Eptifibatide

Overview

The GP IIb/IIIa receptor (integrin αIIbβ3) binds fibrinogen and von Willebrand factor to cross-link platelets, the final step of aggregation regardless of the initiating stimulus. Eptifibatide contains a KGD (Lys-Gly-Asp) sequence that mimics the RGD motif fibrinogen uses to engage the receptor, competitively and reversibly occupying it.

In the pivotal PURSUIT trial of 10,948 patients with non-ST-elevation acute coronary syndromes, adding eptifibatide to aspirin and heparin significantly reduced death or non-fatal myocardial infarction. It is given as a weight-based intravenous bolus followed by a continuous infusion, typically during and after PCI.

Because it acts on the final aggregation pathway, its main risk is bleeding, and it is contraindicated in active bleeding, severe hypertension, recent haemorrhagic stroke or thrombocytopenia. Its short half-life and reversible binding mean platelet function recovers within hours of stopping the infusion. Dose is reduced in renal impairment.

Mechanism of Action

Its cyclic KGD pharmacophore mimics the RGD recognition sequence of fibrinogen, competing for the ligand-binding pocket of αIIbβ3. Occupancy is concentration-dependent and rapidly reversible; a bolus achieves high receptor blockade and the infusion sustains it. On discontinuation, dissociation restores aggregation within ~4 hours, unlike irreversible antibody inhibitors.

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