Nabumetone

Nabumetone is an orally active non-acidic anti-inflammatory agent, acts as a potent and selective COX-2 inhibitor, and is the prodrug of the active metabolite 6MNA. IC50 & Target: COX-2^[1] In Vitro: Nabumetone is a potent and selective COX-2 inhibitor. Nabumetone (50 μmol-2 mmol) dose-dependently inhibits the proliferation of K-562 and Meg-01 cells, but shows no obvious apoptotic effect. Nabumetone potentiates the apoptotic effect of ADR in the K-562 cell line. Moreover, Nabumetone reduces Bcl-2 expression^[1]. In Vivo: Nabumetone (79 mg/kg, p.o.) inhibits paw oedema and paw exudate PGE₂ in rats. Nabumetone does not induce gastric damage and causes only 57% inhibition of gastric mucosal 6-keto-PGF_1α production in rats^[2]. Nabumetone (25, 50, 100 mg/kg, i.p.) dose-dependently inhibits the increase of DDC-induced mucus secretion and stimulates stress-induced mucus secretion in rats. Nabumetone (25 mg/kg, i.p.) significantly suppresses stress-induced ulcer index in rats^[3].