Quick summary
Eptifibatide (Integrilin) is an FDA-approved cyclic heptapeptide from rattlesnake venom that reversibly blocks GPIIb/IIIa to inhibit platelet aggregation. Used IV in acute coronary syndrome and as a PCI adjunct.
Overview
Eptifibatide (Integrilin) is an FDA-approved cyclic heptapeptide antiplatelet agent derived from a disintegrin protein found in the venom of the southeastern pygmy rattlesnake. It is used intravenously in the management of acute coronary syndrome and as an adjunct to percutaneous coronary intervention (PCI) to reduce the risk of cardiac ischemic events.
Mechanism of action
Eptifibatide reversibly inhibits platelet aggregation by selectively blocking the glycoprotein IIb/IIIa (GPIIb/IIIa) receptor on the platelet surface. GPIIb/IIIa is the predominant receptor mediating platelet aggregation; it binds fibrinogen and von Willebrand factor, enabling platelets to cross-link and form a thrombus. Eptifibatide's RGD-mimetic KGD sequence occupies the fibrinogen-binding pocket of GPIIb/IIIa with high affinity, competitively displacing these ligands. Because inhibition is reversible, platelet function recovers within 4–8 hours of discontinuation as drug dissociates and plasma levels fall. The cyclic peptide structure confers selectivity over RGD-binding integrins on other cell types, reducing off-target effects compared to non-cyclic RGD peptides.
Dosing protocols
| Purpose | Route | Dosage | Frequency | Notes |
|---|---|---|---|---|
| acute coronary syndrome | intravenous | 180–180 mcg/kg | IV bolus, then 2 mcg/kg/min infusion for up to 72 hours | Initial 180 mcg/kg bolus followed by continuous infusion. Dose-adjust in renal impairment (CrCl <50 mL/min). Monitor for bleeding. |
| percutaneous coronary intervention adjunct | intravenous | 180–180 mcg/kg | Double bolus 10 min apart, then 2 mcg/kg/min infusion for 18–24 hours | Two 180 mcg/kg boluses 10 minutes apart at time of PCI per ESPRIT protocol. Maintain infusion through procedure and 18–24 hours post-PCI. |
Dosing information is for educational purposes only. Consult a qualified healthcare professional before using any peptide.
Research summary
Eptifibatide received FDA approval in 1998 based on the PURSUIT and ESPRIT clinical trials. PURSUIT (10,948 patients) demonstrated a significant reduction in the composite endpoint of death or myocardial infarction at 30 days compared to placebo in ACS patients. ESPRIT confirmed benefit as a PCI adjunct. Post-approval research has evaluated eptifibatide in combination with thrombolytics and in specific high-risk PCI subgroups. Its short half-life and reversibility make it preferable to abciximab when rapid offset is desired.[1][2][3][4][5]
Evidence grading
Each claimed benefit is graded by the strength of available evidence. Grades reflect study quality, not effect size.
Strong = multiple RCTs · Moderate = limited trials or observational · Preliminary = animal or in vitro only · Insufficient = anecdotal or no published data
Side effects
Side effects vary by individual. This is not an exhaustive list. Report unusual symptoms to a healthcare professional.
Common stacks
Peptides commonly paired with Eptifibatide for synergistic effects.
Legal status
FDA-approved since 1998 for ACS and PCI adjunct therapy. Available as an intravenous injection for hospital and procedural suite use only. Schedule: not a controlled substance. Requires medical supervision and cardiac monitoring during infusion.
Sourcing & access
Prescription required
Eptifibatide is an FDA-approved prescription medication available through licensed healthcare providers, telehealth platforms, and 503A/503B compounding pharmacies.
Frequently asked questions
Eptifibatide (brand name Integrilin) is an FDA-approved cyclic heptapeptide derived from the disintegrin barbourin, found in pygmy rattlesnake venom. It is an intravenous antiplatelet agent used in acute coronary syndrome (ACS) and percutaneous coronary intervention (PCI) to prevent thrombotic complications. Its peptide structure and venomous origin place it among a class of naturally-inspired cardiovascular peptide drugs.
Eptifibatide reversibly blocks the glycoprotein IIb/IIIa (GPIIb/IIIa) receptor on platelet surfaces using a KGD (Lys-Gly-Asp) sequence that mimics the RGD fibrinogen binding sequence. This prevents fibrinogen crosslinking between activated platelets, blocking aggregation. Platelet function recovers within 4 to 8 hours after discontinuation, making eptifibatide one of the shorter-acting agents in this drug class.
The primary risk is bleeding, including major and intracranial hemorrhage. Thrombocytopenia occurs in approximately 0.5 to 1 percent of patients and can be severe. Hypotension and injection site reactions may also occur. Dose adjustment is required for patients with reduced kidney function (creatinine clearance below 50 mL/min) due to renal excretion. It is contraindicated in severe bleeding disorders, recent stroke, and uncontrolled hypertension.
The PURSUIT trial enrolling 10,948 patients with non-ST-elevation ACS demonstrated significant reduction in the composite endpoint of death or myocardial infarction at 30 days. The ESPRIT trial confirmed benefit in elective PCI, showing reduced 48-hour and 30-day ischemic events. These large randomized trials established eptifibatide as a standard component of high-risk ACS and PCI management.
Research references
- Inhibition of Platelet Glycoprotein IIb/IIIa with Eptifibatide in Patients with Acute Coronary Syndromes (PURSUIT Trial)PubMed
- Eptifibatide: A Cyclic Peptide That Selectively Inhibits Platelet Glycoprotein IIb/IIIaPubMed
- Pharmacodynamics and Pharmacokinetics of Eptifibatide in Patients with Acute Coronary Syndromes: Prospective Analysis from PURSUITPubMed
- The Role of Eptifibatide in Patients Undergoing Percutaneous Coronary InterventionPubMed
- Eptifibatide: A Potent Inhibitor of the Platelet Receptor Integrin, Glycoprotein IIb/IIIaPubMed