Lumiracoxib is a COX2 selective inhibitor and a non-steroidal anti-inflammatory drug (NSAID), which inhibits COX2 with IC50 and Ki values of 0.14 μM and 0.06 μM and inhibits COX1 with Ki of 3 μM.
Lumiracoxib is a selective cyclooxygenase (COX)-2 inhibitor that possesses a carboxylic acid group that makes it weakly acidic. It has good oral bioavailability; maximum plasma concentrations are reached two hours after oral administration. Lumiracoxib has been found to be effective at doses of 100 - 400 mg once a day for chronic pain and 400 mg/day for acute pain. In comparison to NSAIDs (nonsteroidal anti-inflammatory drugs), patients taking lumiracoxib experience significantly fewer adverse events and greater tolerability[3]. In single- and multiple-dose well designed trials in patients with acute pain associated with primary dysmenorrhoea, dental or orthopaedic surgery or tension-type headache, lumiracoxib 100 - 800 mg once daily was more effective in relieving acute pain than placebo or controlled-release oxycodone 20 mg, and was at least as effective as selective COX-2 inhibitors or nonselective NSAIDs[4]. COX-2 selectivity of lumiracoxib is associated with a reduced incidence of gastroduodenal erosions compared with naproxen and a lack of effect on both small and large bowel permeability[5].
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