American Society of Hirudotherapy

Direct thrombin inhibitors

Review published in Expert Opin Pharmacother (2003)

Last Updated: June 18, 2026Reviewed by: ASH Editorial Board
Research article — evidence reviewArticle reference
Evidence: Narrative reviewDrug DevelopmentSalivary PharmacologyKaplan KL · Expert opinion on pharmacotherapy, 2003

Abstract

This review deals with a newly-developed category of antithrombotic drugs - the direct thrombin inhibitors. These agents interact with thrombin and block its catalytic activity on fibrinogen, platelets and other substrates. Heparin and its derivatives (low molecular weight heparins and the active pentasaccharide) inhibit thrombin and/or other coagulation serine proteases indirectly via antithrombin, and the warfarin-type drugs interfere with the synthesis of the precursors of the coagulation serine proteases. The direct thrombin inhibitors approved for clinical use at present (lepirudin, desirudin, bivalirudin, argatroban) and another in the advanced clinical testing stage (melagatran/ximelagatran), are the subject of this review. The chemical structure; kinetics of thrombin inhibition; pharmacokinetics and clinical use of each of these is discussed.

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

Publication typeJournal ArticleReview
Indexed MeSH termsAntithrombinsArginineCoronary DiseaseHalf-LifeHirudinsHumansMetabolic Clearance RatePeptide FragmentsPipecolic AcidsRecombinant ProteinsSulfonamidesThrombin

Summary

Foundational pharmacology review of direct thrombin inhibitors approved for clinical use: lepirudin, desirudin, bivalirudin, argatroban, plus melagatran/ximelagatran in development. Chemistry, kinetics, pharmacokinetics, and clinical use covered.

Why This Matters for Hirudotherapy

This review covers direct thrombin inhibitors — lepirudin, desirudin, bivalirudin, argatroban, and melagatran/ximelagatran — discussing their chemical structure, kinetics of thrombin inhibition, pharmacokinetics, and clinical use. The abstract describes these as antithrombotic agents that interact directly with thrombin and block its catalytic activity, contrasting them with indirect inhibitors (heparin derivatives) and warfarin-type drugs. For ASH's domain, the abstract itself does not mention leeches, hirudin, or any leech-derived connection, so a direct link to hirudotherapy or leech biology cannot be established from this text alone. Caveat: this is a pharmacology review with no original experimental data; it addresses pharmaceutical antithrombotic agents rather than leech therapy, and any connection to leech biology would require external knowledge not present in the abstract.

Citation

Direct thrombin inhibitors.

Kaplan KL · Expert opinion on pharmacotherapy, 2003

DOI

Added to ASH library: May 27, 2026 · Site last updated: June 18, 2026

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