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In cellular assays, lumiracoxib had an IC<jats:sub>50<\/jats:sub> of 0.14\u2003<jats:italic>\u03bc<\/jats:italic><jats:sc>M<\/jats:sc> in COX\u20102\u2010expressing dermal fibroblasts, but caused no inhibition of COX\u20101 at concentrations up to 30\u2003<jats:italic>\u03bc<\/jats:italic><jats:sc>M<\/jats:sc> (HEK 293 cells transfected with human COX\u20101).<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>In a human whole blood assay, IC<jats:sub>50<\/jats:sub> values for lumiracoxib were 0.13\u2003<jats:italic>\u03bc<\/jats:italic><jats:sc>M<\/jats:sc> for COX\u20102 and 67\u2003<jats:italic>\u03bc<\/jats:italic><jats:sc>M<\/jats:sc> for COX\u20101 (COX\u20101\/COX\u20102 selectivity ratio 515).<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Lumiracoxib was rapidly absorbed following oral administration in rats with peak plasma levels being reached between 0.5 and 1\u2003h.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p><jats:italic>Ex vivo<\/jats:italic>, lumiracoxib inhibited COX\u20101\u2010derived thromboxane B<jats:sub>2<\/jats:sub> (TxB<jats:sub>2<\/jats:sub>) generation with an ID<jats:sub>50<\/jats:sub> of 33\u2003mg\u2003kg<jats:sup>\u22121<\/jats:sup>, whereas COX\u20102\u2010derived production of prostaglandin E<jats:sub>2<\/jats:sub> (PGE<jats:sub>2<\/jats:sub>) in the lipopolysaccharide\u2010stimulated rat air pouch was inhibited with an ID<jats:sub>50<\/jats:sub> value of 0.24\u2003mg\u2003kg<jats:sup>\u22121<\/jats:sup>.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Efficacy of lumiracoxib in rat models of hyperalgesia, oedema, pyresis and arthritis was dose\u2010dependent and similar to diclofenac. However, consistent with its low COX\u20101 inhibitory activity, lumiracoxib at a dose of 100\u2003mg\u2003kg<jats:sup>\u22121<\/jats:sup> orally caused no ulcers and was significantly less ulcerogenic than diclofenac (<jats:italic>P<\/jats:italic>&lt;0.05).<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Lumiracoxib is a highly selective COX\u20102 inhibitor with anti\u2010inflammatory, analgesic and antipyretic activities comparable with diclofenac, the reference NSAID, but with much improved gastrointestinal safety.<\/jats:p><\/jats:list-item>\n<\/jats:list>\n<\/jats:p><jats:p><jats:italic>British Journal of Pharmacology<\/jats:italic> (2005) <jats:bold>144<\/jats:bold>, 538\u2013550. doi:<jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" ext-link-type=\"doi\" xlink:href=\"10.1038\/sj.bjp.0706078\">10.1038\/sj.bjp.0706078<\/jats:ext-link><\/jats:p>","DOI":"10.1038\/sj.bjp.0706078","type":"journal-article","created":{"date-parts":[[2005,1,17]],"date-time":"2005-01-17T18:25:43Z","timestamp":1105986343000},"page":"538-550","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":90,"title":["Preclinical pharmacology of lumiracoxib: a novel selective inhibitor of cyclooxygenase\u20102"],"prefix":"10.1111","volume":"144","author":[{"given":"Ronald","family":"Esser","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Carol","family":"Berry","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Zhengming","family":"Du","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Janet","family":"Dawson","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Alyson","family":"Fox","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Roger A","family":"Fujimoto","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"William","family":"Haston","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Earl F","family":"Kimble","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Julie","family":"Koehler","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jane","family":"Peppard","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Elizabeth","family":"Quadros","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Joseph","family":"Quintavalla","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Karen","family":"Toscano","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Laszlo","family":"Urban","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"John","family":"van Duzer","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xiaoli","family":"Zhang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Siyuan","family":"Zhou","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Paul J","family":"Marshall","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2009,1,29]]},"reference":[{"key":"e_1_2_7_2_1","unstructured":"ABBOTT LABORATORIES LIMITED(2002). 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