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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.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Acute coronary syndrome (acs) •••••••••••• •••••••••••• •••••••• •••••••••••• ••••• ••••••••• Management of Percutaneous coronary intervention (pci) •••••••••••• •••••••• •••••• ••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- 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.
Target Actions Organism AIntegrin beta-3 modulatorHumans AIntegrin alpha-IIb modulatorHumans UVoltage-dependent N-type calcium channel antagonistHumans - 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
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- 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
Pathway Category Eptifibatide Action Pathway Drug 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbciximab The risk or severity of bleeding can be increased when Eptifibatide is combined with Abciximab. Abrocitinib The risk or severity of bleeding and thrombocytopenia can be increased when Eptifibatide is combined with Abrocitinib. 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. - 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
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- 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 EU 
Eptifibatide Accord Injection, solution 0.75 mg/ml Intravenous Accord Healthcare, S.L.U. 2016-09-08 Not applicable EU Eptifibatide Injection Solution 0.75 mg / mL Intravenous Teva Italia S.R.L. 2013-04-29 2018-04-30 Canada 
Eptifibatide Injection Solution 0.75 mg / mL Intravenous Fresenius Kabi Italia S.R.L. Not applicable Not applicable Canada Eptifibatide Injection Solution 2 mg / mL Intravenous Strides Pharma Canada Inc Not applicable Not applicable Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Eptifibatide Injection 0.75 mg/1mL Intravenous Amneal Pharmaceuticals LLC 2016-12-08 Not applicable US 
Eptifibatide Injection, solution 2 mg/1mL Intravenous Mylan Institutional Inc. 2021-04-01 Not applicable US Eptifibatide Injection 200 mg/100mL Intravenous Aurobindo Pharma (Italia) S.R.L. 2015-12-08 Not applicable US Eptifibatide Injection 2 mg/1mL Intravenous Slate Run Pharmaceuticals, Llc 2019-07-22 Not applicable US Eptifibatide Injection, solution 75 mg/100mL Intravenous McKesson Corporation dba SKY Packaging 2020-03-20 Not applicable US
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
- External Links
- PubChem Substance
- 46505459
- 75635
- ChEMBL
- CHEMBL1174
- Therapeutic Targets Database
- DAP000285
- PharmGKB
- PA449483
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Eptifibatide
- FDA label
- Download (87.5 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Unknown Status Not Available Coronary Ischemia 1 somestatus stop reason just information to hide 4 Completed Treatment Coronary Artery Disease (CAD) / Myocardial Infarction 1 somestatus stop reason just information to hide 4 Completed Treatment Non ST Segment Elevation Myocardial Infarction (NSTEMI) 1 somestatus stop reason just information to hide 4 Terminated Treatment Angioplasty 1 somestatus stop reason just information to hide 4 Terminated Treatment Coronary Artery Disease (CAD) 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Schering corp
- Packagers
- Assia Chemical Industries Ltd.
- Patheon Inc.
- Schering Corp.
- Schering-Plough Inc.
- Teva Pharmaceutical Industries Ltd.
- Dosage Forms
Form Route Strength Injection, solution Intravenous 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 0.75 MG/ML Injection, solution Intravenous 2 MG/ML Injection, solution Injection Intravenous Injection, solution Intravenous; Parenteral 0.75 MG/ML Injection, solution Intravenous; Parenteral 2 MG/ML 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 Injection Intravenous 2 mg/ml Injection Intravenous 0.75 mg/ml - Prices
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 ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5686570 No 1997-11-11 2014-11-11 US CA2133205 No 2007-04-17 2013-04-27 Canada US5807825 No 1998-09-15 2015-09-15 US
Properties
- State
- Liquid
- Experimental Properties
Property Value Source hydrophobicity -2.3 Not Available
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Modulator
- General 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/beta-3 recognize the sequence R-G-D in a wide array of ligands. Integrin alpha-IIb/beta-3 recognizes the sequence H-H-L-G-G-G-A-K-Q-A-G-D-V in fibrinogen gamma chain. Following activation integrin alpha-IIb/beta-3 brings about platelet/platelet interaction through binding of soluble fibrinogen. This step leads to rapid platelet aggregation which physically plugs ruptured endothelial surface. Fibrinogen binding enhances SELP expression in activated platelets (By similarity). ITGAV:ITGB3 binds to fractalkine (CX3CL1) and acts as its coreceptor in CX3CR1-dependent fractalkine signaling (PubMed:23125415, PubMed:24789099). ITGAV:ITGB3 binds to NRG1 (via EGF domain) and this binding is essential for NRG1-ERBB signaling (PubMed:20682778). ITGAV:ITGB3 binds to FGF1 and this binding is essential for FGF1 signaling (PubMed:18441324). ITGAV:ITGB3 binds to FGF2 and this binding is essential for FGF2 signaling (PubMed:28302677). ITGAV:ITGB3 binds to IGF1 and this binding is essential for IGF1 signaling (PubMed:19578119). ITGAV:ITGB3 binds to IGF2 and this binding is essential for IGF2 signaling (PubMed:28873464). ITGAV:ITGB3 binds to IL1B and this binding is essential for IL1B signaling (PubMed:29030430). ITGAV:ITGB3 binds to PLA2G2A via a site (site 2) which is distinct from the classical ligand-binding site (site 1) and this induces integrin conformational changes and enhanced ligand binding to site 1 (PubMed:18635536, PubMed:25398877). ITGAV:ITGB3 acts as a receptor for fibrillin-1 (FBN1) and mediates R-G-D-dependent cell adhesion to FBN1 (PubMed:12807887). In brain, plays a role in synaptic transmission and plasticity. Involved in the regulation of the serotonin neurotransmission, is required to localize to specific compartments within the synapse the serotonin receptor SLC6A4 and for an appropriate reuptake of serotonin. Controls excitatory synaptic strength by regulating GRIA2-containing AMPAR endocytosis, which affects AMPAR abundance and composition (By similarity). ITGAV:ITGB3 act as a receptor for CD40LG (PubMed:31331973). ITGAV:ITGB3 acts as a receptor for IBSP and promotes cell adhesion and migration to IBSP (PubMed:10640428)
- Specific Function
- cell adhesion molecule binding
- Gene Name
- ITGB3
- Uniprot ID
- P05106
- Uniprot Name
- Integrin beta-3
- Molecular Weight
- 87056.975 Da
References
- 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]
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Modulator
- General Function
- Integrin alpha-IIb/beta-3 is a receptor for fibronectin, fibrinogen, plasminogen, prothrombin, thrombospondin and vitronectin. It recognizes the sequence R-G-D in a wide array of ligands. It recognizes the sequence H-H-L-G-G-G-A-K-Q-A-G-D-V in fibrinogen gamma chain. Following activation integrin alpha-IIb/beta-3 brings about platelet/platelet interaction through binding of soluble fibrinogen. This step leads to rapid platelet aggregation which physically plugs ruptured endothelial cell surface
- Specific Function
- extracellular matrix binding
- Gene Name
- ITGA2B
- Uniprot ID
- P08514
- Uniprot Name
- Integrin alpha-IIb
- Molecular Weight
- 113375.96 Da
References
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1B gives rise to N-type calcium currents.
- Specific Function
- Voltage-gated calcium channel activity
Components:
| Name | UniProt ID |
|---|---|
| Voltage-dependent N-type calcium channel subunit alpha | A0A024R8I1 |
| Voltage-dependent N-type calcium channel subunit alpha-1B | Q00975 |
References
- Chong PH: Glycoprotein IIb/IIIa receptor antagonists in the management of cardiovascular diseases. Am J Health Syst Pharm. 1998 Nov 15;55(22):2363-86. doi: 10.1093/ajhp/55.22.2363. [Article]
Drug created at June 13, 2005 13:24 / Updated at October 11, 2024 18:19