptifibatide.Approved
MesalazineThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Mesalazine.Approved
MilrinoneMilrinone may increase the anticoagulant activities of Eptifibatide.Approved
NadroparinEptifibatide may increase the anticoagulant activities of Nadroparin.Approved
NafamostatEptifibatide may increase the anticoagulant activities of Nafamostat.Approved, Investigational
NCX 4016The risk or severity of adverse effects can be increased when Eptifibatide is combined with NCX 4016.Investigational
NimesulideNimesulide may increase the anticoagulant activities of Eptifibatide.Approved, Withdrawn
ObinutuzumabThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Obinutuzumab.Approved
OlsalazineThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Olsalazine.Approved
Omega-3 fatty acidsOmega-3 fatty acids may increase the antiplatelet activities of Eptifibatide.Approved, Nutraceutical
ParnaparinEptifibatide may increase the anticoagulant activities of Parnaparin.Approved
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Eptifibatide.Approved
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Eptifibatide.Approved, Investigational
PhenindioneEptifibatide may increase the anticoagulant activities of Phenindione.Approved
PhenprocoumonEptifibatide may increase the anticoagulant activities of Phenprocoumon.Approved
PrasugrelEptifibatide may increase the anticoagulant activities of Prasugrel.Approved
Protein S humanEptifibatide may increase the anticoagulant activities of Protein S human.Approved
ResveratrolResveratrol may increase the anticoagulant activities of Eptifibatide.Experimental, Investigational
ReteplaseEptifibatide may increase the anticoagulant activities of Reteplase.Approved
ReviparinEptifibatide may increase the anticoagulant activities of Reviparin.Approved
RidogrelRidogrel may increase the anticoagulant activities of Eptifibatide.Approved
RivaroxabanEptifibatide may increase the anticoagulant activities of Rivaroxaban.Approved
RosiglitazoneEptifibatide may increase the anticoagulant activities of Rosiglitazone.Approved, Investigational
Salicylic acidThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Salicylic acid.Approved, Vet Approved
SelexipagEptifibatide may increase the anticoagulant activities of Selexipag.Approved
SevofluraneSevoflurane may increase the anticoagulant activities of Eptifibatide.Approved, Vet Approved
SRT501SRT501 may increase the anticoagulant activities of Eptifibatide.Investigational
StreptokinaseEptifibatide may increase the anticoagulant activities of Streptokinase.Approved
SulodexideEptifibatide may increase the anticoagulant activities of Sulodexide.Approved, Investigational
TenecteplaseEptifibatide may increase the anticoagulant activities of Tenecteplase.Approved
TesmilifeneTesmilifene may increase the anticoagulant activities of Eptifibatide.Investigational
TicagrelorEptifibatide may increase the anticoagulant activities of Ticagrelor.Approved
TiclopidineEptifibatide may increase the anticoagulant activities of Ticlopidine.Approved
TinzaparinEptifibatide may increase the anticoagulant activities of Tinzaparin.Approved
TipranavirTipranavir may increase the antiplatelet activities of Eptifibatide.Approved, Investigational
TirofibanEptifibatide may increase the anticoagulant activities of Tirofiban.Approved
TositumomabThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Tositumomab.Approved
TranilastTranilast may increase the anticoagulant activities of Eptifibatide.Approved, Investigational
TrapidilTrapidil may increase the anticoagulant activities of Eptifibatide.Approved
TreprostinilTreprostinil may increase the antiplatelet activities of Eptifibatide.Approved, Investigational
TriflusalEptifibatide may increase the anticoagulant activities of Triflusal.Approved
UrokinaseEptifibatide may increase the anticoagulant activities of Urokinase.Approved, Investigational, Withdrawn
Vitamin EVitamin E may increase the antiplatelet activities of Eptifibatide.Approved, Nutraceutical, Vet Approved
VorapaxarEptifibatide may increase the anticoagulant activities of Vorapaxar.Approved
WarfarinEptifibatide may increase the anticoagulant activities of Warfarin.Approved
XimelagatranEptifibatide may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
Food InteractionsNot 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
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
1, 2CompletedTreatmentStrokes1
1, 2TerminatedTreatmentSickle Cell Disorders1
2CompletedTreatmentAcute Coronary Syndromes (ACS)1
2CompletedTreatmentBrain Infarction / Stroke, Ischemic / Strokes1
2CompletedTreatmentBrain Infarction / Strokes1
2CompletedTreatmentCoronary Heart Disease (CHD)1
2CompletedTreatmentStroke, Ischemic1
2RecruitingTreatmentAcute Coronary Syndromes (ACS) / Myocardial Infarction (MI) / Unstable Angina (UA)1
2RecruitingTreatmentStable Angina (SA) / Unstable Angina (UA)1
2TerminatedTreatmentPneumonia1
2TerminatedTreatmentST Elevation Myocardial Infarction (STEMI)1
2Unknown StatusTreatmentAcute Myocardial Infarction (AMI)1
2Unknown StatusTreatmentShock, Septic1
3CompletedSupportive CareCardiovascular Disease (CVD)1
3CompletedTreatmentAcute Coronary Syndromes (ACS)1
3CompletedTreatmentAcute Coronary Syndromes (ACS) / Myocardial Ischemia1
3CompletedTreatmentMyocardial Infarction (MI)1
3TerminatedTreatmentMyocardial Infarction (MI)1
4CompletedTreatmentCoronary Artery Disease / Myocardial Infarction (MI)1
4CompletedTreatmentNon ST Elevation Myocardial Infarction1
4TerminatedTreatmentAngioplasty1
4TerminatedTreatmentCoronary Artery Disease1
Not AvailableCompletedTreatmentStable Angina (SA)1
Pharmacoeconomics
Manufacturers
  • Schering corp
Packagers
Dosage forms
FormRouteStrength
InjectionIntravenous.75 mg/mL
InjectionIntravenous2 mg/mL
InjectionIntravenous20 mg/10mL
InjectionIntravenous200 mg/100mL
InjectionIntravenous75 mg/100mL
Injection, solutionIntravenous0.75 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
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

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 ]
Drug created on June 13, 2005 07:24 / Updated on June 24, 2017 04:19