凝血因子Ⅱ在凝血級聯(lián)反應(yīng)中處于下游的關(guān)鍵位置，被激活后形成凝血酶而催化纖維蛋白原產(chǎn)生纖維蛋白導(dǎo)致凝血，因此其為血栓形成的關(guān)鍵因素。抑制凝血酶可以延長凝血時(shí)間，減少血栓形成風(fēng)險(xiǎn)。英國AstraZeneca公司研發(fā)的新一代口服直接凝血酶因子Ⅱa抑制劑AZD0837可用于治療和預(yù)防心房顫動(dòng)引起的卒中和深靜脈血栓的發(fā)生。目前已經(jīng)公布的臨床前、臨床Ⅰ期和Ⅱ期實(shí)驗(yàn)數(shù)據(jù)顯示，其具有優(yōu)于華法林的治療效果，因此具有巨大的市場潛力。

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.

國家重大新藥創(chuàng)制專項(xiàng)（2011ZX09401-009）