Rao P S S, Burkart T
Department of Pharmaceutical Sciences, College of Pharmacy, The University of Findlay, Findlay, OH 45840, USA.
Department of Experiential Education, College of Pharmacy, The University of Findlay, Findlay, OH 45840, USA.
Blood Rev. 2017 Jul;31(4):205-211. doi: 10.1016/j.blre.2017.02.002. Epub 2017 Feb 5.
Approximately 900,000 people are affected by some sort of venous thromboembolic (VTE) event every year in the United States. VTE diagnosis used to mean treatment with medications that required routine lab monitoring for safety and efficacy. Activated factor X (FXa) inhibition has emerged as a convenient pathway for management of VTE and currently three FXa inhibitors are available for anticoagulation management - rivaroxaban, apixaban, and edoxaban. Continued development of medications utilizing this pathway may offer advantages via novel pharmacokinetic or pharmacodynamic properties that may minimize the adverse effects associated with traditional anticoagulant therapy. This review summarizes the available information regarding pharmacokinetic, pharmacodynamic, and early safety and efficacy data for three factor Xa inhibitors being developed - darexaban, betrixaban and nokxaban. The studies reviewed in this article suggests that three newer agents possess the potential for promise based on early phase I and II trials.
在美国，每年约有90万人受到某种静脉血栓栓塞（VTE）事件的影响。VTE的诊断过去意味着使用需要进行常规实验室监测以确保安全性和有效性的药物进行治疗。活化因子X（FXa）抑制已成为管理VTE的便捷途径，目前有三种FXa抑制剂可用于抗凝管理——利伐沙班、阿哌沙班和依度沙班。利用这一途径持续开发药物可能会通过新的药代动力学或药效学特性带来优势，这些特性可能会将与传统抗凝治疗相关的不良反应降至最低。本综述总结了关于正在开发的三种因子Xa抑制剂——达瑞沙班、贝曲沙班和诺沙班的药代动力学、药效学以及早期安全性和有效性数据的现有信息。本文所综述的研究表明，基于早期的I期和II期试验，这三种新型药物具有展现前景的潜力。
