Eptifibatide (Integrilin®) is a highly specific, reversible, intravenously administered glycoprotein (GP) Ilb/IIIa receptor antagonist that acts at the final common step of the platelet aggregation pathway.

Data from large clinical trials indicate that intravenous eptifibatide as adjunctive therapy to standard care is effective in patients with non-ST-segment elevation (NSTE) acute coronary syndromes (ACS) and/or undergoing percutaneous coronary intervention (PCI). In the ESPRIT (Enhanced Suppression of the Platelet glycoprotein Ilb/IIIa Receptor with Integrilin® Therapy) trial in patients undergoing PCI with stenting, eptifibatide, compared with placebo, achieved significant reductions in death and ischaemic complications and was better than a strategy of reserving treatment for the bailout situation. In the large PURSUIT (Platelet IIb/ IIIa in Unstable angina: Receptor Suppression Using Integrilin Therapy) trial in patients with NSTE ACS, eptifibatide was associated with a significant reduction in the incidence of death or myocardial infarction (MI) compared with placebo. Eptifibatide is well tolerated in these trials. Ongoing trials are currently investigating the efficacy and tolerability of regimens that include this agent in other indications, including ST-segment elevation MI (STEMI).

Eptifibatide is a highly specific, reversible antagonist of the GP Ilb/IIIa receptor. It inhibited adenosine diphosphate-induced platelet aggregation as early as 5 minutes after drug administration in patients undergoing PCI or with ACS. After administration of a bolus dose of eptifibatide 180 μg/kg followed by a continuous infusion of 2.0 μg/kg/min to patients with non-ST-segment elevation myocardial infarction (NSTEMI) ACS, ex vivo inhibition of platelet aggregation was 84% at 15 minutes and >90% at steady state, with values returning to <50% of baseline 4 hours after infusion discontinuation.

The antiplatelet activity of eptifibatide was the same when coadministered with either unfractionated heparin or enoxaparin sodium. Additional eptifibatide therapy provides significant antiplatelet activity above that achieved with clopidogrel and aspirin (acetylsalicylic acid) alone.

Eptifibatide has linear, dose-proportional pharmacokinetics and steady state is achieved within 4–6 hours. It is approximately 25% bound to human plasma protein, with a volume of distribution of 0.2 L/kg. About 50% of the total body clearance of eptifibatide occurs via renal mechanisms. The elimination half-life of eptifibatide in patients undergoing PCI is 2.71 hours.

Eptifibatide was effective as adjunctive treatment in patients with low- to moderate-risk coronary artery disease undergoing PCI with intended intracoronary stent placement, in the large (n = 2064) ESPRIT trial. Eptifibatide achieved significant reductions in death and ischaemic complications and was better than a strategy of reserving treatment for the bailout situation. Adjuvant eptifibatide therapy provides significant long-term benefit (up to 12 months), with most of the benefit occurring within the first 48 hours.

In the large (n = 10 948) PURSUIT trial, eptifibatide was effective in patients with NSTE ACS (patients received standard care, including aspirin and unfrac-tionated heparin). Eptifibatide was associated with a significantly lower incidence of death or MI at 30 days than placebo, with the benefit evident early during drug treatment.

Limited data suggest that early administration of eptifibatide in the emergency room before primary PCI or administration of eptifibatide in …