NAPROXCINOD Nonsteroidal Anti-Inflammatory Agent Cyclooxygenase-Inhibiting NO Donor

作者：Fiorucci S^*

来源：Drugs of the Future, 2009, 34(7): 537-543.

DOI：10.1358/dof.2009.34.7.1391338

• Naproxen nitroxybutyl ester
• Nitronaproxen
• NO-naproxen
• AR-P900758XX (former code name)
• AZ-3582 (former code name)
• HCT-3012 (former code name)
• ZD-3582 (former code name)

Naproxcinod (naproxen nitroxybutyl ester, nitronaproxen, NO-naproxen) is a nitric oxide (NO) derivative of the nonsteroidal anti-inflammatory drug (NSAID) naproxen. Naproxcinod is the first of a class of NSAIDs known as cyclooxygenase (COX)-inhibiting NO donors (CINODs), and is currently in phase III clinical development for the treatment of osteoarthritis. Preclinical studies have demonstrated that naproxcinod causes less gastric injury than naproxen, although it exerts similar anti-inflammatory and analgesic activity. Phase II and III trials have shown that naproxcinod is on effective analgesic agent with reduced gastrointestinal toxicity in comparison with naproxen. In contrast to noproxen, naproxcinod reduces systemic blood pressure by 2-3 mmHg. Because it seems prudent to avoid the use of selective COX-2 inhibitors in patients who have or are at risk for cardiovascular disease, naproxcinod represents an alternative to coxibs and traditional NSAIDs in such patients. However, because naproxcinod still increases the risk of gastrointestinal ulcers, comedication with a proton pump inhibitor will be required if patients also present risk factors for gastrointestinal events.

• 出版日期2009-7