NO-NSAIDs: From Inflammatory Mediators to Clinical Readouts

Author(s): Stefano Fiorucci, Elisabetta Antonelli.

Journal Name: Inflammation & Allergy - Drug Targets (Discontinued)
(Formerly Current Drug Targets - Inflammation & Allergy)

Volume 5 , Issue 2 , 2006


Non-steroidal anti-inflammatory drugs (NSAIDs) and cyclo-oxygenase (COX)-2 selective inhibitors (COXIBs) are widely used drugs. However, their use is hampered by gastrointestinal, cardiovascular and renal side effects. Nitric oxide (NO)-releasing NSAIDs, NO-NSAID, are a new class of anti-inflammatory and analgesic drugs generated by adding a nitroxybutyl or a nitrosothiol moiety to the parent NSAID via a short-chain ester linkage. While efficacy of nitrosothiol-NSAIDs still awaits investigation, nitroxybutyl-NO-NSAIDs have been extensively studied in humans. The combination of balanced inhibition of the two main COX isoforms with release of NO confers to NO-NSAIDs reduced gastrointestinal and cardiorenal toxicity. It is suggested that the NO, which is released as the compounds are broken down, may counteract the consequences of the NSAID-induced decrease in gastric mucosal prostaglandins. Recent clinical trials with NO-NSAIDs have provided data consistent with pre-clinical observations.

Keywords: COX-2 selective inhibitors, nitric oxide (NO), rheumatoid arthritis (RA), interferon-gamma, cytokine, immunomodulatory, coagulation network

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Article Details

Year: 2006
Page: [121 - 131]
Pages: 11
DOI: 10.2174/187152806776383161
Price: $58

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