生物活性

• 描述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].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT00170898	Musculoskeletal Pain	Phase 4	Completed	-	United Kingdom ... more >> For site information contact, Novartis Pharmaceuticals UK Limited Frimley, United Kingdom Collapse <<
  NCT00637949	Osteoarthritis	Phase 3	Completed	-	-
  NCT00476034	Osteoarthritis	Phase 3	Completed	-	Australia ... more >> Novartis Investigative Site Malvern, Australia Austria Novartis Investigative Site Vienna, Austria Czech Republic Novartis Investigative Site Prague, Czech Republic Finland Novartis Investigative Site Turku, Finland Germany Novartis Investigative Site Dresden, Germany Hungary Novartis Investigative Site Budapest, Hungary Israel Novartis Investigative Site Haifa, Israel Netherlands Novartis Investigative Site Lisse, Netherlands New Zealand Novartis Investigative Site Rotorua, New Zealand Poland Novartis Investigative Site Poznan, Poland Slovakia Novartis Investigative Site Bratislava, Slovakia South Africa Novartis Investigative Site Johannesburg, South Africa Spain Novartis Investigative Site Sevilla, Spain Sweden Novartis Investigative Site Uppsala, Sweden Turkey Novartis Investigative Site Izmir, Turkey Collapse <<

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• 参考文献

• [1] Dickie AP, Wilson CE, et al. The pharmacokinetics and metabolism of lumiracoxib in chimeric humanized and murinized FRG mice. Biochem Pharmacol. 2017 Jul 1;135:139-150.

  [2] Esser R, Berry C, et al. Preclinical pharmacology of lumiracoxib: a novel selective inhibitor of cyclooxygenase-2. Br J Pharmacol. 2005 Feb;144(4):538-50.

  [3] Buvanendran A, Barkin R. Lumiracoxib. Drugs Today (Barc). 2007;43(3):137-147

  [4] Lyseng-Williamson KA, Curran MP. Lumiracoxib. Drugs. 2004;64(19):2237-2248

  [5] Rordorf CM, Choi L, Marshall P, Mangold JB. Clinical pharmacology of lumiracoxib: a selective cyclo-oxygenase-2 inhibitor. Clin Pharmacokinet. 2005;44(12):1247-1266

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