Eptifibatide

Identification

Summary

Eptifibatide is a peptide-based antagonist for glycoprotein IIb/IIIa used in the medical management of myocardial infarction and as an adjunct to percutaneous coronary intervention.

Brand Names
Integrilin
Generic Name
Eptifibatide
DrugBank Accession Number
DB00063
Background

Synthetic cyclic hexapeptide that binds to platelet receptor glycoprotein and inhibits platelet aggregation. Derived from venom of the Southeastern pygmy rattlesnake (Sistrurus miliarus barbouri), eptifibatide is a cyclic heptapeptide that belongs to the class of arginin-glycin-aspartat-mimetics.

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Other protein based therapies
Protein Chemical Formula
C35H49N11O9S2
Protein Average Weight
831.962 Da
Sequences
Not Available
Synonyms
  • Eptifibatida
  • Eptifibatide
  • Integrelin
  • Intrifiban

Pharmacology

Indication

For treatment of myocardial infarction and acute coronary syndrome.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Eptifibatide is an anti-coagulant that selectively and reversibly blocks the platelet glycoprotein IIb/IIIa receptor.

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.

TargetActionsOrganism
AIntegrin beta-3Not AvailableHumans
Absorption

Not Available

Volume of distribution

Not 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 elimination

Not Available

Half-life

Approximately 2.5 hours

Clearance
  • 55 mL/kg/h [patients with coronary artery disease]
Adverse Effects
Medicalerrors
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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)

Pathways
PathwayCategory
Eptifibatide Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbciximabThe risk or severity of bleeding can be increased when Eptifibatide is combined with Abciximab.
AceclofenacThe risk or severity of bleeding can be increased when Aceclofenac is combined with Eptifibatide.
AcemetacinThe risk or severity of bleeding can be increased when Acemetacin is combined with Eptifibatide.
AcenocoumarolThe risk or severity of bleeding can be increased when Eptifibatide is combined with Acenocoumarol.
Acetylsalicylic acidAcetylsalicylic acid may increase the antiplatelet activities of Eptifibatide.
AlclofenacThe risk or severity of bleeding can be increased when Alclofenac is combined with Eptifibatide.
AldesleukinThe risk or severity of bleeding can be increased when Eptifibatide is combined with Aldesleukin.
AlemtuzumabThe risk or severity of bleeding can be increased when Eptifibatide is combined with Alemtuzumab.
AlteplaseThe risk or severity of bleeding can be increased when Eptifibatide is combined with Alteplase.
AltretamineThe risk or severity of bleeding can be increased when Eptifibatide is combined with Altretamine.
Interactions
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Food Interactions
  • Avoid herbs and supplements with anticoagulant/antiplatelet activity. The use of anticoagulant/antiplatelet herbs with eptifibatide may increase the risk of bleeding. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Products

Products
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Eptifibatide AccordInjection, solution2 mg/mlIntravenousAccord Healthcare S.L.U.2016-09-08Not applicableEU flag
Eptifibatide AccordInjection, solution0.75 mg/mlIntravenousAccord Healthcare S.L.U.2016-09-08Not applicableEU flag
Eptifibatide InjectionSolution0.75 mg / mLIntravenousOmega Laboratories LtdNot applicableNot applicableCanada flag
Eptifibatide InjectionSolution2 mg / mLIntravenousTEVA Canada Limited2013-04-292018-04-30Canada flag
Eptifibatide InjectionSolution2 mg / mLIntravenousAccord Healthcare IncNot applicableNot applicableCanada flag
Eptifibatide InjectionSolution0.75 mg / mLIntravenousStrides Pharma Canada IncNot applicableNot applicableCanada flag
Eptifibatide InjectionSolution2 mg / mLIntravenousFresenius KabiNot applicableNot applicableCanada flag
Eptifibatide InjectionSolution0.75 mg / mLIntravenousAccord Healthcare IncNot applicableNot applicableCanada flag
Eptifibatide InjectionSolution2 mg / mLIntravenousOmega Laboratories LtdNot applicableNot applicableCanada flag
Eptifibatide InjectionSolution0.75 mg / mLIntravenousTEVA Canada Limited2013-04-292018-04-30Canada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
EptifibatideInjection, solution2 mg/1mLIntravenousMylan Institutional LLC2021-04-01Not applicableUS flag
EptifibatideInjection2 mg/1mLIntravenousSlate Run Pharmaceuticals, Llc2019-07-22Not applicableUS flag
EptifibatideInjection, solution0.75 mg/1mLIntravenousSagent Pharmaceuticals2018-07-15Not applicableUS flag
EptifibatideInjection200 mg/100mLIntravenousAuro Medics Pharma Llc2015-12-08Not applicableUS flag
EptifibatideInjection, solution20 mg/10mLIntravenousMcKesson Corporation dba SKY Packaging2020-03-20Not applicableUS flag
EptifibatideInjection200 mg/100mLIntravenousAurobindo Pharma2015-12-08Not applicableUS flag
EptifibatideInjection, solution2 mg/1mLIntravenousAkorn, Inc.2017-04-18Not applicableUS flag
EptifibatideInjection200 mg/100mLIntravenousBaxter Healthcare Corporation2019-02-01Not applicableUS flag
EptifibatideInjection, solution2 mg/1mLIntravenousMylan Institutional LLC2018-10-01Not applicableUS flag
EptifibatideInjection, solution0.75 mg/1mLIntravenousTeva Parenteral Medicines, Inc.2015-12-142018-10-11US flag

Categories

ATC Codes
B01AC16 — Eptifibatide
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
NA8320J834
CAS number
188627-80-7

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. [Article]
PubChem Substance
46505459
RxNav
75635
ChEMBL
CHEMBL1174
Therapeutic Targets Database
DAP000285
PharmGKB
PA449483
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Eptifibatide
AHFS Codes
  • 20:12.18 — Platelet Aggregation Inhibitors
FDA label
Download (87.5 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentCoronary Artery Disease (CAD) / Myocardial Infarction1
4CompletedTreatmentNon ST Elevation Myocardial Infarction1
4TerminatedTreatmentAngioplasty1
4TerminatedTreatmentCoronary Artery Disease (CAD)1
3CompletedSupportive CareCardiovascular Disease (CVD)1
3CompletedTreatmentAcute Coronary Syndrome (ACS)1
3CompletedTreatmentAcute Coronary Syndrome (ACS) / Myocardial Ischemia1
3CompletedTreatmentMyocardial Infarction2
3RecruitingTreatmentAcute Ischemic Stroke (AIS)2
3TerminatedTreatmentMyocardial Infarction1

Pharmacoeconomics

Manufacturers
  • Schering corp
Packagers
  • Assia Chemical Industries Ltd.
  • Patheon Inc.
  • Schering Corp.
  • Schering-Plough Inc.
  • Teva Pharmaceutical Industries Ltd.
Dosage Forms
FormRouteStrength
InjectionIntravenous0.75 mg/1mL
InjectionIntravenous2 mg/1mL
InjectionIntravenous20 mg/10mL
InjectionIntravenous200 mg/100mL
InjectionIntravenous75 mg/100mL
Injection, solutionIntravenous0.75 mg/1mL
Injection, solutionIntravenous2 mg/1mL
Injection, solutionIntravenous20 mg/10mL
Injection, solutionIntravenous200 mg/100mL
Injection, solutionIntravenous75 mg/100mL
Injection, solutionIntravenous
Injection, solution
InjectionIntravenous
Injection, solutionIntravenous0.75 mg/ml
Injection, solutionIntravenous2 mg/ml
Injection, solutionIntravenous; Parenteral
SolutionIntravenous0.75 mg / mL
SolutionIntravenous2 mg / mL
SolutionIntravenous2 mg/1ml
SolutionIntravenous0.75 mg/1ml
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)Region
US5686570No1997-11-112014-11-11US flag
CA2133205No2007-04-172013-04-27Canada flag
US5807825No1998-09-152015-09-15US flag

Properties

State
Liquid
Experimental Properties
PropertyValueSource
hydrophobicity-2.3Not Available

Targets

Drugtargets
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Kind
Protein
Organism
Humans
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 Wil...
Gene Name
ITGB3
Uniprot ID
P05106
Uniprot Name
Integrin beta-3
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. [Article]
  2. Schror K, Weber AA: Comparative pharmacology of GP IIb/IIIa antagonists. J Thromb Thrombolysis. 2003 Apr;15(2):71-80. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]

Drug created on June 13, 2005 13:24 / Updated on June 13, 2021 16:24