DT-Web

DB00063 - Eptifibatide


Identification
Name Eptifibatide
Accession Number DB00063 (BIOD00063, BTD00063)
Type biotech
Description Synthetic cyclic hexapeptide that binds to platelet receptor glycoprotein and inhibits platelet aggregation.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 831.9620
Groups approved
Monoisotopic Weight Not Available
Pharmacology
Indication For treatment of myocardial infarction and acute coronary syndrome.
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.
Absorption Not Available
Protein binding Approximately 25%
Biotransformation 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
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
Interactions
Drug Interactions
Drug Mechanism of interaction
Ginkgo biloba Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
Tirofiban Additive effects. Concomitant use is contraindicated.
Treprostinil The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Eptifibatide. Monitor for increased bleeding during concomitant thearpy.
Food Interactions Not Available

Targets


Integrin beta-3
Name Integrin beta-3
Gene Name ITGB3
Pharmacological action yes
Actions Not Available
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. - Pubmed
  • Schror K, Weber AA: Comparative pharmacology of GP IIb/IIIa antagonists. J Thromb Thrombolysis. 2003 Apr;15(2):71-80. - Pubmed
  • 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
  • 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
  • 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
  • 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
  • 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
DTHybrid score 0.8413

Predictions


Id Partner name Gene Name Score
488 Integrin alpha-IIb ITGA2B 0.2792
6065 Integrin beta-1 ITGB1 0.0625
660 T-cell surface glycoprotein CD1a CD1A 0.0624
6063 Major histocompatibility complex class I-related gene protein MR1 0.0624
5955 T-cell surface glycoprotein CD4 CD4 0.0624
6066 Integrin alpha-V ITGAV 0.0624
3820 Low affinity immunoglobulin gamma Fc region receptor II-b FCGR2B 0.0563
942 T-lymphocyte activation antigen CD86 CD86 0.0501
1733 Vitronectin VTN 0.0401
572 Integrin alpha-L ITGAL 0.0383
2782 Complement C1s subcomponent C1S 0.0246
3815 Complement C1q subcomponent subunit A C1QA 0.0225
3816 Complement C1q subcomponent subunit B C1QB 0.0225
3817 Complement C1q subcomponent subunit C C1QC 0.0225
1102 Low affinity immunoglobulin gamma Fc region receptor III-B FCGR3B 0.0223
3818 Low affinity immunoglobulin gamma Fc region receptor III-A FCGR3A 0.0223
3819 Low affinity immunoglobulin gamma Fc region receptor II-a FCGR2A 0.0223
3821 Low affinity immunoglobulin gamma Fc region receptor II-c FCGR2C 0.0223
3814 Complement C1r subcomponent C1R 0.0223
784 High affinity immunoglobulin gamma Fc receptor I FCGR1A 0.0216
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