on March 22, 2007
Published online before print March 22, 2007, doi: 10.1161/ATVBAHA.107.139402
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Submitted on January 3, 2007
Accepted on March 9, 2007
Oral Direct Factor Xa Inhibitors in Development for the Prevention and Treatment of Thromboembolic Diseases
Alexander G.G. Turpie *
From HHS-General Hospital, Hamilton, Canada.
* To whom correspondence should be addressed. E-mail: turpiea{at}mcmaster.ca.
Abstract--Anticoagulants are recommended for the prevention and treatment of a wide variety of thromboembolic events. Although existing anticoagulants are effective, their use is limited by parenteral administration or the requirement for frequent monitoring and subsequent dose adjustment. Therefore, there is an urgent need for novel oral agents with a predictable anticoagulant action. Because of its key position in the coagulation cascade and its limited roles outside of coagulation, Factor Xa has emerged as an attractive target for novel anticoagulants. As a result, the past decade has witnessed an explosion of research into small-molecule, oral, direct Factor Xa inhibitors, and several are now in clinical development. Rivaroxaban, LY517717, YM150, apixaban, PRT054021, and DU-176b, among others, have shown considerable promise; rivaroxaban is currently furthest ahead in its developmental program, having entered phase III in 3 indications. It is hoped that before long, these anticoagulants will allow us to enter an era of convenient oral anticoagulation without the need for regular monitoring or dose adjustment.
Key words: anticoagulant • atrial fibrillation • Factor Xa inhibitor • stroke • venous thromboembolism
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