Development of new anticoagulants has been in constant demand throughout the world due
to increasing rate of morbidity and mortality caused by thrombotic diseases. Factor Xa (FXa), one of
the enzymes and validated target for anticoagulation, regulates the production of thrombin in the coagulation
cascade. The importance of oral FXa inhibitors like rivaroxaban, apixaban and edoxaban in
thromboembolic conditions is well supported by increasing number of patents and research publications
during the recent years. Direct FXa inhibitors as antithrombotic agents offer selective, efficacious
and orally active therapy with respect to the other traditional anticoagulants. Newly developed patented
molecules are mainly structural bioisosteres of existing drugs and have exhibited better efficacy and
safety profile. Development of antidotes for oral direct FXa inhibitors is in pipeline and their expected
approval for therapeutic purposes will be further beneficial to anticoagulation therapy. This review is
mainly focused on industrial and academic patents on the discovery of direct FXa inhibitors. The review
covers patented compounds from December 2011 till date, describing various structural modifications
along with biological activity data and advances in the process and formulation technologies of
the reported FXa inhibitors.
Keywords: Anticoagulant, apixaban, factor Xa inhibitor, rivaroxaban, thrombosis, VTE.
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