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阿哌沙班:用于静脉血栓栓塞症的治疗。

Apixaban: A Review in Venous Thromboembolism.

机构信息

Springer, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand.

出版信息

Drugs. 2016 Oct;76(15):1493-1504. doi: 10.1007/s40265-016-0644-6.

Abstract

Apixaban (Eliquis) is an oral, direct factor Xa inhibitor that is available for use in the treatment and secondary prevention of venous thromboembolism (VTE). Like other direct oral anticoagulants (DOACs), apixaban has generally predictable pharmacological properties and does not require routine anticoagulation monitoring. In large phase III trials, oral apixaban was noninferior to subcutaneous enoxaparin sodium overlapped with and followed by oral warfarin (enoxaparin/warfarin) in the treatment of adults with acute VTE over 6 months with regard to the incidence of recurrent VTE or VTE-related death (AMPLIFY), and was significantly more effective than placebo in the prevention of recurrent VTE or all-cause mortality over 12 months in patients who had completed 6-12 months' anticoagulation treatment for VTE (AMPLIFY-EXT). Apixaban was generally well tolerated in these trials; the risks of major bleeding and the composite endpoint of major or clinically relevant nonmajor (CRNM) bleeding with apixaban were significantly lower than enoxaparin/warfarin in AMPLIFY and not significantly different from that of placebo in AMPLIFY-EXT. Similarly, in Japanese adults with acute VTE (AMPLIFY-J), apixaban was associated with a significantly lower risk of major or CRNM bleeding than unfractionated heparin plus warfarin, and no cases of recurrent VTE or VTE-related death over 24 weeks. Thus, apixaban is useful therapeutic alternative for the management of adults with VTE.

摘要

阿哌沙班(艾乐妥)是一种可口服的直接因子 Xa 抑制剂,可用于治疗和二级预防静脉血栓栓塞症(VTE)。与其他直接口服抗凝剂(DOAC)一样,阿哌沙班通常具有可预测的药理学特性,不需要常规抗凝监测。在大型 III 期临床试验中,与皮下依诺肝素钠重叠并随后口服华法林(依诺肝素/华法林)相比,口服阿哌沙班在治疗急性 VTE 超过 6 个月方面非劣效于治疗成人急性 VTE,复发 VTE 或 VTE 相关死亡(AMPLIFY),并且在完成 6-12 个月抗凝治疗后 12 个月内预防复发 VTE 或全因死亡率方面显著优于安慰剂在接受 VTE 治疗的患者中(AMPLIFY-EXT)。在这些试验中,阿哌沙班通常具有良好的耐受性;大出血风险和主要或临床上显著非主要(CRNM)出血复合终点的风险明显低于 AMPLIFY 中的依诺肝素/华法林,并且在 AMPLIFY-EXT 中与安慰剂无显著差异。同样,在急性 VTE 的日本成年人(AMPLIFY-J)中,与未分级肝素加华法林相比,阿哌沙班与主要或 CRNM 出血风险显著降低,24 周内无复发性 VTE 或 VTE 相关死亡。因此,阿哌沙班是治疗 VTE 成人的有用治疗选择。

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