PRODUCT LITERATURE
Clinical Pharmacology of Eptifibatide
Activation of receptor function of platelet membrane
glycoprotein (GP) IIb-IIIa leads to the binding of fibrinogen and is the final common pathway to platelet aggregation. Platelet aggregates provide the structural basis
for coronary thrombosis, a major cause of ischemic
heart disease. GP IIb-IIIa has a narrow tissue distribution, being found only on platelets and their progenitors,
and inhibition of its receptor function has emerged as a
promising new therapeutic strategy for management of
acute ischemic coronary syndromes and acute ischemic
complications of percutaneous coronary interventions.
Eptifibatide (INTEGRILIN) is a cyclic heptapeptide inhibitor of GP IIb-IIIa, with an active pharmacophore that is
derived from the structure of barbourin, a GP IIb-IIIa
inhibitor from the venom of the southeastern pigmy
rattlesnake. Like barbourin, eptifibatide is a specific and
robust inhibitor of the GP IIb-IIIa receptor function, having a low affinity for other integrins and strongly preventing platelet aggregation
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