新一代口服直接凝血酶因子Ⅱa抑制剂AZD0837  

A new generation of oral direct thrombin factorⅡa inhibitor AZD0837

作　　者：刘洪强[1,2] 蔡志强[1] 张伟光[1,2] 徐为人[1] 汤立达[1] 申秀萍[1] 韩书文[2] 

机构地区：[1]天津药物研究院天津市新药设计与发现重点实验室,释药技术与药代动力学国家重点实验室,天津300193 [2]天津中医药大学,天津300193

出　　处：《现代药物与临床》2012年第3期262-267,共6页Drugs & Clinic

基　　金：国家重大新药创制专项(2011ZX09401-009)

摘　　要：凝血因子Ⅱ在凝血级联反应中处于下游的关键位置,被激活后形成凝血酶而催化纤维蛋白原产生纤维蛋白导致凝血,因此其为血栓形成的关键因素。抑制凝血酶可以延长凝血时间,减少血栓形成风险。英国AstraZeneca公司研发的新一代口服直接凝血酶因子Ⅱa抑制剂AZD0837可用于治疗和预防心房颤动引起的卒中和深静脉血栓的发生。目前已经公布的临床前、临床Ⅰ期和Ⅱ期实验数据显示,其具有优于华法林的治疗效果,因此具有巨大的市场潜力。Clotting factor Ⅱ is the key factor of the blood coagulation cascade in the downstream position,activated to form blood coagulation enzyme（IIa）,catalyze fibrinogen production of fiber protein,and lead to blood coagulation,so it is the crucial factor for the formation of blood clots.The inhibition of thrombin could extend the coagulation time and reduce the risk of thrombosis.AZD0837 is a new generation of oral direct thrombin factor Ⅱa inhibitor which is developed and researched by British AstraZeneca Company,and could be used to prevent and treat stroke and the deep vein thrombosis caused by atrial fibrillation（AF）.Published data of pre-clinical and clinical phases I and II experiments showed that the AZD0837 had a better treatment effect than Warfarin with a great market potential in the future.

关 键 词：AZD0837 抗血栓 抗凝血药 心房颤动 

分 类 号：R97[医药卫生—药品]