Direct thrombin inhibitors.

Karen L Kaplan

doi:10.1517/14656566.4.5.653

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PubMed · 12739991

Direct thrombin inhibitors.

Karen L Kaplan

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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.

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Antithrombins Arginine Coronary Disease Half-Life Hirudins Humans Metabolic Clearance Rate Peptide Fragments Pipecolic Acids Recombinant Proteins Sulfonamides Thrombin Venous Thrombosis Journal Article Review

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Karen L Kaplan. 2003. Direct thrombin inhibitors.. https://doi.org/10.1517/14656566.4.5.653

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