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 demonstrates significant efficacy in acute and chronic inflammation models in rats, with ED50 values of 0.06 mg/kg for carrageenan air-pouch inflammation, 5.9 mg/kg for paw edema, and 0.03 mg/kg for nonspecific arthritis. When administered alone, valdecoxib shows slow absorption in vivo, achieving a maximum inhibition of 16% in edema at 3 hours post-administration. In contrast, the valdecoxib complexes VALD-βCd and VALD-SBE7βCd exhibit high absorption rates, suppressing over 50% of edema within 1 hour, and achieving a maximum inhibition of 66% at 3 hours. Orally administered valdecoxib inhibits carrageenan-induced rat paw edema with an ED50 value of 10.2 mg/kg. In a rat model of nonspecific arthritis, oral valdecoxib shows chronic anti-inflammatory activity, with an ED50 of 0.032 mg/kg/day. Valdecoxib also inhibits prostaglandin production at the inflammation site in rats with carrageenan air-pouch inflammation when administered orally, with an ED50 value of 0.02 mg/kg.

Valdecoxib inhibits the production of PGE2 in plasma induced by lipopolysaccharides (IC50: 0.89 μM) and suppresses the generation of TxB2 in plasma (IC50: 25.4 μM). It binds to COX-2 with a Ka of 1.1×10^5 M/s and exhibits a strong overall saturable binding affinity to COX-2 of 2.6 nM. After 15 minutes (DP15), valdecoxib has a solubility percentage of 10.5%, while its hydrophilic derivatives (VALD-βCd, VALD-HPβCd, and VALD-SBE7βCd complexes) display significantly increased solubility percentages of 50%, 91%, and 93%, respectively.