期刊文献+

口服Xa因子直接抑制剂阿哌沙班的临床研究进展 被引量:26

Development of clinical research on apixaban, an oral direct inhibitor of factor Xa
下载PDF
导出
摘要 阿哌沙班是口服Xa因子直接抑制剂,继达比加群酯和利伐沙班后上市,用于择期髋关节或膝关节置换手术的成年患者,以预防静脉血栓形成。本文主要介绍这个新药的研发背景、作用机制、药动学和临床试验。 As an oral direct inhibitor of factor Xa, Apixaban is approved after dabigatran etexilate and rivaroxaban, which has been used for prevention of venous thromboembolic events in adult patients who have undergone elective hip or knee replacement surgery. This article discusses the discovery, mechanism, pharmacokinetics, and clinical trials of this emerging drug.
出处 《上海医药》 CAS 2012年第17期17-20,共4页 Shanghai Medical & Pharmaceutical Journal
关键词 阿哌沙班 XA因子抑制剂 静脉血栓 apixaban factor Xa inhibitor venous thromboembolism
  • 相关文献

参考文献18

  • 1Donald JP, Michael JO, Stephanie K, et al. Discovery of 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin- 1-yl) phenyl)-4,5,6,7-tetrahydro- 1H-pyrazolo[3,4-c]pyridine-3- carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa[J]. J Med Chem, 2007, 50(22): 5339-5356.
  • 2Kylie L, Mark C. New anticoagulants for the prevention of thromboembolism[J]. Curr Phar Des, 2010, 16(31): 3472- 3474.
  • 3Ann KW. New oral anticoagulants: a practical guide for clinicians[J]. J Thromb Thrombolysis, 2010, 29(2): 182-191.
  • 4许昕,薛晓文.开发中的新型口服抗凝血药-Xa因子抑制剂[J].药学与临床研究,2010,18(3):294-298. 被引量:9
  • 5Donglu Z, Kan H, Nirmala R, et al. Metabolism,pharmacokinetics and pharmacodynamics of the factor Xa inhibitor apixaban in rabbits[J]. J Thromb Thrombolysis, 2010, 29(1): 70-80.
  • 6Raghavan N, Frost CE, Yu Z, et al. Apixaban metabolism and pharmacokinetics after oral administration to humans[J]. Drug Metab Dispos, 2008, 37(1 ): 74-81.
  • 7John WE, Martin OD, Salim Y, et al. Rationale and design of AVERROES: apixaban versus acetylsalicylic acid to prevent stroke in atrial fibrillation patients who have failed or are unsuitable for vitamin K antagonist treatment[J]. Am Heart J, 2010, 159(3): 348-353.
  • 8Jennifer C, Jack A. Apixaban, an oral direct Factor Xa inhibitor: awaiting the verdict[J]. Expert Opin Investig Dru2s. 2008. 17(12: 1937-1945.
  • 9Roser-Jones C, Becker RC. Apixaban: an emerging oral factor Xa inhibitor[J]. J Thromb Thrombolysis, 2010, 29(1): 141- 146.
  • 10Lassen MR, Davidson BL, Gallus A, et al. The efficacy and safety of apixaban, an oral, direct factor Xa inhibitor, as thromboprophylaxis in patients following total knee replacement[J]. J Thromb Haemost, 2007, 5(12): 2368-2375.

二级参考文献28

  • 1Hirsh J,Dalen J,Anderson DR,et al.Oral anticoagulants:mechanism of action,clinical effectiveness,and optimal therapeutic range[J].Chest,2001,119(1):8S-21S.
  • 2McBride BF.A preliminary assessment of the critical differences between novel oral anticoagulants currently in development[J].J Clin Pharmacol,2005,45(9):1004-7.
  • 3Gómez-Outes A,Lecumberri R,et al.New Anticoagulants:Focus on Venous Thromboembolism[J].Curr Vasc Pharmacol,2009,7(3):309-29.
  • 4Perzbom E,Strassburger J,Wilmen A,et al.In vitro and in vivo studies of the novel antithrombotic agent BAY 59-7939-an oral,direct factor Xa inhibitor[J].J Thromb Haemost,2005,3(3):514-21.
  • 5Wong PC,Crain EJ,Xin B,et al.Apixaban,an oral,direct and highly selective factor Xa inhibitoc in vitro,antithrombotic and antihemostatic studies[J].J Thromb Haemosy,2008,6 (5):820-9.
  • 6Eriksson BI,Quinlan DJ,Weitz JI Comparative pharmacodynamics and pharmacokinetics of oral direct thrombin and factor Xa inhibitors in development[J].Clin Pharmacokinet,2009,48 (1):1-22.
  • 7Saiah E,Soares C.Small molecule coagulation cascade inhibitors in the clinic[J].Curr Top Med Chem,2005,5(16):1677-95.
  • 8Turpie AG.Oral,direct factor Xa inhibitors in development for the prevention and treatment of thromboembolic diseases[J].Arterioscler.Thromb Vase Biol,2007,27 (6):1238-47.
  • 9Furugobri T,Isobe K,Honda Y,et al.DU-176b,a potent and orally active factor Xa inhibitor:in vitro and in vivo pharmacological profiles[J].J Thromb Haemost,2008,6(9):1542-9.
  • 10青爱国 武建卓.抗凝血的低分子量肽类似物.生命的化学,2008,28(4):395-8.

共引文献8

同被引文献150

引证文献26

二级引证文献67

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部