Lumiracoxib

Lumiracoxib is a potent,selective and orally active COX-2 inhibitor with a K_i value of 0.06?μM^[1]. Lumiracoxib acts as a nonselective NSAID with?anti-inflammatory, analgesic and antipyretic activities. Lumiracoxib can be used for osteoarthritis and bone cancer research^[1][2]. In Vitro: Lumiracoxib inhibits purified COX-1 and COX-2 with?K_i values of 3 μM and 0.06?μM, respectively. In cellular assays, Lumiracoxib has an IC₅₀?of 0.14?μM in COX-2-expressing dermal fibroblasts, but causesno inhibition of COX-1 at concentrations up to 30?μM in HEK293 cells transfected with human COX-1^[1].
In a human whole blood assay, IC₅₀?values for Lumiracoxib are 0.13?μM for COX-2 and 67?μM?for COX-1^[1].
In Vivo: Lumiracoxib (oral administration; 10 and 30 mg/kg; single dose) significantly reverses the established hyperalgesia with a maximal 58% reversal observed 3 h following administration in rat model^[1].
Lumiracoxib (oral administration; 10 and 30 mg/kg; twice daily; from day 10 to day 20 following MRMT-1 cell injection) significantly attenuates the weight-bearing difference observed on days 14, 17 and 20. The repeated administration significantly reverses static allodynia measured 90 min following the final administration.It significantly reduces the radiologically observed structural changes 20 days after inoculation of MRMT-1 cells in rat^[1].