Pharmacology and Clinical Potential of Direct Thrombin Inhibitors

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 t...

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Bibliographic Details
Published inCurrent pharmaceutical design Vol. 11; no. 30; pp. 3877 - 3884
Main Authors Linkins, Lori-Ann, Weitz, Jeffrey I
Format Journal Article
LanguageEnglish
Published United Arab Emirates Bentham Science Publishers Ltd 01.01.2005
Subjects
Animals
Anticoagulants - chemistry
Anticoagulants - pharmacology
Anticoagulants - therapeutic use
Blood Coagulation Disorders - blood
Blood Coagulation Disorders - drug therapy
Humans
Thrombin - antagonists & inhibitors
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Summary: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.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-3
content type line 23
ObjectType-Review-1
ISSN:1381-6128
1873-4286
DOI:10.2174/138161205774580598