DCSIMG

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Last updated on 9th March 2010

Xarelto®: Directly Targeting Factor Xa Leads to Improved Efficacy

Xarelto® is the first oral, direct inhibitor of Factor Xa available for clinical use. It is leading a new generation of Factor Xa-inhibiting drugs designed to meet a pressing clinical need for improved antithrombotic therapy. It is approved in Europe for the prevention of venous thromboembolism (VTE) in adult patients undergoing elective hip or knee replacement surgery.1, 25, 26

The coagulation cascade

Xarelto® precisely targets at the pivotal point in the coagulation cascade, which is a chain of biochemical reactions leading to the formation of blood clots.1, 8, 26

The central role of
Factor Xa

Activated Factor X (Factor Xa) is the primary site of amplification, as 1 molecule catalyses the formation of approximately 1,000 thrombin molecules.25, 26, 27

Xarelto® — excellent efficacy and convenience with reassuring safety

The advantages of Xarelto® include oral administration without the need for ongoing routine coagulation monitoring. Other therapies, such as unfractionated heparins (UFHs), low-molecular-weight heparins (LMWHs), and fondaparinux, can only be administered by injection. On the other hand, oral vitamin K antagonists (VKAs) have a narrow therapeutic window and significant interactions with food and other drugs, leading to the need for strict monitoring.7, 8, 27, 30
  • 1 - Xarelto® (rivaroxaban) Summary of Product Characteristics as approved by the European Commission.
  • 25 - Mann KG, Brummel K, Butenas S. What is all that thrombin for? J Thromb Haemost. 2003;1(7):1504-1514.
  • 26 - Turpie AG. Oral, direct factor Xa inhibitors in development for the prevention and treatment of thromboembolic diseases. Arterioscler Thromb Vasc Biol. 2007;27(6):1238-1247.
  • 8 - Kubitza D, Haas S. Novel factor Xa inhibitors for prevention and treatment of thromboembolic diseases. Expert Opin Investig Drugs. 2006;15(8):843-855.
  • 27 - Haas S. New oral Xa and IIa inhibitors: updates on clinical trial results. J Thromb Thrombolysis. 2008;25(1):52-60.
  • 7 - Cohen AT, Tapson VF, Bergmann JF, et al; ENDORSE Investigators. Venous thromboembolism risk and prophylaxis in the acute hospital care setting (ENDORSE study): a multinational cross-sectional study. Lancet. 2008;371(9610):387-394.
  • 30 - Ansell J, Hirsh J, Hylek E, Jacobson A, Crowther M, Palareti G. Pharmacology and management of the vitamin K antagonists: American College of Chest Physicians Evidence-Based Clinical Practice Guidelines (8th Edition). Chest. 2008;133(6 suppl):160S-198S.
Factor Xa
Pivotal component of blood clotting cascade. Stimulates the production of thrombin, the enzyme in the coagulation cascade that promotes the formation of blood clots.
Venous thromboembolism
A disease process beginning with a blood clot occurring within the venous system, including deep vein thrombosis and pulmonary embolism.
Coagulation cascade
A chain of biochemical reactions that result in clot formation. Anticoagulants work by blocking or regulating a stage, or stages, of the coagulation cascade.
Thrombin
Enzyme in the blood clotting cascade that promotes the formation of blood clots.