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Current Pharmaceutical Design

Editor-in-Chief

ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

Pharmacology and Clinical Potential of Direct Thrombin Inhibitors

Author(s): L- A. Linkins and J. I. Weitz

Volume 11, Issue 30, 2005

Page: [3877 - 3884] Pages: 8

DOI: 10.2174/138161205774580598

Price: $65

Abstract

Direct thrombin inhibitors represent a new class of anticoagulants that bind directly to thrombin and block the enzymes interactions with its substrates. These agents have been developed, at least in part, to overcome the limitations of heparin and vitamin K antagonists. This paper (a) reviews why thrombin is an ideal target for new anticoagulants, (b) describes the pharmacological profiles of the various direct thrombin inhibitors, (c) outlines the potential mechanistic advantages of parenteral direct thrombin inhibitors over heparin, (d) defines the potential benefits of ximelagatran, the first orally active direct thrombin inhibitor, over vitamin K antagonists, and (e) provides clinical perspective on the strengths and weaknesses of the various parenteral and oral direct thrombin inhibitors.

Keywords: Anticoagulants, thromboxane, heparin-induced thrombocytopenia (HIT), Hirudin, Ximelagatran, Vitamin K antagonists


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