Eptifibatide
Cardiovascular / AntiplateletAlso known as: Integrilin, Eptifibatide Injection
Mechanism
Eptifibatide is an IV antiplatelet drug derived from the venom of the southeastern pygmy rattlesnake. It blocks the GPIIb/IIIa receptor on platelets — the final common pathway for platelet clumping — making it one of the most potent antiplatelet agents available. It is used during heart attacks and coronary procedures to prevent blood clots.
Technical detail
Eptifibatide is a cyclic heptapeptide containing a KGD (Lys-Gly-Asp) motif, designed from barbourin (a disintegrin from Sistrurus miliarius barbouri venom). It is a competitive, reversible antagonist of the platelet glycoprotein IIb/IIIa (integrin alphaIIb-beta3) receptor, blocking fibrinogen, von Willebrand factor, and other ligand binding to prevent platelet cross-linking and aggregation. >80% inhibition of platelet aggregation achieved at therapeutic doses. Short half-life (~2.5 hours) with rapid offset, and predominantly renal clearance. The KGD motif provides selectivity over other RGD-dependent integrins.