Eptifibatide is a synthetic cyclic heptapeptide (MW ~831.9 g/mol) that acts as a reversible antagonist of the platelet glycoprotein IIb/IIIa (GP IIb/IIIa) receptor, inhibiting platelet aggregation. It was FDA-approved in 1998 (Integrilin) for the treatment of acute coronary syndrome (ACS) managed medically or with percutaneous coronary intervention (PCI). Eptifibatide is modeled after the Lys-Gly-Asp (KGD) sequence found in barbourin, a disintegrin from the venom of the southeastern pygmy rattlesnake (Sistrurus miliarius barbouri).
Category: Cardiovascular / Antiplatelet. Evidence rating: A (strong human clinical data).
Clinical status: FDA-approved (Integrilin for ACS/PCI, 1998)
Eptifibatide is a competitive, reversible antagonist of the glycoprotein IIb/IIIa (integrin alpha-IIb/beta-3) receptor on the platelet surface. GP IIb/IIIa is the final common pathway of platelet aggregation, binding fibrinogen and von Willebrand factor to crosslink activated platelets.…
Safety considerations: Common: bleeding is the primary adverse effect — major bleeding (4.4% eptifibatide vs 3.3% placebo in PURSUIT), including access site bleeding during PCI; Thrombocytopenia: acute profound thrombocytopenia (<20,000/mm3) reported in ~0.2% of patients; platelet counts should be monitored within 6 hours of treatment initiation; Hypotension may occur, particularly in the setting of bleeding.
Reviewed by the PeptideAtlas Editorial Team.
| Molecular weight | ~831.9 g/mol |
|---|---|
| CAS number | 148031-34-9 |
| Half-life | ~2.5 hours |
| Bioavailability | 100% (intravenous) |
| Production method | synthetic |
| Anti-doping status | not-listed |
| US regulatory status | FDA-approved (Integrilin, 1998) for ACS managed medically or with PCI. Generic versions available. |
Both are GP IIb/IIIa inhibitors used during PCI, but they differ in structure and pharmacokinetics. Eptifibatide is a small cyclic peptide with reversible binding and a short half-life (~2.5 hours), while abciximab (ReoPro) is a monoclonal antibody fragment with tighter, longer-lasting binding (platelet inhibition persists 24-48 hours). Eptifibatide's rapid reversibility is advantageous when…
Use of GP IIb/IIIa inhibitors has declined with the advent of potent oral P2Y12 inhibitors (prasugrel, ticagrelor) and bivalirudin as alternatives during PCI. However, eptifibatide remains available and is used selectively, particularly in high-risk PCI settings or as bailout therapy for thrombotic complications.
Eptifibatide was designed based on barbourin, a disintegrin protein found in the venom of the southeastern pygmy rattlesnake. Barbourin contains a unique KGD motif (instead of the usual RGD) that selectively inhibits GP IIb/IIIa. Eptifibatide is a synthetic cyclic peptide incorporating this KGD sequence; it is not extracted from snake venom.