Direct thrombin inhibitors

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.

Review of direct thrombin inhibitors approved for clinical use — lepirudin, desirudin, bivalirudin, and argatroban — plus melagatran/ximelagatran in advanced clinical testing, covering their chemical structure, thrombin-inhibition kinetics, pharmacokinetics, and clinical use.

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