Etoricoxib is a highly selective COX-2 inhibitor (coxib) approved in Europe for the treatment of osteoarthritis (OA), rheumatoid arthritis and acute gouty arthritis. Etoricoxib is an effective analgesic drug that has shown some improved efficacy versus traditional NSAIDs and it is the only coxib approved for the treatment of acute gouty arthritis. Moreover, recent studies evidence its efficacy in patients with ankylosing spondylitis. In the Etoricoxib Diclofenac Gastrointestinal Evaluation study performed in patients with OA, etoricoxib significantly reduced the rate of discontinuation by 50% due to gastrointestinal adverse events versus diclofenac. Comparable rates of thrombotic cardiovascular events were detected. Rates of discontinuation due to hypertension-related adverse effects were higher on etoricoxib than diclofenac. Similarly to other selective COX-2 inhibitors, etoricoxib is contraindicated in patients with ischaemic heart disease or stroke and it should be used with caution in patients with risk factors for heart disease. The European Medicines Agency has contraindicated the use of etoricoxib in patients with uncontrolled hypertension. Selective COX-2 inhibitors remain an appropriate choice in patients at low cardiovascular risk, but with increased risk of gastrointestinal complications.
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http://dx.doi.org/10.1517/17425255.1.2.269 | DOI Listing |
Bioorg Chem
January 2025
Department of Radiology, the Affiliated Hospital of Southwest Medical University, Luzhou 646000 China; Precision Imaging and Intelligent Analysis Key Laboratory of Luzhou City, Luzhou 646000 China. Electronic address:
Hypochlorite anion (ClO) is closely associated with cancer development and progression, necessitating precise monitoring of ClO in tumor sites, and Cyclooxygenase-2 (COX-2 is highly expressed in tumor cells. So we rationally designed two ClO-specific responsive fluorescent probes COX2-ClO1 and COX2-ClO2, using indomethacin (IMC) as the COX-2 targeting moiety and methylene blue as fluorophore unit. Both probes exhibited high selectivity and sensitivity towards ClO in the in vitro solution assays and possess excellent biocompatibility in cellular experiments.
View Article and Find Full Text PDFEur J Med Chem
January 2025
School of Life Sciences and Medicine, Shandong University of Technology, Zibo, 255049, PR China. Electronic address:
A library comprising twenty-four isosteric derivatives of celecoxib substituted with carboxylic acid (labeled as 5a-5x), was synthesized and characterized through H NMR, C NMR, HRMS, and elemental analysis. Molecular docking studies revealed that all compounds successfully docked into the binding pocket of COX-2, and the introduction of carboxyl group enhances the interaction between the derivatives and COX-2. The compounds were further evaluated for cell toxicity, and in vitro anti-inflammatory activity.
View Article and Find Full Text PDFJ Nucl Med
January 2025
Intramural Research Program, National Institute of Mental Health, Bethesda, Maryland;
Cyclooxygenase-2 (COX-2) is present in a healthy brain at low densities but can be markedly upregulated by excitatory input and by inflammogens. This study evaluated the sensitivity of the PET radioligand [C]-6-methoxy-2-(4-(methylsulfonyl)phenyl)--(thiophen-2-ylmethyl)pyrimidin-4-amine ([C]MC1) to detect COX-2 density in a healthy human brain. The specificity of [C]MC1 was confirmed using lipopolysaccharide-injected rats and transgenic mice expressing the human gene, with 120-min baseline and blocked scans using COX-1 and COX-2 selective agents.
View Article and Find Full Text PDFFront Pharmacol
January 2025
Lab of Hepatopharmacology and Ethnopharmacology, School of Pharmaceutical Sciences, South-Central Minzu University, Wuhan, China.
Background: (Lour.) Merr. is a plant used in traditional Chinese medicine that reduces hepatotoxicity, relieves kidney discomfort, and has anti-inflammatory and antioxidant properties.
View Article and Find Full Text PDFAm J Med Genet A
January 2025
Division of Human Genetics, Cincinnati Children's Hospital Medical Center, Cincinnati, Ohio, USA.
Primary Hypertrophic Osteoarthropathy (PHOAR1) is characterized by autosomal recessive loss of function variants in 15-hydroxyprostaglandin dehydrogenase (HPGD) leading to digital clubbing, periostosis, pachydermia, and severe hyperhidrosis. HPGD catalyzes the first step of prostaglandin E2 (PGE2) degradation. Selective COX-2 inhibitors have proved beneficial in adults, though it is unknown if early initiation of COX-2 inhibitors can alter the natural history of PHOAR1.
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