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贝曲西班:一种直接口服的活化因子X抑制剂,用于预防因急性内科疾病住院患者的静脉血栓栓塞。

Betrixaban: a direct oral inhibitor of activated factor X for the prophylaxis of venous thromboembolism in patients hospitalized for acute medical illness.

作者信息

Escolar G, Díaz-Ricart M, Arellano-Rodrigo E

机构信息

Servicio de Anatomía Patológica, Hematopatología, Hospital Clínic,IDIBAPS, Universitat de Barcelona, Barcelona, Spain.

Servicio de Hemostasia, ICHMO, Hospital Clínic, Barcelona, Spain.

出版信息

Drugs Today (Barc). 2017 Aug;53(8):423-434. doi: 10.1358/dot.2017.53.8.2681448.

Abstract

Venous thromboembolism (VTE), comprising deep vein thrombosis and pulmonary embolism, is a serious clinical and public health concern. Hospitalization is a major risk factor for developing VTE. Hospital-associated events account for more than 50% of all cases of VTE. Heparins have demonstrated to be efficacious in the prevention of VTE in medically ill patients. Despite the demonstrated efficacy and safety of the available direct oral anticoagulants in the prevention and treatment of different thromboembolic conditions, their net benefit in the prevention of VTE in hospitalized medically ill patients has not been fully confirmed. Betrixaban is an oral, specific and direct inhibitor of human coagulation factor Xa with demonstrated efficacy and safety for the prevention of VTE in patients undergoing total knee replacement and in patients with nonvalvular atrial fibrillation. Recent studies have successfully evaluated betrixaban 80 mg once daily in the prevention of VTE in acute medically ill patients in a large phase III trial. This review will address preclinical pharmacology and main aspects of the clinical development of betrixaban as an antithrombotic agent, with specific attention to recent studies on the prophylaxis of VTE in a specific population of patients hospitalized for acute medical illnesses.

摘要

静脉血栓栓塞症(VTE),包括深静脉血栓形成和肺栓塞,是一个严重的临床和公共卫生问题。住院是发生VTE的主要危险因素。医院相关事件占所有VTE病例的50%以上。肝素已被证明在预防内科疾病患者的VTE方面有效。尽管现有直接口服抗凝剂在预防和治疗不同血栓栓塞性疾病方面已证明其有效性和安全性,但其在预防住院内科疾病患者VTE方面的净效益尚未得到充分证实。贝曲西班是一种口服、特异性的人凝血因子Xa直接抑制剂,在全膝关节置换患者和非瓣膜性心房颤动患者中已证明其预防VTE的有效性和安全性。最近的研究在一项大型III期试验中成功评估了每日一次80mg贝曲西班预防急性内科疾病患者VTE的效果。本综述将阐述贝曲西班作为抗血栓药物的临床前药理学及临床开发的主要方面,特别关注近期针对因急性内科疾病住院的特定患者群体预防VTE的研究。

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