Valdecoxib

Valdecoxib was removed from the Canadian, U.S., and E.U. markets in 2005 due to concerns about possible increased risk of heart attack and stroke. (In Vitro) :Valdecoxib (Compound 2) is a highly potent, selective and orally active inhibitor of COX-2, with IC50s of 5 nM and 140 μM for COX-2 and COX-1, respeceively. Valdecoxib (10, 100 μM) inhibits LPS-induced proliferation of endothelial cells and bFGF secretion in a dose-dependent manner. Valdecoxib stimulates VEGF formation via HMEC-1 under inflammatory conditions. (In Vivo) :Valdecoxib (Compound 2) shows potent oral activity in an acute antiinflammatory assay (rat carrageenan foot pad edema; ED50 = 10.2 ± 1.4 mg/kg) . Valdecoxib also has chronic antiinflammatory activity in the rat adjuvant arthritis model, with an ED50 of 0.032 ± 0.002 mg/kg/day. Valdecoxib (10 mg/kg, i.p.) significantly attenuates the behavioral and biochemical (oxidative damage) alterations in chronic-stressed mice.