Лумиракоксиб

Описание

As a second-generation, selective cyclooxygenase (COX-2) inhibitor, lumiracoxib is devoid of the gastrointestinal issues that plague other non-selective, nonsteroidal, anti-inflammatory drugs (NSAIDs) that crossover to COX-1. As an inhibitor of the inducible COX-2 that is up-regulated in pathological processes of pain and inflammation, lumiracoxib blocks the conversion of arachidonic acid to prostaglandins, the mediators of the pathological effects. It’s mode of binding to COX-2 has been found to differ from the other selective COX-2 inhibitors; the carboxylic acid forms hydrogen bonds with Tyr-385 and Ser-530 in the catalytic site rather than seeking interactions within the larger hydrophobic side pocket. Since lumiracoxib is mainly metabolized by CYP2C9, a study evaluating the co-administration of lumiracoxib with fluconazole, a potent inhibitor of CYP2C9, was conducted, and it concluded that there was no need for lumiracoxib dose adjustment, since changes in the systemic exposure were not significant. No serious adverse effects were reported, but in the small number of cases where treatment was discontinued, Gastro intestinal (GI) and musculoskeletal complaints were common.

Химические свойства

Pale Yellow Solid

Использование

Lumiracoxib is a selective cyclooxygenase-2-(COX-2) inhibitor and an anti-inflammatory agent (1,2,3,4).

Определение

ChEBI: An amino acid that is phenylacetic acid which is substituted at position 2 by the nitrogen of 2-chloro-6-fluoroaniline and at position 5 by a methyl group. A highly selective cyclooxygenase 2 inhibitor, it was briefly used for the treatment of osteoarthrit s, but was withdrawn due to concersns of hepatotoxicity.