凝血因子Ⅺa小分子抑制剂研究进展

Research Progress in Small Molecular Inhibitors of Coagulation Factor XIa

血栓性疾病严重影响着人类的生活质量,其发病率呈逐年上升的趋势。目前临床上用于治疗血栓性疾病的药物主要是抗凝药物,尽管其抗血栓效果较好,但往往伴随着出血风险。近几年研究发现,凝血因子Ⅺa(FⅪa)抑制剂能够降低静脉血栓的发病率而对出血并没有明显影响,因而在治疗血栓性疾病方面具有重要潜在价值。因此,FⅪa抑制剂可作为一种新型的抗血栓药物。综述近年来发现的源自天然产物和化学合成的小分子FⅪa抑制剂的研究进展,为FⅪa抑制剂类药物设计和发现提供参考。

Thrombosis has serious impact on people＇s quality of life, and its morbidity has an increasing tendency year by year. Currently available treatments are mainly anticoagulants. Although these anticoagulants have better antithrombotic effects, they are often associated with bleeding risk. Recent study revealed that coagulation factor Xla （FXIa） inhibitors can reduce the incidence of venous thrombosis without any effect on bleeding, which was of great importance in the treatment of thrornbotic diseases. Therefore, FXIa inhibitors have the potential to be developed into a new type of antithrombotic drugs. Recent advances in the research of small molecular FXIa inhibitors derived from natural products and produced by chemical syntheses are reviewed, so as to provide reference for new drug design and discovery of FXIa inhibitors.