Valdecoxib (SC 65872) is a prescription drug used in the treatment of osteoarthritis, rheumatoid arthritis, and painful menstruation and menstrual symptoms. It is classified as a nonsteroidal anti-inflammatory drug, or NSAID, and should not be taken by anyone allergic to these types of medications.

COX-2:5 nM

Valdecoxib在急慢性炎症大鼠模型中效果显著,气囊炎、足肿胀和非特异性关节炎ED50分别为0.06 mg/kg、5.9 mg/kg和0.03 mg/kg. Valdecoxib单独在体内吸收较慢,在3小时后,最大抑制16%的水肿.相反,VALD-βCd 和VALD-SBE7βCd复合物在体内具有高吸收率,在1小时内能够抑制超过50%的水肿,3小时后,抑制水肿的最大百分比为66%.Valdecoxib口服给药抑制大鼠角叉菜胶脚垫水肿,ED50=10.2 mg/kg.在大鼠非特异性关节炎模型中,口服给药Valdecoxib具有慢性抗炎活性,ED50=0.032 mg/kg/天.患有角叉菜胶气囊炎的大鼠口服给药Valdecoxib能够阻滞炎症部位前列腺素的产生,ED50=0.02 mg/kg.

Valdecoxib抑制脂多糖诱导的血浆中PGE2产生（IC50：0.89 μM）,抑制血浆中TxB2产生（IC50：25.4 μM）。Valdecoxib与COX-2结合,Ka为1.1×105 M/s。Valdecoxib对COX-2的总体的饱和结合亲和力为2.6 nM。Valdecoxib在15分钟(DP15)时溶解的百分比为10.5%,其亲水性衍生物(VALD-βCd,VALD-HPβCd和VALD-SBE7βCd 复合物)溶解百分比分别为50%,91%和 93%。