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环氧化酶和5-脂氧合酶双重抑制剂利考昔酮是抗炎治疗中一种有前景的替代药物吗?

Is licofelone, a dual inhibitor of cyclo-oxygenase and 5-lipoxygenase, a promising alternative in anti-inflammatory therapy?

作者信息

Bannwarth Bernard

机构信息

Service de Rhumatologie, Groupe hospitalier Pellegrin & Laboratoire de Thérapeutique, EA 525, Université Victor Segalen, Bordeaux, France.

出版信息

Fundam Clin Pharmacol. 2004 Feb;18(1):125-30. doi: 10.1046/j.1472-8206.2003.00217.x.

Abstract

As prostaglandins and leukotrienes are critical in inflammation, dual cyclo-oxygenase and 5-lipoxygenase enzymes inhibitors, especially licofelone, are being developed by pharmaceutical companies. Experimental data indicate that licofelone shares the antipyretic, analgesic, anti-inflammatory and anti-platelet activities of conventional nonsteroidal anti-inflammatory drugs (NSAIDs), and exhibits anti-allergic properties. Although licofelone may lead to similar adverse effects on the kidney than available NSAIDs, it appeared to induce less gastrointestinal damaging effects than nonselective NSAIDs in animals. Unfortunately, preliminary clinical studies provided less impressive data with respect to efficacy. Finally, the experimental promise of licofelone as a safe and potent anti-inflammatory and analgesic agent remains to be proved in humans.

摘要

由于前列腺素和白三烯在炎症过程中起关键作用,制药公司正在研发双环氧化酶和5-脂氧合酶双重抑制剂,尤其是利考昔。实验数据表明,利考昔具有传统非甾体抗炎药(NSAIDs)的解热、镇痛、抗炎和抗血小板活性,并具有抗过敏特性。尽管利考昔对肾脏可能产生与现有NSAIDs类似的不良反应,但在动物实验中,它对胃肠道的损害作用似乎比非选择性NSAIDs小。遗憾的是,初步临床研究在疗效方面提供的数据并不那么令人印象深刻。最后,利考昔作为一种安全有效的抗炎和镇痛药的实验前景仍有待在人体中得到证实。

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