Oral, direct Factor Xa inhibitors in development for the prevention and treatment of thromboembolic diseases

被引:183
作者
Turpie, Alexander G. G.
机构
[1] Hamilton Hlth Sci Corp, Dept Med, Gen Div, Hamilton, ON L8L 2X2, Canada
[2] HHS Gen Hosp, Hamilton, ON, Canada
关键词
anticoagulant; atrial fibrillation; Factor Xa inhibitor; stroke; venous thromboembolism;
D O I
10.1161/ATVBAHA.107.139402
中图分类号
R5 [内科学];
学科分类号
1002 ; 100201 ;
摘要
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. Rivafoxaban, 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.
引用
收藏
页码:1238 / 1247
页数:10
相关论文
共 78 条
[1]  
Abe K, 2006, BLOOD, V108, p270A
[2]  
Agnelli G, 2006, EUR HEART J, V27, P761
[3]   Current issues in anticoagulation [J].
Agnelli, G .
PATHOPHYSIOLOGY OF HAEMOSTASIS AND THROMBOSIS, 2005, 34 :2-9
[4]  
AGNELLI G, 2005, AM SOC HEM 47 ANN M, V106
[5]   Antithrombotic and thrombolytic therapy for ischemic stroke [J].
Albers, GW ;
Amarenco, P ;
Easton, JD ;
Sacco, RL ;
Teal, P .
CHEST, 2004, 126 (03) :483S-512S
[6]   Current options in the prevention of thromboembolic disease [J].
Ansell, J ;
Bergqvist, D .
DRUGS, 2004, 64 (Suppl 1) :1-5
[7]   The pharmacology and management of the vitamin K antagonists [J].
Ansell, J ;
Hirsh, J ;
Poller, L ;
Bussey, H ;
Jacobson, A ;
Hylek, E .
CHEST, 2004, 126 (03) :204S-233S
[8]   The status of new anticoagulants [J].
Bates, Shannon M. ;
Weitz, Jeffrey I. .
BRITISH JOURNAL OF HAEMATOLOGY, 2006, 134 (01) :3-19
[9]   New anticoagulants: Anti IIa vs anti Xa - Is one better? [J].
Bauer, KA .
JOURNAL OF THROMBOSIS AND THROMBOLYSIS, 2006, 21 (01) :67-72
[10]  
Bauer Kenneth A, 2006, Hematology Am Soc Hematol Educ Program, P450