选择性凝血因子Ⅺa抑制剂防治血栓性疾病的临床研究进展

Research progress in clinical trials of the coagulation factor XIa inhibitors for the prevention and treatment of thrombotic diseases

血栓性疾病严重威胁人类生命健康,影响生活质量。虽然近年来不断有新型抗血栓药物上市应用,但往往伴随着不同程度的高出血风险,因此研发效果好而出血风险低的抗血栓药物显得尤为重要。凝血因子Ⅺa(FⅪa)是主要参与凝血过程内源性途径的关键蛋白酶因子,抑制该因子功能可发挥抗血栓作用。近期研究显示,特异性FⅪa抑制剂能够降低静脉血栓栓塞症发病率而对出血无明显影响,因此在防治血栓性疾病方面具有重要潜在价值。目前已有多个FⅪa抑制剂类药物处在不同的研究和开发阶段,适应证均为血栓性疾病。本文综述了近年正在开展临床研究的FⅪa抑制剂,为该类药物进一步上市及临床应用提供参考。

Thrombotic diseases have a high morbidity and exert a serious impact on life quality of human.Although some anticoagulants have been marketed and applied in recent years,they are often associated with bleeding risk.Therefore,the development of anticoagulants with lower bleeding risk is particularly important.Coagulation factorⅪa(FⅪa)is a key factor controlling the production of thrombin and plays an important role in the formation of thrombus.Researches have shown that FⅪa inhibitors can reduce the incidence of thrombotic diseases while reducing bleeding events,which have the potential to be developed into a new type of anticoagulants.Currently,several FⅪa inhibitors are in different stages of research and development for prevention and treatment of thrombotic diseases;however,none of them has been approved for marketing.Therefore,this review summarizes recent advances in the clinical research of FⅪa inhibitors,in order to provide reference for further marketing and clinical application of FⅪa inhibitors.