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Eptifibatide: quick citable summary
Eptifibatide is listed by PeptaHub as a other peptide with a prescription legal-status classification. The page summarizes mechanism, research context, common routes, safety notes, and references for writers and AI answer engines.
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What is Eptifibatide?
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 quickly once the infusion stops: US labeling states that inhibition of platelet aggregation falls below 50% within 4 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.
Reported study ranges
| Purpose | Route | Reported range | 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 as soon as possible after diagnosis, then continuous infusion until hospital discharge or CABG, up to 72 hours. If creatinine clearance is below 50 mL/min, reduce the infusion to 1 mcg/kg/min; the bolus is unchanged. Contraindicated in dialysis-dependent patients. 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 | First 180 mcg/kg bolus immediately before PCI with the infusion started at the same time, then a second 180 mcg/kg bolus 10 minutes after the first, per the ESPRIT protocol. Maintain the infusion through the procedure and for 18 to 24 hours post-PCI. Reduce the infusion to 1 mcg/kg/min if creatinine clearance is below 50 mL/min. |
Reported ranges are for research context only. Consult a qualified healthcare professional before using any peptide.
Convert Eptifibatide research-range units
Need to convert mg to mcg, dose volume, or U-100 syringe units? Use the peptide dose unit converter for educational calculation support.
Research summary
Eptifibatide received FDA approval in 1998 on the basis of PURSUIT, which enrolled 10,948 patients with non-ST-elevation ACS and showed a significant reduction in the composite endpoint of death or myocardial infarction at 30 days versus placebo. ESPRIT (Lancet 2000, n=2,064) tested the double-bolus regimen in planned coronary stent implantation and was stopped early for efficacy: the 48-hour primary composite fell from 10.5% to 6.6% (P=0.0015) and the 30-day secondary composite from 10.5% to 6.8% (P=0.0034). That benefit came with more bleeding — major bleeding 1.3% versus 0.4% (P=0.027) — which is the trade-off the trial was designed to quantify. Post-approval research has evaluated eptifibatide with thrombolytics and in high-risk PCI subgroups. Its short half-life and reversibility are the practical reasons it is chosen when rapid offset matters.[1][2][3][4][5][6]
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, pharmacies, and label-appropriate access programs; compounded access depends on current FDA shortage status and compounding rules.
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. Inhibition of platelet aggregation drops below 50 percent within about 4 hours of stopping the infusion, making eptifibatide one of the shorter-acting agents in this drug class.
The primary risk is bleeding, including major and intracranial hemorrhage. Thrombocytopenia occurred in 1.2 percent of eptifibatide patients versus 0.6 percent on placebo in ESPRIT, and can be severe. Hypotension and injection site reactions may also occur. In patients with creatinine clearance below 50 mL/min the labeled infusion rate is reduced to 1 mcg/kg/min. US labeling contraindicates eptifibatide in: bleeding diathesis or bleeding within the previous 30 days; severe uncontrolled hypertension; major surgery within the preceding 6 weeks; stroke within 30 days or any history of hemorrhagic stroke; coadministration of another parenteral GP IIb/IIIa inhibitor; dependency on renal dialysis; and known hypersensitivity to the drug or its components.
The PURSUIT trial enrolling 10,948 patients with non-ST-elevation ACS demonstrated a significant reduction in the composite endpoint of death or myocardial infarction at 30 days. ESPRIT, in 2,064 patients undergoing planned coronary stent implantation, was terminated early for efficacy: the 48-hour composite endpoint fell from 10.5 to 6.6 percent and the 30-day composite from 10.5 to 6.8 percent. Major bleeding was more frequent on eptifibatide (1.3 versus 0.4 percent). These trials established eptifibatide as a standard component of high-risk ACS and PCI management, with bleeding risk as the counterweight.
Research references
- Inhibition of Platelet Glycoprotein IIb/IIIa with Eptifibatide in Patients with Acute Coronary Syndromes (PURSUIT Trial)PubMed
- Novel dosing regimen of eptifibatide in planned coronary stent implantation (ESPRIT): a randomised, placebo-controlled trialPubMed
- 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