Lepirudin is a protein-based direct thrombin inhibitor used as an anticoagulant in patients with heparin-induced thrombocytopenia. Lepirudin is a recombinant hirudin formed by 65 amino acids that acts as a highly specific and direct thrombin inhibitor.
- Mechanism
- Curator reviewed · 6 references
Lepirudin is a direct thrombin inhibitor used as an anticoagulant in patients for whom heparin is contraindicated. Thrombin is a serine protease that participates in the blood-clotting cascade, and it is formed by the cleavage of pro-thrombin. Active thrombin cleaves fibrinogen and generates fibrin monomers that polymerize to form fibrin clots.
Lepirudin binds to the catalytic and substrate-binding sites of thrombin, forming a stable, irreversible and non-covalent complex. This blocks the protease activity of thrombin and inhibits the coagulation process. Each molecule of lepirudin binds to a single molecule of thrombin, and unlike heparin, it is able to inhibit thrombin in both its clot-bound or free states.
- Primary indication
- Lepirudin is indicated for anticoagulation in adult patients with acute coronary syndromes (ACS) such as unstable angina and acute myocardial infarction without ST elevation.Curator reviewed · 2 structured indications
- Formula / weight
- C287H440N80O111S6 · 6979.0 Da
- First approval
- Canada, 2007 · United States, 1998
- Also known as
- [Leu1, Thr2]-63-desulfohirudin · Desulfatohirudin · Hirudin variant-1 · Lepirudin recombinant · R-hirudin
Resolves to
What you can answer from here — as of September 12, 2026
Which drugs share a target with Lepirudin, and which of those have an active Phase 3 trial?
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