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萘普生辛可,一种新型环氧化酶抑制性一氧化氮供体(CINOD)。

Naproxcinod, a new cyclooxygenase-inhibiting nitric oxide donator (CINOD).

机构信息

University Hasselt, University Hospital, The Netherlands.

出版信息

Expert Opin Biol Ther. 2009 May;9(5):649-57. doi: 10.1517/14712590902926071.

Abstract

BACKGROUND

COX-inhibiting nitric oxide donators (CINODs) are a new class of drugs that combine the actions of the parent COX inhibitor with nitric oxide (NO), with the aim of reducing potential toxicity of the parent drug, while maintaining its analgesic and anti-inflammatory effects. AZD3582 (Naproxcinod) is the first in the class of CINODs.

OBJECTIVE/METHODS: To review the effects of NO donation, CINODS in general and naproxen in osteoarthritis (OA), based on literature in PubMed.

RESULTS

In preclinical and human studies, this drug produced similar analgesic and anti-inflammatory effects to its parent naproxen, with improved gastrointestinal safety in OA patients. The results of recent clinical trials, which were designed to study effects on blood pressure, are expected shortly, after peer-review.

CONCLUSIONS

As naproxen is considered the safest COX inhibitor choice from a cardiovascular perspective, AZD3582 has the potential to become a new drug treatment in patients with OA, in whom pain and function are not controlled by the use of analgesics.

摘要

背景

环氧化酶抑制性一氧化氮供体(CINODs)是一类新型药物,将母体 COX 抑制剂与一氧化氮(NO)结合,旨在降低母体药物的潜在毒性,同时保持其镇痛和抗炎作用。AZD3582(萘普生昔诺)是 CINODs 类药物中的首个药物。

目的/方法:根据 PubMed 中的文献,综述 NO 供体、一般 CINODs 和萘普生昔诺在骨关节炎(OA)中的作用。

结果

在临床前和人体研究中,该药物在 OA 患者中产生了与母体萘普生相似的镇痛和抗炎作用,胃肠道安全性得到改善。旨在研究对血压影响的最近临床试验结果预计将在同行评审后不久公布。

结论

鉴于从心血管角度考虑,萘普生被认为是 COX 抑制剂的最佳选择,因此 AZD3582 有可能成为 OA 患者的新药治疗方法,对于那些使用镇痛药无法控制疼痛和功能的患者尤其适用。

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