American Society of Hirudotherapy

Clinical pharmacology of recombinant hirudin

Research article published in Haemostasis (1991)

Last Updated: June 18, 2026Reviewed by: ASH Editorial Board
Research article — evidence reviewArticle reference
Evidence: Research reportDrug DevelopmentMarkwardt F, Nowak G, Stürzebecher J · Haemostasis, 1991

Abstract

Pharmacological profiling of recombinant hirudin (r-hirudin) has shown that this selective tight-binding thrombin inhibitor is a potent, well-tolerated anticoagulant. Clinical pharmacological studies were performed in human volunteers after single and repeated doses of 0.1-0.5 mg/kg. Generally, administration of r-hirudin was tolerated without side effects. Thrombin time and partial thromboplastin time were prolonged dependent on the r-hirudin level in plasma. Platelet counts, fibrinogen level and fibrinolytic system remained unchanged. Bleeding time was not prolonged. On intravenous injection, r-hirudin was rapidly distributed into the extracellular space and eliminated, with a dose-dependent half-life of 1-2 h (first-order kinetics). After subcutaneous administration, the rH level in blood reached plateau values within 60-120 min. The high recovery of unchanged r-hirudin in the urine identified renal excretion as the predominant route of r-hirudin clearance.

Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.

Publication typeJournal Article
Indexed MeSH termsFibrinogenFibrinolysisHalf-LifeHirudinsHumansInjections, IntravenousInjections, SubcutaneousPartial Thromboplastin TimePlatelet CountRecombinant Fusion ProteinsThrombinThrombin Time

Summary

Pharmacological profiling of recombinant hirudin (r-hirudin) has shown that this selective tight-binding thrombin inhibitor is a potent, well-tolerated anticoagulant.

Why This Matters for Hirudotherapy

This article reports clinical pharmacological studies of recombinant hirudin (r-hirudin) in human volunteers at single and repeated doses of 0.1–0.5 mg/kg, finding it to be a potent, well-tolerated selective thrombin inhibitor. Key findings include dose-dependent prolongation of thrombin time and partial thromboplastin time, no changes in platelet counts or fibrinogen levels, no prolongation of bleeding time, a half-life of 1–2 hours via intravenous injection, and predominant renal excretion. For ASH's domain, this study provides foundational pharmacokinetic and pharmacodynamic data for the signature leech-derived anticoagulant used in hirudotherapy and its recombinant formulations. Caveat: these studies were conducted in healthy volunteers rather than patients, and the abstract does not address therapeutic outcomes or clinical efficacy in disease states.

Citation

Clinical pharmacology of recombinant hirudin.

Markwardt F, Nowak G, Stürzebecher J · Haemostasis, 1991

DOI

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