Eptifibatide
Also known as: ABT-527, Integrelin, Integrilin, L-734217
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Summary
Eptifibatide is a cyclic heptapeptide that acts as a Glycoprotein IIb/IIIa (integrin αIIbβ3) inhibitor. It is approved for intravenous use and is marketed for cardiovascular indications where rapid platelet inhibition is required. The drug blocks the final common pathway of platelet aggregation, thereby reducing thrombus formation.
Mechanism of Action
Eptifibatide binds with high affinity to the GP IIb/IIIa receptor (integrin αIIbβ3) on activated platelets. This prevents fibrinogen and von Willebrand factor from cross‑linking adjacent platelets, halting the final step of platelet aggregation. By targeting this integrin, eptifibatide interrupts the cellular adhesion cascade that underlies arterial thrombus formation.
What the Research Shows
A phase‑3 stroke trial found that adding eptifibatide to standard intravenous thrombolysis did not improve functional outcomes and was associated with higher 90‑day mortality, while symptomatic intracranial hemorrhage rates were similar to placebo. A review of drug‑induced immune thrombocytopenia lists eptifibatide among agents that can trigger severe platelet‑destruction via drug‑dependent antibodies. Integrin‑targeting reviews note eptifibatide as one of the few approved agents that block αIIbβ3. Reviews of cerebral venous thrombosis and peri‑operative bridging after coronary stenting report little or no supportive evidence for eptifibatide in those settings, highlighting a paucity of randomized data.
Reported Benefits
Eptifibatide’s approved status reflects demonstrated efficacy in rapidly inhibiting platelet aggregation, a therapeutic advantage in acute coronary syndromes where fast‑acting antiplatelet effect is needed. Its specific targeting of the GP IIb/IIIa receptor provides a direct blockade of the final common pathway of clot formation.
Limitations of the Evidence
Clinical data do not support benefit of eptifibatide as an adjunct to thrombolysis in acute ischemic stroke and suggest a possible increase in mortality. Evidence for its use in cerebral venous thrombosis or as a peri‑operative bridging agent after stent placement is limited and largely observational. Additionally, the drug can provoke immune‑mediated thrombocytopenia, a serious but rare adverse effect.
Safety Considerations
Bleeding is an expected risk due to potent platelet inhibition; rates of symptomatic intracranial hemorrhage were comparable to placebo in the stroke trial. Mortality was higher in the eptifibatide arm of that trial. Case reports and reviews identify drug‑induced immune thrombocytopenia as a potential severe complication, requiring vigilance for abrupt platelet count drops and bleeding. Routine monitoring of platelet function and counts is advised during therapy.
How It Is Administered
Eptifibatide is administered exclusively by intravenous infusion. It is supplied as a sterile solution for bolus or continuous infusion, typically given in a hospital setting under cardiac or neurologic monitoring.
Routes of Administration
Goals & Uses
- Adjunct to percutaneous coronary interventionInterventional CardiologyHigh
- Prevention of abrupt vessel closure post-PCICardiovascular / Thrombosis PreventionHigh
- Prevention of acute coronary thrombosisCardiovascularHigh
- Percutaneous Coronary Intervention (PCI) adjunctCardiovascular / AntiplateletHigh
- Acute Coronary Syndrome (ACS) managementCardiovascular / AntiplateletHigh
Contraindications
- Thrombocytopenia (<100,000/µL)HematologicModerate
- Thrombocytopenia (platelet count <100,000/mm³)HematologicalHigh
- Major surgery or trauma within 6 weeksSurgicalHigh
- Recent intracranial hemorrhage (≤30 days)NeurologicHigh
- Severe renal impairment (creatinine ≥4 mg/dL or dialysis dependency)RenalHigh
- Active pathological bleedingBleeding RiskHigh
- Known hypersensitivity to eptifibatide or any component of the formulationAllergyModerate
- History of stroke within 30 days or hemorrhagic stroke at any timeNeurologicalHigh
- Active internal bleeding or bleeding diathesis within 30 daysBleeding RiskHigh
- Severe uncontrolled hypertension (SBP >180 mmHg or DBP >110 mmHg)CardiovascularModerate
- Severe hypertension (uncontrolled, systolic >200 mmHg or diastolic >110 mmHg)CardiovascularHigh
Adverse Effects
- ThrombocytopeniaHematologicUncommonLow platelet count
- HeadacheNeurologicCommonPain in the head or upper neck
- HypotensionCardiovascularUncommonLow blood pressure
- NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
- Allergic/hypersensitivity reactionsImmunologicalRare
- BleedingHematologicCommonAbnormal bleeding or hemorrhage
- Bleeding (minor and major)HemorrhagicCommon
Drug Interactions
- HeparinHigh
- Heparin / Low-molecular-weight heparinsModerate
- Thienopyridines (clopidogrel, ticagrelor)Moderate
- WarfarinHigh
- Aspirin / NSAIDsModerate
- Other GPIIb/IIIa inhibitors (abciximab, tirofiban)High
- Other GP IIb/IIIa inhibitors (e.g., abciximab, tirofiban)High
- Warfarin / oral anticoagulantsHigh
- Clopidogrel or other ADP‑P2Y12 inhibitorsModerate
Population Constraints
- PregnancyReproductive SafetyRelative
- Renal impairment (moderate: CrCl <50 mL/min)RenalRelative
- Low body weight patients (<60 kg)AnthropometricRelative
- Pediatric patientsAgeRelative
- Elderly patients (≥75 years)AgeRelative
- Elderly (≥75 years)AgeRelative
Regulatory Status
- European UnionApprovedApproved: Acute coronary syndrome, PCIApproved in EU member states; same brand name
- United StatesApprovedApproved: Unstable angina, NSTEMI, Adjunct to PCIApproved under prescription; marketed as Integrilin
- United KingdomApprovedApproved: Acute coronary syndrome, PCIApproved by MHRA; prescription only
FDA approved in 1998 (brand Integrilin); also approved in the EU and UK for acute coronary syndrome and PCI.
Evidence & Sources
- Journal ArticleModerateAdeoye O, et al.2024-01-01T00:00:00.000000Z
- Journal ArticleModerateVayne C, et al.2020-01-01T00:00:00.000000Z
- Journal ArticleModeratePang X, et al.2023-01-01T00:00:00.000000Z
- Journal ArticleModeratePatel H, et al.2024-01-01T00:00:00.000000Z
- Journal ArticleHighSullivan AE, et al.2021-01-01T00:00:00.000000Z
Frequently Asked Questions
What clinical condition is eptifibatide approved to treat?
It is approved for intravenous use to provide rapid platelet inhibition in acute cardiovascular settings, such as during percutaneous coronary intervention for acute coronary syndromes.
How does eptifibatide prevent clot formation?
The peptide binds to the GP IIb/IIIa (αIIbβ3) integrin on activated platelets, blocking fibrinogen binding and thereby stopping platelets from linking together to form a thrombus.
Is eptifibatide beneficial for acute ischemic stroke?
A recent randomized trial showed that adding eptifibatide to standard thrombolysis did not improve disability outcomes and was linked to higher mortality, indicating no proven benefit in this setting.
What are the main safety concerns with eptifibatide?
The principal risks are bleeding, including intracranial hemorrhage, and rare immune‑mediated thrombocytopenia that can cause severe platelet loss and bleeding. Mortality was higher in the stroke trial.
Can eptifibatide be used as a bridging antiplatelet after coronary stent placement?
While it is listed as a possible intravenous bridging agent, current reviews note a lack of randomized evidence to define its safety or efficacy for peri‑operative bridging after stenting.
What is Eptifibatide?
Eptifibatide is a cyclic heptapeptide that acts as a Glycoprotein IIb/IIIa (integrin αIIbβ3) inhibitor. It is approved for intravenous use and is marketed for cardiovascular indications where rapid platelet inhibition is required. The drug blocks the final common pathway of platelet aggregation, thereby reducing thrombus formation.
What is Eptifibatide used for?
Eptifibatide is educationally associated with: Adjunct to percutaneous coronary intervention, Prevention of abrupt vessel closure post-PCI, Prevention of acute coronary thrombosis, Percutaneous Coronary Intervention (PCI) adjunct, Acute Coronary Syndrome (ACS) management. Educational only — not medical advice.
How is Eptifibatide administered?
Recorded routes of administration: Intravenous.
What are the potential side effects of Eptifibatide?
Reported adverse effects include: Thrombocytopenia, Headache, Hypotension, Nausea, Allergic/hypersensitivity reactions, Bleeding, Bleeding (minor and major). This list is not exhaustive — consult a qualified clinician.
Who should avoid Eptifibatide?
Recorded contraindications: Thrombocytopenia (<100,000/µL), Thrombocytopenia (platelet count <100,000/mm³), Major surgery or trauma within 6 weeks, Recent intracranial hemorrhage (≤30 days), Severe renal impairment (creatinine ≥4 mg/dL or dialysis dependency), Active pathological bleeding, Known hypersensitivity to eptifibatide or any component of the formulation, History of stroke within 30 days or hemorrhagic stroke at any time, Active internal bleeding or bleeding diathesis within 30 days, Severe uncontrolled hypertension (SBP >180 mmHg or DBP >110 mmHg), Severe hypertension (uncontrolled, systolic >200 mmHg or diastolic >110 mmHg). Consult a qualified clinician before use.