Journal
THROMBOSIS RESEARCH
Volume 127, Issue 6, Pages 497-504Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.thromres.2010.09.008
Keywords
Anticoagulants; Direct Factor Xa inhibitors; Direct thrombin inhibitors; Rivaroxaban
Categories
Funding
- Bayer Schering Pharma AG
- Johnson & Johnson Pharmaceutical Research & Development, L.L.C.
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Although results of some phase III clinical trials of new oral anticoagulants are now known, it is important to understand the mechanisms of their actions. These new agents exert their anticoagulant effect via direct inhibition of a single Factor within the coagulation cascade (such as Factor Xa or thrombin). Rivaroxaban - the first oral, direct Factor Xa inhibitor - is a small-molecule oxazolidinone derivative that binds directly and reversibly to Factor Xa via the S1 and S4 pockets. Rivaroxaban competitively inhibits Factor Xa and is more than 10,000-fold more selective for Factor Xa than other related serine proteases, and it does not require cofactors (such as antithrombin) to exert its anticoagulant effect. Unlike indirect Factor Xa inhibitors, rivaroxaban inhibits both free and clot-bound Factor Xa, as well as prothrombinase activity, thereby prolonging clotting times. Dabigatran etexilate is a direct thrombin inhibitor that inhibits both free and fibrin-bound thrombin. Although the mechanism of action differs between the direct Factor Xa and direct thrombin inhibitors, phase III studies of these new agents confirmed that both Factor Xa and thrombin are viable anticoagulation targets. (C) 2010 Elsevier Ltd. All rights reserved.
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