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
- Generic Name
- DrugBank Accession Number
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.
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Other protein based therapies
- Protein Chemical Formula
- Protein Average Weight
- 831.962 Da
- Not Available
For treatment of myocardial infarction and acute coronary syndrome.Accelerate your drug discovery research with the industry’s only fully connected ADMET dataset, ideal for:Accelerate your drug discovery research with our fully connected ADMET dataset
- Associated Conditions
- Contraindications & Blackbox Warnings
- Contraindications & Blackbox WarningsWith our commercial data, access important information on dangerous risks, contraindications, and adverse effects.Our Blackbox Warnings cover Risks, Contraindications, and Adverse Effects
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.
Target Actions Organism AIntegrin beta-3 Not Available Humans
- Volume of distribution
- Protein binding
No major metabolites have been detected in human plasma. Deamidated eptifibatide and other, more polar metabolites have been detected in urine.
- Route of elimination
Approximately 2.5 hours
- 55 mL/kg/h [patients with coronary artery disease]
- Adverse Effects
- Reduce medical errorsand improve treatment outcomes with our comprehensive & structured data on drug adverse effects.Reduce medical errors & improve treatment outcomes with our adverse effects data
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)
Pathway Category Eptifibatide Action Pathway Drug action
- Pharmacogenomic Effects/ADRs
- Not Available
- 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.
Drug Interaction Abciximab The risk or severity of bleeding can be increased when Eptifibatide is combined with Abciximab. Aceclofenac The risk or severity of bleeding can be increased when Aceclofenac is combined with Eptifibatide. Acemetacin The risk or severity of bleeding can be increased when Acemetacin is combined with Eptifibatide. Acenocoumarol The risk or severity of bleeding can be increased when Eptifibatide is combined with Acenocoumarol. Acetylsalicylic acid Acetylsalicylic acid may increase the antiplatelet activities of Eptifibatide. Alclofenac The risk or severity of bleeding can be increased when Alclofenac is combined with Eptifibatide. Aldesleukin The risk or severity of bleeding can be increased when Eptifibatide is combined with Aldesleukin. Alemtuzumab The risk or severity of bleeding can be increased when Eptifibatide is combined with Alemtuzumab. Alteplase The risk or severity of bleeding can be increased when Eptifibatide is combined with Alteplase. Altretamine The risk or severity of bleeding can be increased when Eptifibatide is combined with Altretamine.Improve patient outcomesBuild effective decision support tools with the industry’s most comprehensive drug-drug interaction checker.Learn more
- 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.
- Comprehensive & structured drug product infoFrom application numbers to product codes, connect different identifiers through our commercial datasets.Easily connect various identifiers back to our datasets
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Eptifibatide Accord Injection, solution 2 mg/ml Intravenous Accord Healthcare S.L.U. 2016-09-08 Not applicable Eptifibatide Accord Injection, solution 0.75 mg/ml Intravenous Accord Healthcare S.L.U. 2016-09-08 Not applicable Eptifibatide Injection Solution 0.75 mg / mL Intravenous Omega Laboratories Ltd Not applicable Not applicable Eptifibatide Injection Solution 2 mg / mL Intravenous TEVA Canada Limited 2013-04-29 2018-04-30 Eptifibatide Injection Solution 2 mg / mL Intravenous Accord Healthcare Inc Not applicable Not applicable Eptifibatide Injection Solution 0.75 mg / mL Intravenous Strides Pharma Canada Inc Not applicable Not applicable Eptifibatide Injection Solution 2 mg / mL Intravenous Fresenius Kabi Not applicable Not applicable Eptifibatide Injection Solution 0.75 mg / mL Intravenous Accord Healthcare Inc Not applicable Not applicable Eptifibatide Injection Solution 2 mg / mL Intravenous Omega Laboratories Ltd Not applicable Not applicable Eptifibatide Injection Solution 0.75 mg / mL Intravenous TEVA Canada Limited 2013-04-29 2018-04-30
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Eptifibatide Injection, solution 2 mg/1mL Intravenous Mylan Institutional LLC 2021-04-01 Not applicable Eptifibatide Injection 2 mg/1mL Intravenous Slate Run Pharmaceuticals, Llc 2019-07-22 Not applicable Eptifibatide Injection, solution 0.75 mg/1mL Intravenous Sagent Pharmaceuticals 2018-07-15 Not applicable Eptifibatide Injection 200 mg/100mL Intravenous Auro Medics Pharma Llc 2015-12-08 Not applicable Eptifibatide Injection, solution 20 mg/10mL Intravenous McKesson Corporation dba SKY Packaging 2020-03-20 Not applicable Eptifibatide Injection 200 mg/100mL Intravenous Aurobindo Pharma 2015-12-08 Not applicable Eptifibatide Injection, solution 2 mg/1mL Intravenous Akorn, Inc. 2017-04-18 Not applicable Eptifibatide Injection 200 mg/100mL Intravenous Baxter Healthcare Corporation 2019-02-01 Not applicable Eptifibatide Injection, solution 2 mg/1mL Intravenous Mylan Institutional LLC 2018-10-01 Not applicable Eptifibatide Injection, solution 0.75 mg/1mL Intravenous Teva Parenteral Medicines, Inc. 2015-12-14 2018-10-11
- ATC Codes
- B01AC16 — Eptifibatide
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Not Available
- Organic Compounds
- Super Class
- Organic Acids
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Alternative Parents
- Not Available
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
- CAS number
- 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
- 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]
- AHFS Codes
- 20:12.18 — Platelet Aggregation Inhibitors
- FDA label
- Download (87.5 KB)
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Coronary Artery Disease (CAD) / Myocardial Infarction 1 4 Completed Treatment Non ST Elevation Myocardial Infarction 1 4 Terminated Treatment Angioplasty 1 4 Terminated Treatment Coronary Artery Disease (CAD) 1 3 Completed Supportive Care Cardiovascular Disease (CVD) 1 3 Completed Treatment Acute Coronary Syndrome (ACS) 1 3 Completed Treatment Acute Coronary Syndrome (ACS) / Myocardial Ischemia 1 3 Completed Treatment Myocardial Infarction 2 3 Recruiting Treatment Acute Ischemic Stroke (AIS) 2 3 Terminated Treatment Myocardial Infarction 1
- Schering corp
- Assia Chemical Industries Ltd.
- Patheon Inc.
- Schering Corp.
- Schering-Plough Inc.
- Teva Pharmaceutical Industries Ltd.
- Dosage Forms
Form Route Strength Injection Intravenous 0.75 mg/1mL Injection Intravenous 2 mg/1mL Injection Intravenous 20 mg/10mL Injection Intravenous 200 mg/100mL Injection Intravenous 75 mg/100mL Injection, solution Intravenous 0.75 mg/1mL Injection, solution Intravenous 2 mg/1mL Injection, solution Intravenous 20 mg/10mL Injection, solution Intravenous 200 mg/100mL Injection, solution Intravenous 75 mg/100mL Injection, solution Intravenous Injection, solution Injection Intravenous Injection, solution Intravenous 0.75 mg/ml Injection, solution Intravenous 2 mg/ml Injection, solution Intravenous; Parenteral Solution Intravenous 0.75 mg / mL Solution Intravenous 2 mg / mL Solution Intravenous 2 mg/1ml Solution Intravenous 0.75 mg/1ml Solution Intravenous 0.75 mg Solution Intravenous 2 mg
Unit description Cost Unit Integrilin 20 mg/10 ml vial 12.41USD ml Integrilin 200 mg/100 ml vial 10.74USD ml Integrilin 75 mg/100 ml vial 3.88USD mlDrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patent Number Pediatric Extension Approved Expires (estimated) Region US5686570 No 1997-11-11 2014-11-11 CA2133205 No 2007-04-17 2013-04-27 US5807825 No 1998-09-15 2015-09-15
- Experimental Properties
Property Value Source hydrophobicity -2.3 Not Available
- Pharmacological action
- 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
- Uniprot ID
- Uniprot Name
- Integrin beta-3
- Molecular Weight
- 87056.975 Da
- 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]
- Schror K, Weber AA: Comparative pharmacology of GP IIb/IIIa antagonists. J Thromb Thrombolysis. 2003 Apr;15(2):71-80. [Article]
- 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]
- 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]
- 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]
- 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]
- 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