NDLI: Direct thrombin inhibitors – a survey of recent developments

Content Provider	Springer Nature Link
Author	Schwienhorst, A.
Copyright Year	2006
Abstract	Thrombin is a plasma serine protease that plays a key role in coagulation and hemostasis but also in thromboembolic diseases. Direct thrombin inhibitors could, therefore, be beneficial for future anticoagulant therapy in the prophylaxis of venous and arterial thrombosis as well as myocardial infarction. However, development of direct thrombin inhibitors has brought researchers more heartache than success. The most recent setback came this year when AstraZeneca withdrew Ximelagatran, the first orally bioavailable direct thrombin inhibitor that had received regulatory approval (France, 2003), after reports of serious hepatoxicity in a fraction of patients. This review describes the status of direct thrombin inhibitors, focusing on drug candidates that are at present in clinical trials. In addition, some more recent research strategies in the design of novel direct thrombin inhibitors are discussed, which may very well contribute to future developments of potent anticoagulants.
Starting Page	2773
Ending Page	2791
Page Count	19
File Format	PDF
ISSN	1420682X
Journal	Cellular and Molecular Life Sciences
Volume Number	63
Issue Number	23
e-ISSN	14209071
Language	English
Publisher	Birkhäuser-Verlag
Publisher Date	2006-11-13
Publisher Place	Basel
Access Restriction	Subscribed
Subject Keyword	Direct thrombin inhibitor hirudin anticoagulant therapy thromboembolic disease drug candidate oral bioavailability neutral P1 moiety Biomedicine general Life Sciences Biochemistry Cell Biology
Content Type	Text
Resource Type	Article
Subject	Cell Biology Molecular Biology Molecular Medicine Pharmacology Cellular and Molecular Neuroscience

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