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Factor Xa inhibitors block the serine protease that converts prothrombin to thrombin in blood coagulation. Factor Xa sits where the intrinsic and extrinsic coagulation pathways converge and assembles with factor Va into the prothrombinase complex. Direct inhibitors bind the active site of free and complex-bound factor Xa without a cofactor. Rivaroxaban was described in 2005 as BAY 59-7939, an oral, direct factor Xa inhibitor. The discovery of apixaban from a pyrazolopyridine carboxamide series was reported in 2007. Edoxaban, betrixaban and otamixaban are further direct inhibitors, while RWJ-445167 blocks both factor Xa and thrombin.
