Eptifibatide is a potent glycoprotein IIb/IIIa antagonist (GPIIb/IIIa; Kd = 120 nM) that inhibits platelet aggregation.1,2 Eptifibatide prevents binding of the adhesion proteins fibrinogen and von Willebrand factor to GPIIb/IIIa on the surface of activated platelets to prevent aggregation and thrombus formation.3 It inhibits ADP-induced citrated blood aggregation (IC50 = 0.11-0.22 μg/ml) in vitro and in vivo (IC50 = 52 μg/ml in porcine plasma).1,4 Formulations containing eptifibatide have been used to reduce risk of thrombolysis in myocardial infarction in patients undergoing percutaneous coronary intervention.5
1.Harder, S., Klinkhardt, U., Graff, J., et al.In vitro dose response to different GPIIb/IIIa-antagonists: Inter-laboratory comparison of various platelet function testsThromb. Res.102(1)39-48(2001) 2.Moser, M., Bertram, U., Peter, K., et al.Abciximab, eptifibatide, and tirofiban exhibit dose-dependent potencies to dissolve platelet aggregatesJ. Cardiovasc. Pharmacol.41(4)586-592(2003) 3.Scarborough, R.M.Development of eptifibatideAm. Heart J.138(6 Pt 1)1093-1104(1999) 4.Ciborowski, M., and Tomasiak, M.The in vitro effect of eptifibatide, a glycoprotein IIb/IIIa antagonist, on various responses of porcine blood plateletsActa Pol. Pharm.66(3)235-242(2009) 5.Zhou, X., Wu, X., Sun, H., et al.Efficacy and safety of eptifibatide versus tirofiban in acute coronary syndrome patients: A systematic review and meta-analysisJ. Evid. Based Med.10(2)136-144(2017)