Apixaban

Apixaban is a potent, orally effective reversible, direct, highly selective Factor Xa active site inhibitor whose antithrombotic activity is independent of antithrombin III. Apoxaban can inhibit free and thrombus binding factor Xa and inhibit prothrombin activity. Apoxaban had no direct effect on platelet aggregation, but indirectly inhibited thrombine-induced platelet aggregation. By inhibiting factor Xa, Apixaban inhibits thrombin production and inhibits thrombus formation. Preclinical results in animal models show that Apoxaban has an antithrombotic effect and can prevent arterial and venous thrombosis at dose levels that do not affect hemostatic function.
In the 10mg dose range, the absolute bioavailability of Apixaban is about 50%. Apixaban is rapidly absorbed and reaches maximum concentration (Cmax) 3 to 4 hours after administration, and eating has no effect on AUC or Cmax of 10mg of Apixaban. Apixaban can be taken with or without meals.
In the dose range of 10mg, Apixaban showed linear pharmacokinetics and was dose-dependent. When the dose of Apixaban was ≥25mg, it showed dissolution restricted absorption and decreased bioavailability. The exposure parameters of Apixaban showed low to moderate variation, with a coefficient of variation (CV) of about 20% within individuals and about 30% between individuals.