The selectivity and bioavailability improvement of novel oral anticoagulants: An overview
The selectivity and bioavailability improvement of novel oral anticoagulants: An overview
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新型口服抗凝剂的选择性和生物利用度的提高：概述
DOI：
10.1016/j.ejmech.2018.01.067
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发表时间：
2018
影响因子：
6.7
通讯作者：
Liao Chenzhong
中科院分区：
文献类型：
--
作者：
Xie Zhouling;Tian Yongbing;Lv Xiao;Xiao Xuan;Zhan Meimiao;Cheng Kai;Li Shiyu;Liao Chenzhong
抗凝剂在预防和/或治疗血栓性疾病中发挥着关键作用。迄今为止，已开发出多种新型口服抗凝剂，其抑制凝血级联中的血浆丝氨酸蛋白酶，以克服经典抗凝剂（如华法林和肝素）的临床局限性。其中一些药物，如阿哌沙班，利伐沙班，依度沙班和达比加群，近年来已被FDA批准。本文综述了新型口服抗凝药的发现和优化，旨在提高化合物的选择性和生物利用度。还讨论了级联反应中不同靶点对出血风险的影响。我们希望在这些设计经验的基础上，将来能开发出更有效、更安全、更有选择性的抗凝药物。
Anticoagulants have exhibited a critical role in the prevention and/or treatment of thrombotic diseases. Up to now, kinds of novel oral anticoagulants, inhibiting plasma serine proteases in the coagulation cascade, have been developed to overcome the clinical limitations of classical anticoagulants (like warfarin and heparins). Some of them, such as Apixaban, Rivaroxaban, Edoxaban, and Dabigatran, have been approved by FDA in recent years. This review summarizes the discovery and optimization of representative novel oral anticoagulants with the aim to improve selectivity and bioavailability of compounds. The impact of different targets in the cascade on bleeding risk also is discussed. We hope some more effective, selective, and safer anticoagulants can be developed in the future on the basis of these design experiences.