Apixaban, Dabigatran, Rivaroxaban

Apixaban

A number of small-molecule, orally administered direct Factor Xa inhibitors are currently in development, including apixaban and a group of as yet unnamed clinical entities (LY517717, YM150, PRT054021, and DU-176b).
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Dabigatran

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.15, 88
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.89
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Rivaroxaban

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.17, 89
A number of small-molecule, orally administered direct Factor Xa inhibitors are currently in development. At present, the clinical trial program for rivaroxaban is the most advanced.17
Learn more about rivaroxaban.
Find out more about apixaban, dabigatran, and rivaroxaban.
See also: Coagulation
See also: Symptoms of Thrombosis
  • 15 - Hoffman M, Monroe DM. Coagulation 2006: a modern view of hemostasis. Hematol Oncol Clin North Am. 2007;21(1):1-11.
  • 88 - Spyropoulos AC. Investigational treatments of venous thromboembolism. Expert Opin Investig Drugs. 2007;16(4):431-440.
  • 89 - Haas S. New oral Xa and IIa inhibitors: updates on clinical trial results. J Thromb Thrombolysis. 2008;25(1):52-60.
  • 17 - 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.