Darexaban

Darexaban (YM150) is a potent, selective and orally active factor Xa (FXa) inhibitor with an IC₅₀ of 54.6 nM. Darexaban shows high selectivity against other related serine proteases, such as trypsin, thrombin, and kallikrein. Darexaban has anticoagulant and antithrombotic effects^[1][2][3]. In Vitro: Darexaban is an oral direct factor Xa (FXa) inhibitor that is rapidly and extensively metabolized into its glucuronide conjugate (YM-222714) post-administration. Darexaban competitively and selectively inhibits human FXa, and also inhibits the prothrombin activation induced by prothrombinase complex or whole blood clot with similar potency to free FXa^[2]. In Vivo: In mice, Darexaban inhibits FXa activity in plasma with an ED₅₀ value of 24.8 mg/kg. Darexaban prolonges prothrombin time (PT) at 3 mg/kg^[2].
In a pulmonary thromboembolism (PE) mouse model, Darexaban dose-dependently reduces the mortality rate, significantly so at 10 mg/kg^[2].
In a FeCl3-induced venous thrombosis (VT) mouse model, Darexaban (0.3-10 mg/kg) dose-dependently decreases the thrombus protein content, significantly so at doses of 3 mg/kg or higher^[2].