IV antiplatelet · coronary syndromes
Eptifibatide is a small cyclic peptide given intravenously in hospital to keep platelets from clumping during acute coronary syndromes and coronary stenting. Its design was modeled on barbourin, a peptide from the venom of the southeastern pygmy rattlesnake. It was first marketed as Integrilin and is now available as generics.
When platelets are activated, a surface receptor called glycoprotein IIb/IIIa changes shape and binds fibrinogen and von Willebrand factor, which link neighboring platelets together into a clot. Eptifibatide occupies this receptor and blocks those binding proteins, so activated platelets cannot cross-link5. Its receptor-binding motif was modeled on barbourin's lysine-glycine-aspartate sequence, which favors the platelet receptor over related integrins found on other cells1,2. The block is reversible: when the infusion stops, eptifibatide is thought to dissociate from platelets and aggregation recovers5. Because it acts on the final shared step of platelet aggregation, it has been studied as an addition to aspirin and heparin rather than a replacement for them.
Researchers screening 62 snake venoms in 1991 found that only one, from the southeastern pygmy rattlesnake, blocked the platelet receptor selectively; the active peptide, barbourin, owed that selectivity to its lysine-glycine-aspartate motif1. Chemists then built that motif into a small, ring-constrained peptide, which became eptifibatide2.
In the PURSUIT trial, 10,948 patients with acute coronary syndromes without persistent ST elevation received eptifibatide or placebo on top of standard care including aspirin and heparin. Death or heart attack at 30 days fell from 15.7 to 14.2 percent, a modest absolute benefit; bleeding was more common, without a rise in hemorrhagic stroke, and the benefit was not apparent in women3.
In ESPRIT, 2,064 patients having non-urgent coronary stenting were randomized to eptifibatide or placebo; by six months, death or heart attack had occurred in 7.5 versus 11.5 percent, with most of the benefit arising in the first 48 hours4. The label's clinical data come from these trials and a third, IMPACT II, in patients mostly having balloon angioplasty5.
The FDA approved eptifibatide in 1998, as Integrilin, for acute coronary syndromes managed medically or with percutaneous coronary intervention, and for patients undergoing PCI including stenting5. The Integrilin brand is discontinued, but generic versions remain approved6.
Bleeding is the most common complication, most often at the catheter access site or in the gut or urinary tract, and the label calls for minimizing punctures and other trauma. Low blood pressure is the other frequent reaction, and low platelet counts can occur. It must not be used after a recent bleed, recent major surgery, a recent stroke or any past brain bleed, with severe uncontrolled high blood pressure, with dialysis dependence, or with another IV IIb/IIIa blocker. Anaphylaxis has been reported5.
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