2. Background
• Rivaroxaban (BAY 59-7939) is an oral
anticoagulant invented and manufactured by
Bayer; in a number of countries it is marketed
as Xarelto.
3. • It is the first available orally active
direct factor Xa inhibitor.
• Rivaroxaban is well absorbed from the gut
and maximum inhibition of factor Xa occurs
four hours after a dose. The effects lasts 8–12
hours, but factor Xa activity does not return to
normal within 24 hours so once-daily dosing is
possible.
4. • Rivaroxaban is an oxazolidinone derivative
optimized for inhibiting both free Factor Xa
and Factor Xa bound in the
prothrombinase complex.
• It is a highly selective
direct Factor Xa inhibitor with oral
bioavailability and rapid onset of action.
5. • Inhibition of Factor Xa interrupts the intrinsic
and extrinsic pathway of the
blood coagulation cascade, inhibiting
both thrombin formation and development of
thrombi. Rivaroxaban does not inhibit
thrombin (activated Factor II), and no effects
on platelets have been demonstrated.
6. • ROCKET AF is double-blind phase 3 study in
more than 14 000 patients with nonvalvular
atrial fibrillation (AF).
• They were randomized to 20-mg rivaroxaban
once daily (or 15 mg in patients with
moderate renal impairment at screening) or
to dose-adjusted warfarin (titrated to an
international normalized ratio [INR] of 2.5).
7. • The study was led by the Duke Clinical
Research Institute, Durham, NC, and an
international academic executive committee.
8. Higher Risky AF
• It has recently been reported that the patients
enrolled in ROCKET-AF are at higher risk of
stroke than those who have participated in
other similar trials, with 90% having a
CHADS2 score of 3 or higher compared with
fewer than 50% of those enrolled in four
comparable studies: RE-LY, ACTIVE
W,AMADEUS, and SPORTIF V.