Apixaban, Dabigatran, Rivaroxaban
A number of small-molecule, orally administered direct Factor Xa inhibitors are currently in development, including rivaroxaban, apixaban, betrixaban, and a group of as yet unnamed clinical entities (YM150, DU-176b).
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Thrombin has a central role in the coagulation cascade. Produced in small amounts in the initiation phase and large amounts in the propagation phase, thrombin is essential for the amplification of coagulation and fibrin formation.23, 108
A second direct oral thrombin inhibitor, dabigatran etexilate, was approved for marketing in the European Union in March 2008 for primary prevention of venous thromboembolic events in adult patients who have undergone elective total hip replacement surgery or total knee replacement surgery.
Dabigatran etexilate is a small-molecule prodrug that does not exhibit any pharmacological activity. After oral administration, dabigatran etexilate is rapidly absorbed and converted to its active principal dabigatran by esterase-catalysed hydrolysis in plasma and in the liver. Further studies in stroke prevention in atrial fibrillation (AF) and other thromboembolic conditions are under way.100
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Direct Factor Xa inhibitors in development have many properties of an ideal anticoagulant, including oral administration, rapid onset of action, and predictable pharmacokinetics and pharmacodynamics.25, 100
A number of small-molecule, orally administered direct Factor Xa inhibitors are currently in development. These include rivaroxaban, apixaban, betrixaban, and a group of as yet unnamed clinical entities (YM150, DU-176b). At present, the clinical trial program for rivaroxaban is the most advanced.25 Rivaroxaban has been approved in September 2008 in the European Union for the prevention of venous thromboembolism (VTE) in adult patients undergoing elective hip or knee replacement surgery.378
Learn more about rivaroxaban.
See also: Coagulation
See also: Symptoms of Thrombosis