文档介绍：达比加群酯研发经历总结
摘要
达比加群酯,美国FDA和欧盟分别于2010年l 0月19日和2008年3月18日批准Boellringer Ingelllein制药公司的达比加群醋胶囊用于心房颤动患者预防中风和血栓生成。分子式为C34H41N7O5,。达比加群酯是最前沿的新一代口服抗凝药物直接凝血酶抑制剂(DTIs),针对急性和慢性血栓栓塞性疾病的预防及治疗这一急需满足的临床需求。
Dabigatran etexilate, American FDA and European Union respectively in 2010 L 0 on 19 March and March 18, 2008 approved Boellringer Ingelllein pharmaceuticals of dabigatran vinegar capsule for the prevention of stroke in patients with atrial fibrillation and thrombus formation. The molecular formula is C34H41N7O5, relative molecular quality . Dabigatran is a new oral anticoagulant direct thrombin inhibitor most front (DTIs), according to clinical demand for prevention of acute and chronic thromboembolic disease and treatment of the need to meet.
药物简介
达比加群酯是一种新型的合成的直接凝血酶抑制剂,是dabigatran的前体药物,属非肽类的凝血酶抑制剂。口服经胃肠吸收后,在体内转化为具有直接抗凝血活性的dabigatran。dabigatran结合于凝血酶的纤维蛋白特异结合位点,阻止纤维蛋白原裂解为纤维蛋白,从而阻断了凝血瀑布网络的最后步骤及血栓形成。dabigatran可以从纤维蛋白一凝血酶结合体上解离,发挥可逆的抗凝作用。
Dabigatran is a new synthetic direct thrombin inhibitor, is a prodrug of dabigatran, is a thrombin inhibitor non-peptide. Oral absorbed by the gastrointestinal, converted in the body to have direct anticoagulant activity of dabigatran. Fibrin specific dabigatran binding to thrombin binding sites, preventing fibrinogen lysis fibrin, thereby blocking the last step and thrombus coagulation work formation. Dabigatran can be from binati