Rivaroxaban is a small-molecule,
direct factor Xa inhibitor that is under investigation for the prevention and treatment of venous and arterial
thrombosis. To date, oral
anticoagulants have been limited largely to
vitamin K antagonists. Despite their remarkable benefits,
vitamin K antagonists are limited by their narrow therapeutic window, the existence of multiple food and drug interactions, and the need for frequent monitoring and dose-adjustment.
Rivaroxaban represents a potentially attractive alternative to
warfarin, as it could enable simplified once-daily dosing, requires no therapeutic monitoring, and has a lower potential for drug interactions. At present, the safety and efficacy of
rivaroxaban for the prophylaxis and treatment of
venous thromboembolism has been evaluated in phase-II and phase-III trials involving over 24,000 patients.
Rivaroxaban is also being evaluated for the treatment of
pulmonary embolism,
secondary prevention after
acute coronary syndromes, and the prevention of
stroke and non-central nervous system
embolism in patients with non-valvular
atrial fibrillation. The need for new oral
anticoagulants, the development and pharmacology of
rivaroxaban, results of completed studies of
rivaroxaban, and details of ongoing phase-II and phase-III trials with
rivaroxaban are the subjects of this chapter.