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Targeting selectivity for COX-2 reduces the risk of peptic ulceration and is the main feature of celecoxib, rofecoxib, and other members of this drug class. [1] After several COX-2–inhibiting drugs were approved for marketing, data from clinical trials revealed that COX-2 inhibitors caused a significant increase in heart attacks and strokes ...
The importance of developing such drugs was increased when COX-2-specific NSAIDs rofecoxib (Vioxx) and lumiracoxib (Prexige) were removed from major pharmaceutical markets in the mid-2000s due to vascular safety concerns. In addition, traditional NSAIDs increase blood pressure and interfere with the actions of antihypertensive drugs.
DuP-697 was a building-block for synthesis of COX-2 inhibitors and served as the basic chemical model for the coxibs that are the only selective COX-2 inhibitors on the market today. DuP-697 is a diaryl heterocycle with cis-stilbene moiety. Structure activity relationship (SAR) studies for diaryl heterocyclic compounds have indicated that a cis ...
5743 19225 Ensembl ENSG00000073756 ENSMUSG00000032487 UniProt P35354 Q05769 RefSeq (mRNA) NM_000963 NM_011198 RefSeq (protein) NP_000954 NP_035328 Location (UCSC) Chr 1: 186.67 – 186.68 Mb Chr 1: 149.98 – 149.98 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse Cyclooxygenase-2 (COX-2), also known as prostaglandin-endoperoxide synthase 2 (HUGO PTGS2), is an enzyme that in humans is ...
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]
Pages in category "COX-2 inhibitors" The following 24 pages are in this category, out of 24 total. This list may not reflect recent changes. * Cyclooxygenase-2 ...
Lumiracoxib is a COX-2 selective inhibitor nonsteroidal anti-inflammatory drug.. Its structure is different from that of other COX-2 inhibitors, such as celecoxib: lumiracoxib is an analogue of diclofenac (one chlorine substituted by fluorine, the phenylacetic acid has another methyl group in meta position), making it a member of the arylalkanoic acid class of NSAIDs; it binds to a different ...
Corticosteroids inhibit phospholipase A 2 production by boosting production of lipocortin, an inhibitor protein. Relatively new NSAIDs, known as COX-2 selective inhibitors or coxibs, are used as specific inhibitors of the COX-2 isoform of cyclooxygenase. The development of these drugs allowed the circumvention of the negative gastrointestinal ...