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Current Pharmaceutical Design

Editor-in-Chief

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

Recent Advances in Serine Protease Inhibitors as Anticoagulant Agents

Author(s): Andrej Prezelj, Petra Stefanic Anderluh, Luka Peternel and Uros Urleb

Volume 13, Issue 3, 2007

Page: [287 - 312] Pages: 26

DOI: 10.2174/138161207779313605

Price: $65

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Abstract

The drawbacks and limitations of existing anticoagulant therapy which may result in serious adverse effects and a high mortality rate, have given rise to many anticoagulant development programmes in the last decade, focusing mainly at development of thrombin and FXa low-molecular weight inhibitors. A detailed understanding of blood coagulation pathways, functioning of the serine proteases thrombin, FXa, FVIIa and FIXa and elucidation of their crystal structures resulted in many potent compounds, among which some have entered the clinical phase or have been approved for use in clinical practice. Recently, the focus of anticoagulant research turned to inhibition of the TF:FVIIa complex, with some promising clinical candidates on the horizon. This article provides an overview of the current development status of serine protease inhibitors as anticoagulants, including new trends such as dual coagulation factor inhibitors.

Keywords: Anticoagulants, thrombin, FXa and TF, FVIIa inhibitors


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