LUMIRACOXIB

Biochem/physiol Actions

Lumiracoxib (COX189) is an orally active, potent and selective cyclooxygenase-2 inhibitor (K_i = 60 nM/COX-2 vs. 3.2 µM/COX-1) that inhibits COX-2-mediated PGE2 production in human whole blood (IC₅₀ = 130 nM; stimulation = 50 µM A23187), but not COX-1-dependent TxB2 production (IC₅₀ = 67 µM; stimulation = 10 µg/mL LPS). Lumiracoxib shows in vivo anti-inflammatory efficacy against carrageenan-induced paw oedema (ED₃₀ = 0.35 mg/kg p.o.), CFA-induced hyperalgesia (ED₃₀ = 5.1 mg/kg p.o.), as well as adjuvant-induced arthritis (ED₅₀ = 3 mg/kg/day p.o.) in rats in vivo.