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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]
The inhibition of COX-2 is paramount for the anti-inflammatory and analgesic function of the selective COX-2 inhibitor celecoxib. However, with regard to this drug's promise for the therapy of advanced cancers, it is unclear whether the inhibition of COX-2 plays a dominant role, and this has become a controversial and intensely researched issue.
This has been studied using SC-58125 (an analogue of celecoxib) and mutated COX-2, wherein the valine 523 residue was replaced by isoleucine 523. The irreversible inhibition did not happen, but reversible inhibition was noticed. A model has been made to explain this three-step mechanism behind the inhibitory effects of selective COX-2 inhibitors.
Suzetrigine is the first new painkiller approved in the US since Celebrex, a type of nonsteroidal anti-inflammatory drug called a Cox-2 inhibitor, which was approved in 1998.
Selectivity for COX-2 is the main feature of celecoxib, etoricoxib, and other members of this drug class. Because COX-2 is usually specific to inflamed tissue, there is much less gastric irritation associated with COX-2 inhibitors, with a decreased risk of peptic ulceration.
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.
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]
Karen Seibert (c.1959 – November 9, 2020) was an American pharmacological scientist, instrumental in the elaboration of the COX-2 inflammatory pathway [1] and in the discovery of inhibitors of COX-2, such as celecoxib (Celebrex), used to relieve pain and treat arthritis. [2]