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Nitroflurbiprofen NicOx SA.

X Wang1

  • 1Cornell University Medical College, 450 East 63rd Street, Rm 7G, New York, NY 10021, USA. sw001@yahoo.com

Idrugs : the Investigational Drugs Journal
|May 10, 2008
PubMed
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See all related articles

Nitroflurbiprofen, a novel nitric oxide-releasing non-steroidal anti-inflammatory drug (NSAID), demonstrates excellent tolerability and reduced gastrointestinal damage compared to traditional NSAIDs. It shows potent and long-lasting effects in early clinical trials.

Area of Science:

  • Pharmacology
  • Gastroenterology
  • Drug Development

Background:

  • Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used for pain and inflammation but are associated with gastrointestinal (GI) side effects.
  • Nitroflurbiprofen (HCT-1026) is a novel NSAID developed by NicOx, designed to release nitric oxide (NO).
  • Nitric oxide release may mitigate the GI toxicity associated with conventional NSAIDs.

Purpose of the Study:

  • To evaluate the safety, tolerability, and efficacy of nitroflurbiprofen.
  • To compare the GI safety profile of nitroflurbiprofen with conventional flurbiprofen.
  • To investigate the pharmacological mechanisms of nitroflurbiprofen, including its NO-releasing properties.

Main Methods:

  • Phase I clinical trials in healthy volunteers.

Related Experiment Videos

  • Single and repeated dose oral administration of nitroflurbiprofen.
  • Endoscopic studies to assess gastrointestinal damage.
  • Pharmacokinetic and pharmacodynamic assessments, including serum thromboxane inhibition.
  • In vitro studies on endothelial cells and inducible nitric oxide synthase expression.

    • Main Results:

    • Nitroflurbiprofen exhibited excellent tolerability and potent, long-lasting serum thromboxane inhibition in healthy volunteers.
    • Repeated dose endoscopic studies indicated less gastrointestinal damage with nitroflurbiprofen compared to flurbiprofen.
    • Preclinical studies showed nitroflurbiprofen was better tolerated than flurbiprofen in various animal models.
    • Nitroflurbiprofen releases NO, increases cGMP in endothelial cells, and inhibits inducible nitric oxide synthase and endotoxin in the GI tract.

    Conclusions:

    • Nitroflurbiprofen represents a promising NSAID with an improved gastrointestinal safety profile.
    • Its ability to release nitric oxide may be key to its enhanced tolerability.
    • Further clinical development, including phase II studies, is warranted to confirm its therapeutic potential for inflammatory conditions.