Factor Xa
Factor X (the eponym Stuart–Prower factor) is an enzyme of the coagulation cascade. It is a serine endopeptidase (protease group S1, PA clan).Factor X is synthesized in the liver and requires vitamin K for its synthesis. Factor X is activated, by hydrolysis, into factor Xa by both factor IX and factor VII with its cofactor, tissue factor . It is therefore the first member of the final common pathway or thrombin pathway. It acts by cleaving prothrombin in two places (an arg-thr and then an arg-ile bond), which yields the active thrombin. This process is optimized when factor Xa is complexed with activated co-factor V in the prothrombinase complex. Factor Xa is inactivated by protein Z-dependent protease inhibitor (ZPI), a serine protease inhibitor (serpin). The affinity of this protein for factor Xa is increased 1000-fold by the presence of protein Z, while it does not require protein Z for inactivation of factor XI. Defects in protein Z lead to increased factor Xa activity and a propensity for thrombosis.
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Apixaban is a highly selective, reversible, and direct inhibitor of Human Factor X and Rabbit Factor X with Ki of 0.08 nM and 0.17 nM, respectively. Apixaban exhibits a high degree of potency, selectivity, and efficacy on Factor X with Ki of 0.08 nM and 0.17 nM for Human Factor X and Rabbit Factor X, respectively.
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Edoxaban是factor Xa选择性抑制剂，也是具有口服效应的抗凝药物。
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Rivaroxaban是一种口服具有直接作用的Factor Xa抑制剂，Ki值为0.4 nM，IC50值为0.7 nM。
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