Department of Medicine, Lenox Hill Hospital, New York, NY 10075, USA.
Hematol Oncol Clin North Am. 2010 Aug;24(4):739-53, ix. doi: 10.1016/j.hoc.2010.05.001.
Direct oral factor IIa inhibitors represent a new class of anticoagulants for the prevention and treatment of venous and selected arterial thomboembolisms. Dabigatran etexilate is the most studied and promising of the oral direct thrombin inhibitors. Preclinical and early-phase clinical studies show it to have a predictable and reliable pharmacokinetic and pharmacodynamic profile, whereas advanced phase 3 trials prove it to be noninferior to traditional anticoagulants in selective conditions for the prevention and treatment of venous and arterial thromboembolism. Other advantages of this drug, including a lack of interaction with cytochrome P450 enzymes or with food and drugs, rapid onset of action, good safety profile, lack of need for routine monitoring, broad therapeutic window, and fixed-dose administration, make this a competitive oral anticoagulant.
直接口服 IIa 因子抑制剂是预防和治疗静脉和特定动脉血栓栓塞的新型抗凝药物。达比加群酯是研究最多且最有前途的口服直接凝血酶抑制剂之一。临床前和早期临床研究表明，它具有可预测和可靠的药代动力学和药效学特征，而高级 3 期试验证明，在预防和治疗静脉和动脉血栓栓塞的特定情况下，它与传统抗凝剂一样有效。该药的其他优点包括与细胞色素 P450 酶或食物和药物无相互作用、起效迅速、安全性良好、无需常规监测、治疗窗宽、固定剂量给药等，使其成为一种有竞争力的口服抗凝剂。
