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Celecoxib, sold under the brand name Celebrex among others, is a COX-2 inhibitor and nonsteroidal anti-inflammatory drug (NSAID). [7] It is used to treat the pain and inflammation in osteoarthritis, acute pain in adults, rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, painful menstruation, and juvenile rheumatoid arthritis. [7]
COX-2 can act as an anti-tumor enzyme, but only in specific cases. [13] The FDA has approved Celebrex for treatment of familial adenomatous polyposis (FAP). [14] COX-2 inhibitors are currently being studied in breast cancer [15] and appear to be beneficial. [16]
[5] [6] It took less than eight years to develop and market the first COX-2 inhibitor, with Celebrex launched in December 1998 and Vioxx launched in May 1999. [7] [8] Celecoxib and other COX-2 selective inhibitors, valdecoxib, parecoxib, and mavacoxib, were discovered by a team at the Searle division of Monsanto led by John Talley.
COX-2 is an enzyme facultatively expressed in inflammation, and it is inhibition of COX-2 that produces the desirable effects of NSAIDs. [125] When nonselective COX-1/COX-2 inhibitors (such as aspirin, ibuprofen, and naproxen) lower stomach prostaglandin levels, ulcers of the stomach or duodenum and internal bleeding can result. [126]
Prostaglandin inhibitors are drugs that inhibit the synthesis of prostaglandin in human body. [1] There are various types of prostaglandins responsible for different physiological reactions such as maintaining the blood flow in stomach and kidney, regulating the contraction of involuntary muscles and blood vessels, and act as a mediator of inflammation and pain.
Rofecoxib is a selective COX-2 inhibitor, or "coxib". Though the class of coxibs includes several agents, degrees of COX-2 selectivity vary among them, with celecoxib (Celebrex) being the least COX-2 selective, and rofecoxib (Vioxx), valdecoxib (Bextra), and etoricoxib (Arcoxia), being highly COX-2 selective. [10]
Cyclooxygenase-2 (COX-2), also known as prostaglandin-endoperoxide synthase 2 (HUGO PTGS2), is an enzyme that in humans is encoded by the PTGS2 gene. [5] In humans it is one of three cyclooxygenases. It is involved in the conversion of arachidonic acid to prostaglandin H 2, an important precursor of prostacyclin, which is expressed in inflammation.
Daniel L. Simmons is a professor of chemistry and former director of the Cancer Research Center at Brigham Young University (BYU). He was the discoverer of the COX-2 enzyme that is the target of celecoxib (Celebrex) and other COX-2 inhibitors.