Description: Betrixaban (PRT054021) is a non-vitamin K oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor Xa [1]. It was selected among all lead compounds due to its low hERG channel affinity while sustaining its factor Xa inhibition capacity [3]. Betrixaban, now...

Betrixaban is an inhibitor of the serine protease Factor Xa (Ki = 0.117 nM, IC50 = 1.5 nM), the enzyme that activates prothrombin in the blood coagulation cascade. It is selective for Factor Xa over hERG channels (Ki = 1.8 µM, IC50 = 8.9 µM), indicating a low potential for adverse cardiac effects. In vitro,...