Efegatran
Also known as: efegatran sulfate, LY294468
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Summary
Efegatran (LY294468) is a synthetic tripeptide-based direct thrombin inhibitor developed by Eli Lilly. It was investigated in the 1990s for anticoagulation in acute coronary syndromes and percutaneous coronary interventions but did not advance to regulatory approval due to insufficient clinical benefit over heparin in pivotal trials.
Mechanism of Action
Selectively and reversibly inhibits thrombin (factor IIa) by binding to its active site, thereby blocking thrombin-mediated conversion of fibrinogen to fibrin, thrombin-induced platelet aggregation, and amplification of the coagulation cascade.
Routes of Administration
Goals & Uses
- Anticoagulation during percutaneous coronary intervention (PCI)AnticoagulationModerate
- Anticoagulation in acute coronary syndromesCardiovascular / ThrombosisModerate
- Prevention of thrombus formationHematology / AnticoagulationModerate
Contraindications
- Recent intracranial surgery or hemorrhagic strokeNeurologicHigh
- Active major bleedingHemorrhagic RiskHigh
- Known hypersensitivity to efegatran or arginine-based peptidesImmunologicHigh
Adverse Effects
- Injection site reactionsLocalUncommon
- ThrombocytopeniaHematologicRareLow platelet count
- Bleeding / hemorrhageHematologicCommon
Drug Interactions
- Antiplatelet agents (aspirin, clopidogrel)Moderate
- Other anticoagulants (heparin, warfarin, LMWH)High
- Thrombolytics (alteplase, streptokinase)High
Population Constraints
- PregnancyReproductive SafetyRelative
- Hepatic impairmentOrgan FunctionRelative
- Renal impairmentOrgan ImpairmentRelative
- Elderly patientsAgeRelative
Regulatory Status
- European UnionUnapprovedNo marketing authorization granted. Not approved by EMA or predecessor agencies.
- United StatesUnapprovedPhase II/III clinical development conducted by Eli Lilly in the 1990s; never approved by FDA. Development discontinued.
- United KingdomUnapprovedNo regulatory approval. Not licensed in the UK.
Never received regulatory approval in the US, EU, or UK. Clinical development was discontinued following Phase II/III trial results. No current active IND or approved indication known.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Efegatran?
Efegatran (LY294468) is a synthetic tripeptide-based direct thrombin inhibitor developed by Eli Lilly. It was investigated in the 1990s for anticoagulation in acute coronary syndromes and percutaneous coronary interventions but did not advance to regulatory approval due to insufficient clinical benefit over heparin in pivotal trials.
What is Efegatran used for?
Efegatran is educationally associated with: Anticoagulation during percutaneous coronary intervention (PCI), Anticoagulation in acute coronary syndromes, Prevention of thrombus formation. Educational only — not medical advice.
How is Efegatran administered?
Recorded routes of administration: Intravenous.
What are the potential side effects of Efegatran?
Reported adverse effects include: Injection site reactions, Thrombocytopenia, Bleeding / hemorrhage. This list is not exhaustive — consult a qualified clinician.
Who should avoid Efegatran?
Recorded contraindications: Recent intracranial surgery or hemorrhagic stroke, Active major bleeding, Known hypersensitivity to efegatran or arginine-based peptides. Consult a qualified clinician before use.