Abstract
Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used drugs but their use is hampered by gastrointestinal side effects. Cyclo-oxygenase Inhibitor Nitric Oxide Donors (CINODs) are a new class of antiinflammatory and analgesic drugs generated by adding a nitric oxide generating moiety to the parent NSAID via an ester linkage. The combination of balanced inhibition of the two main COX isoforms with release of NO confers to CINODs a reduced gastrointestinal toxicity and a potent anti-inflammatory activity. It is suggested that the NO, which is released by the metabolism of nitrate as the compounds are broken down, may counteract the consequences of the NSAID-induced decrease in gastric mucosal prostaglandins. Recent clinical trials with CINODs (previously termed NO-NSAIDs) have provided data consistent with pre-clinical observations
Keywords: NSAID, cyclooxygenase 2, Nitric oxide, NCX-4016, gastrointestinal injury, immunomodulatory
Current Topics in Medicinal Chemistry
Title: Cyclo-Oxygenase (COX) Inhibiting Nitric Oxide Donating (CINODs) Drugs: A Review of Their Current Status
Volume: 7 Issue: 3
Author(s): Fiorucci Stefano and Eleonora Distrutti
Affiliation:
Keywords: NSAID, cyclooxygenase 2, Nitric oxide, NCX-4016, gastrointestinal injury, immunomodulatory
Abstract: Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used drugs but their use is hampered by gastrointestinal side effects. Cyclo-oxygenase Inhibitor Nitric Oxide Donors (CINODs) are a new class of antiinflammatory and analgesic drugs generated by adding a nitric oxide generating moiety to the parent NSAID via an ester linkage. The combination of balanced inhibition of the two main COX isoforms with release of NO confers to CINODs a reduced gastrointestinal toxicity and a potent anti-inflammatory activity. It is suggested that the NO, which is released by the metabolism of nitrate as the compounds are broken down, may counteract the consequences of the NSAID-induced decrease in gastric mucosal prostaglandins. Recent clinical trials with CINODs (previously termed NO-NSAIDs) have provided data consistent with pre-clinical observations
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Stefano Fiorucci and Distrutti Eleonora, Cyclo-Oxygenase (COX) Inhibiting Nitric Oxide Donating (CINODs) Drugs: A Review of Their Current Status, Current Topics in Medicinal Chemistry 2007; 7 (3) . https://dx.doi.org/10.2174/156802607779941350
DOI https://dx.doi.org/10.2174/156802607779941350 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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