Oral, Direct Thrombin and Factor Xa Inhibitors: The Replacement for Warfarin, Leeches, and Pig Intestines?
Article first published online: 29 APR 2011
Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Angewandte Chemie International Edition
Volume 50, Issue 20, pages 4574–4590, May 9, 2011
How to Cite
Straub, A., Roehrig, S. and Hillisch, A. (2011), Oral, Direct Thrombin and Factor Xa Inhibitors: The Replacement for Warfarin, Leeches, and Pig Intestines?. Angew. Chem. Int. Ed., 50: 4574–4590. doi: 10.1002/anie.201004575
- Issue published online: 4 MAY 2011
- Article first published online: 29 APR 2011
- Manuscript Received: 26 JUL 2010
- antithrombotic agents;
- drug design;
- structure–activity relationships
To prevent thromboses after surgery, patients have until now had to inject themselves daily with heparin. For stroke prophylaxis in atrial fibrillation, patients take vitamin K antagonists of the coumarin type, which have a narrow therapeutic window and whose dosage must be regularly monitored. In order to improve the standard of therapy in thromboembolic diseases such as deep-vein thrombosis, pulmonary embolism, and stroke in atrial fibrillation, intensive research has been carried out over the last decade in the search for new, orally active thrombin and factor Xa inhibitors. A number of these compounds are already on the market or are in advanced clinical development; they could revolutionize the anticoagulant market.