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正在研发的新型口服抗凝药物:达比加群、利伐沙班和阿哌沙班。

Novel oral anticoagulants in development: Dabigatran, Rivaroxaban, and Apixaban.

机构信息

Department of Internal Medicine, University of Florida, College of Medicine, Gainesville, FL, USA.

出版信息

Am J Ther. 2011 Jul;18(4):332-8. doi: 10.1097/MJT.0b013e3181da0773.

Abstract

Venous thromboembolic disease, including deep vein thrombosis and pulmonary embolism, is a cause of significant mortality and morbidity. For several decades, anticoagulant options for the treatment and prevention of thrombosis have been limited mainly to agents such as unfractionated heparin and oral vitamin K antagonists, such as warfarin. Although these therapies have proven benefits, they also have important limitations that result in their underuse in routine clinical practice. A variety of novel anticoagulants with improved pharmacologic and clinical profiles are in development, offering benefits over traditional therapies. Specifically, progress has been made in the development of small molecule factor Xa inhibitors and thrombin inhibitors. With their potentially consistent and predictable clinical profile, oral formulation, and decreased need for coagulation monitoring, these new agents will likely increase the use and duration of anticoagulation treatment in thromboembolic disorders and reduce the burden associated with long-term management.

摘要

静脉血栓栓塞疾病,包括深静脉血栓形成和肺栓塞,是导致高死亡率和高发病率的一个原因。几十年来,治疗和预防血栓形成的抗凝药物选择主要局限于未分级肝素和口服维生素 K 拮抗剂,如华法林。尽管这些治疗方法已被证明有效,但它们也存在重要的局限性,导致它们在常规临床实践中的使用不足。目前正在开发各种新型抗凝药物,具有改善的药理学和临床特征,优于传统疗法。具体而言,在小分子 Xa 因子抑制剂和凝血酶抑制剂的开发方面取得了进展。这些新药物具有潜在的一致且可预测的临床特征、口服制剂和减少对凝血监测的需求,可能会增加在血栓栓塞性疾病中抗凝治疗的使用和持续时间,并降低与长期管理相关的负担。

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