Wednesday, May 2, 2012

Rivaroxaban




Rivaroxaban
Systematic (IUPAC) name
(S)-5-chloro-N-{[2-oxo-3-[4-(3-oxomorpholin-4-yl)
phenyl]oxazolidin-5-yl]methyl} thiophene-2-carboxamide
Clinical data
Trade namesXarelto
AHFS/Drugs.comMicromedex Detailed Consumer Information
Licence dataEMA:LinkUS FDA:link
Pregnancy cat.C (US)
Legal statusPOM (UK) -only (US)
Routesoral
Pharmacokinetic data
Bioavailability80% to 100%; Cmax = 2 – 4 hours (10 mg oral)[1]
MetabolismCYP3A4 , CYP2J2 and CYP-independent mechanisms[1]
Half-life10 mg oral 7 – 11 hours[1]
Excretion2/3 metabolized in liver and 1/3 eliminated unchanged[1]
Identifiers
CAS number366789-02-8 http://www.casbook.com/366789-02-8 
ATC codeB01AX06
PubChemCID 6433119
DrugBankDB06228
ChemSpider8051086 Yes
UNII9NDF7JZ4M3 Yes
ChEMBLCHEMBL198362 Yes
Chemical data
FormulaC19H18ClN3O5S 
Mol. mass435.882 g/mol
SMILESeMolecules & PubChem
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Rivaroxaban (BAY 59-7939) is an oral anticoagulant invented and manufactured by Bayer; in a number of countries it is marketed as Xarelto.[1] In the United States, it is marketed by Janssen Pharmaceutica.[2] 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.