Valdecoxib (SC65872)

Description: Valdecoxib (SC-65872; SC65872; SC 65872; Bextra), a nonsteroidal anti-inflammatory drug (NSAID), is a potent and selective inhibitor of COX-2 enzyme with potential anti-inflammatory activity. It inhibits COX-2 with an IC50 of 5 nM. Valdecoxib has been approved for the treatment of pain and inflammation. Valdecoxib and its intravenous prodrug parecoxib exert significant opioid-sparing effects after dental, gynecologic, orthopedic and other noncardiac surgical procedures. In the cellular assay, valdecoxib shows inhibitory activity on human recombinant COX-2 with IC50 value of 5nM. It shows no significant effect on COX-1 with IC50 value of 140uM. In the ex vivo assay using human whole blood, valdecoxib prevents PGE2 production with IC50 value of 0.89uM.

References: J Med Chem. 2000 Mar 9; 43(5):775-7; J Pharmacol Exp Ther. 2005 Mar; 312(3):1206-12.