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How XARELTO® Works

Targeting Factor Xa to address thrombotic risk

XARELTO® targets Factor Xa at a central point in the coagulation cascade XARELTO® targets Factor Xa at a central point in the coagulation cascade

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

The clinical significance of this mechanistic information has not been established.

 

The XARELTO® MOA

See how XARELTO® works at a central point in the coagulation cascade.

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 the elderly.

Bioavailability

  • 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

There are no dose modifications required for age, weight, or gender.

 

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.

 

Indications

 

IMPORTANT SAFETY INFORMATION

 

Indication and Important saftey Information

 

INDICATIONS

  • Reducing the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation (AF). There are limited data on the relative effectiveness of XARELTO® (rivaroxaban) and warfarin in reducing the risk of stroke and systemic embolism when warfarin therapy is well controlled.
  • Treatment of deep vein thrombosis (DVT).
  • Treatment of pulmonary embolism (PE).
  • Reduction in the risk of recurrence of DVT and of PE following initial 6 months treatment for DVT and/or PE.
  • Prophylaxis of DVT, which may lead to PE in patients undergoing knee replacement surgery.
  • Prophylaxis of DVT, which may lead to PE in patients undergoing hip replacement surgery.

References:

  1. Perzborn E, Strassburger J, Wilmen A, et al. In vitro and in vivo studies of the novel antithrombotic agent BAY 59-7939—an oral, direct Factor Xa inhibitor. J Thromb Haemost. 2005;3(3):514-521.
  2. Depasse F, Busson J, Mnich J, et al. Effect of BAY 59-7939—a novel, oral, direct Factor Xa inhibitor—on clot-bound Factor Xa activity in vitro. J Thromb Haemost. 2005;3(suppl 1). Abstract P1104.
  3. Turpie AG. Oral, direct Factor Xa inhibitors in development for the prevention and treatment of thromboembolic diseases. Arterioscler Thromb Vasc Biol. 2007;27(6):1238-1247.
  4. Davie EW, Fujikawa K, Kisiel W. The coagulation cascade: initiation, maintenance, and regulation. Biochemistry. 1991;30(43):10363-10370.
  5. Hoffman M, Monroe DM. Coagulation 2006: a modern view of hemostasis. Hematol Oncol Clin North Am. 2007;21(1):1-11.
  6. Kubitza D, Becka M, Voith B, Zuehlsdorf M, Wensing G. Safety, pharmacodynamics, and pharmacokinetics of single doses of BAY 59-7939, an oral, direct Factor Xa inhibitor. Clin Pharmacol Ther. 2005;78(4):412-421.