How XARELTO® Works
Targeting Factor Xa to address thrombotic risk
XARELTO® is a selective inhibitor of Factor Xa (FXa). It does not require a cofactor (such as Anti-thrombin III) for activity. Rivaroxaban inhibits free FXa and prothrombinase activity. Rivaroxaban has no direct effect on platelet aggregation, but indirectly inhibits platelet aggregation induced by thrombin. By inhibiting FXa, rivaroxaban decreases thrombin generation. Based on in vitro studies, rivaroxaban demonstrated selective inhibition of both free and clot-bound FXa as well as FXa in the prothrombinase complex.1-3 Watch this patient-friendly MOA video
The clinical significance of this mechanistic information has not been established.
XARELTO® has a distinct pharmacologic profile
Rapid onset of action
XARELTO® reaches maximum plasma concentrations and inhibits Factor Xa 2 to 4 hours after the medication is taken.†6
The terminal elimination half-life is 5 to 9 hours in healthy subjects aged 20 to 45 years and 11 to 13 hours in healthy, elderly subjects.
Approximately one-third (36%) of the administered compound was recovered as unchanged drug in the urine and 7% was recovered as unchanged drug in feces. This may be an important consideration for patients with renal impairment (creatinine clearance [CrCl] ≤50 mL/min).
A 10-mg dose of XARELTO® has nearly complete bioavailability and is not affected by food. XARELTO® 10-mg tablets can be taken with or without food
A 20-mg dose of XARELTO® has nearly complete bioavailability when taken with food. XARELTO® 15-mg and 20-mg tablets should be taken with food
The clinical significance of this pharmacokinetic information has not been established.
†Phase 1, randomized, single-blinded, placebo-controlled, dose-escalation study in 108 healthy white males aged 19 to 45 years. Single doses of rivaroxaban 1.25-, 5-, 10-, 15-, 20-, 30-, 40-, 60-, or 80-mg tablets were tested.