Apixaban

被引:8
作者
Bates, S. M. [1 ]
Weitz, J. I. [1 ,2 ]
机构
[1] McMaster Univ, Dept Med, Hamilton, ON, Canada
[2] McMaster Univ, Dept Biochem, Hamilton, ON, Canada
关键词
factor Xa inhibitor; anticoagulant;
D O I
10.1358/dof.2008.033.04.1187022
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Currently available anticoagulants include heparin, low-molecular-weight heparin, fondaparinux and warfarin. Despite advances, currently available agents have limitations that have provided the impetus for the development of new drugs for the prevention and treatment of both venous and arterial thromboembolism. Novel anticoagulants targeting specific steps in coagulation are in various stages of development. Apixaban (BMS-562247) is an orally available, highly selective, reversible inhibitor of factor Xa that is currently in late-stage clinical development. Preclinical and phase I studies showed that this agent is safe, well tolerated and has antithrombotic activity. Promising phase II studies evaluating apixaban for the prevention and treatment of venous thromboembolism have been completed and phase III clinical studies are ongoing.
引用
收藏
页码:293 / 301
页数:9
相关论文
共 59 条
[1]   Randomized clinical trial of postoperative fondaparinux versus perioperative dalteparin for prevention of venous thromboembolism in high-risk abdominal surgery [J].
Agnelli, G ;
Bergqvist, D ;
Cohen, AT ;
Gallus, AS ;
Gent, M .
BRITISH JOURNAL OF SURGERY, 2005, 92 (10) :1212-1220
[2]  
[Anonymous], W02007001385, Patent No. 2007001385
[3]   Oral anticoagulants - The old and the new [J].
Ansell, J .
DM DISEASE-A-MONTH, 2005, 51 (2-3) :208-212
[4]   Fondaparinux compared with enoxaparin for the prevention of venous thromboembolism after elective major knee surgery. [J].
Bauer, KA ;
Eriksson, BI ;
Lassen, MR ;
Turpie, AGG .
NEW ENGLAND JOURNAL OF MEDICINE, 2001, 345 (18) :1305-1310
[5]   The use of prothrombin(S525C) labeled with fluorescein to directly study the inhibition of prothrombinase by antithrombin during prothrombin activation [J].
Brufatto, N ;
Nesheim, ME .
JOURNAL OF BIOLOGICAL CHEMISTRY, 2001, 276 (21) :17663-17671
[6]   Fondaparinux or Enoxaparin for the initial treatment of symptomatic deep venous thrombosis -: A randomized trial [J].
Büller, HR ;
Davidson, BL ;
Decousus, H ;
Gallus, A ;
Gent, M ;
Piovella, F ;
Prins, MH ;
Raskob, G ;
Segers, AEM ;
Cariou, R ;
Leeuwenkamp, O ;
Lensing, AWA .
ANNALS OF INTERNAL MEDICINE, 2004, 140 (11) :867-873
[7]  
Büller HR, 2003, NEW ENGL J MED, V349, P1695
[8]  
Buller HR, 2007, 21 C INT SOC THROMB
[9]  
CAPRINI JA, 2007, 21 C INT SOC THROMB
[10]   Efficacy and safety of fondaparinux for the prevention of venous thromboembolism in older acute medical patients: randomised placebo controlled trial [J].
Cohen, AT ;
Davidson, BL ;
Gallus, AS ;
Lassen, MR ;
Prins, MH ;
Tomkowski, W ;
Turpie, AGG ;
Egberts, JFM ;
Lensing, AWA .
BMJ-BRITISH MEDICAL JOURNAL, 2006, 332 (7537) :325-327