Celecoxib pathways: Pharmacokinetics and pharmacodynamics

摘要

Gelecoxib is a nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgestic, and antipyretic properties. It is approved for the treatment of osteoarthritis, rheumatoid arthritis, ankylosing spondy-litis, and acute pain [1-3]. Gelecoxib has also shown promise in prevention of cancer, and has been used as an adjunct to surgery to reduce the number of adenomatous colorectal polyps in patients with the hereditary colon cancer susceptibility syndrome, familial adenomatous polyposis (FAP) [4-6]. The anti-inflammatory and pain-relieving properties of celecoxib result from inhibition of prostaglandin (PG) synthesis by selective inhibition of PG G/H synthase-2 (encoded by gene PTGS2). The two PTGS isoforms, PTGS1 and PTGS2, are bisfunctional enzymes with both cyclooxygenase (COX) and hydro-peroxidase activities, but they are commonly referred to as COX; see ('Pharmacodynamics' section) [1,7,8].