Efegatran

Direct Thrombin Inhibitor (peptidomimetic / Small Peptide)Rx: ResearchCompound: Investigational

Also known as: efegatran sulfate, LY294468

Educational Only — Not medical advice. Consult a qualified clinician before using any peptide.

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

Intravenous

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.

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