Lumiracoxib, a selective COX-2 inhibitor discovered and
developed by Novartis, was approved in September, 2003 in
the UK for the symptomatic relief of osteoarthritis and short term relief of moderate to severe acute pain associated with
primary dysmenorrhea, dental surgery and orthopedic surgery. After an initial not approvable letter issued by FDA in
September 2003, Novartis expects to re-submit a NDA by
early 2006 following the completion of several studies
requested by FDA.
使用
Treatment of rheumatoid arthritis, osteoarthritis, and pain prevention.
薬物動態学
Lumiracoxib is rapidly absorbed, with an oral bioavailability of 74%, and
reaches a maximum plasma concentration 2 hour after dosing. It is highly plasma protein bound and has a short
elimination half-life of approximately 4 hours, demonstrating linear plasma pharmacokinetics with no accumulation
during multiple dosing.
臨床応用
Lumiracoxib is a selective COX-2 inhibitor developed for the treatment of osteoarthritis, rheumatoid
arthritis, and acute pain. It structurally differs from the other selective COX-2 inhibitors in being a phenylacetic acid
with a carboxylic acid group (pKa = 4.7).
代謝
Lumiracoxib is extensively metabolized involving oxidation of its 5-Me group and
4′-hydroxylation of the dihalogenated aromatic ring. The major in vitro oxidative pathways is catalyzed primarily by
CYP2C9. Lumiracoxib and its metabolites are excreted via renal and fecal routes in approximately equal amounts.
The COX-2 selectivity was confirmed by a lack of inhibition of arachidonic acid and collagen-induced platelet
aggregation. As with other selective coxibs, lumiracoxib exhibits a reduced incidence of gastroduodenal erosions
compared with that of naproxen. It was approved for use in the United Kingdom and the United States in 2007.
