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(Arteriosclerosis, Thrombosis, and Vascular Biology. 2007;27:1238.)
© 2007 American Heart Association, Inc.

Brief Reviews

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.

Correspondence to Alexander G.G. Turpie, Department of Medicine, Hamilton Health Sciences Corporation, General Division, 237 Barton Street East, Hamilton, Ontario L8L 2X2, Canada. E-mail turpiea{at}mcmaster.ca

Series Editor: Jeffrey I. Weitz
Emerging Anticoagulant Drugs
ATVB In Focus

Previous Brief Review in this Series:

•Howard EL, Becker KCD, Rusconi CP, Becker RC. Factor IXa inhibitors as novel anticoagulants. 2007;27:722–727.

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.

Anticoagulants are recommended in a wide variety of indications. There is a need for novel oral anticoagulants that do not require frequent monitoring or dose adjustment. Factor Xa is an attractive target for novel anticoagulants.

Key Words: anticoagulant • atrial fibrillation • Factor Xa inhibitor • stroke • venous thromboembolism

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