rivaroxaban-bay-59-7939

Description: Rivaroxaban (BAY59-7939; BAY-59-7939; trade name: Xarelto), an approved anticoagulant drug used to treat and prevent blood clots, is the first orally bioavailable, selective and direct inhibitor of Factor Xa with potential anti-coagulant activity. It inhibits Factor Xa with a Ki and IC50 of 0.4 nM and 0.7 nM in cell-free assays, respectively. Rivaroxaban binds to the Tyr288 in S1 pocket of factor Xa through the interaction of Tyr288 and the chlorine substituent of the chlorothiophene moiety. Rivaroxabanis used as an oral anticoagulant developed by Bayer amd was marketed in many countries with the trade name of Xarelto. Rivaroxaban is well absorbed from the gut and maximum inhibition of factor Xa occurs four hours after a dose. The effects lasts 8A–12 hours, but factor Xa activity does not return to normal within 24 hours so once-daily dosing is possible.

References: J Thromb Haemost. 2005 Mar; 3(3):514-21; J Pharmacol Exp Ther. 2011 Jul; 338(1):372-80.

Related CAS: 865479-71-6 (R-enantiomer of Rivaroxaban)