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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.

DOI:10.1046/j.1472-8206.2003.00217.x
PMID:14748764
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。

相似文献

1
Is licofelone, a dual inhibitor of cyclo-oxygenase and 5-lipoxygenase, a promising alternative in anti-inflammatory therapy?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?
Fundam Clin Pharmacol. 2004 Feb;18(1):125-30. doi: 10.1046/j.1472-8206.2003.00217.x.
2
The metabolic effects of inhibitors of 5-lipoxygenase and of cyclooxygenase 1 and 2 are an advancement in the efficacy and safety of anti-inflammatory therapy.5-脂氧合酶以及环氧化酶1和2抑制剂的代谢效应是抗炎治疗在疗效和安全性方面的一项进展。
Prostaglandins Other Lipid Mediat. 2003 Jul;71(3-4):147-62. doi: 10.1016/s1098-8823(03)00039-x.
3
Activity and potential role of licofelone in the management of osteoarthritis.利考昔在骨关节炎治疗中的活性及潜在作用。
Clin Interv Aging. 2007;2(1):73-9. doi: 10.2147/ciia.2007.2.1.73.
4
Licofelone, a dual lipoxygenase-cyclooxygenase inhibitor, downregulates polymorphonuclear leukocyte and platelet function.利考非隆,一种双脂氧合酶 - 环氧化酶抑制剂,可下调多形核白细胞和血小板功能。
Eur J Pharmacol. 2002 Oct 18;453(1):131-9. doi: 10.1016/s0014-2999(02)02385-3.
5
Licofelone--clinical update on a novel LOX/COX inhibitor for the treatment of osteoarthritis.利考非洛酮——一种用于治疗骨关节炎的新型脂氧合酶/环氧化酶抑制剂的临床进展
Rheumatology (Oxford). 2004 Feb;43 Suppl 1:i21-5. doi: 10.1093/rheumatology/keh105.
6
Dual inhibition of cyclo-oxygenases and 5-lipoxygenase: a novel therapeutic approach to inflammation?环氧化酶和5-脂氧合酶的双重抑制:一种治疗炎症的新方法?
Joint Bone Spine. 2005 May;72(3):199-201. doi: 10.1016/j.jbspin.2004.04.008.
7
The protective effect of licofelone on experimental osteoarthritis is correlated with the downregulation of gene expression and protein synthesis of several major cartilage catabolic factors: MMP-13, cathepsin K and aggrecanases.利考非隆对实验性骨关节炎的保护作用与几种主要软骨分解代谢因子(基质金属蛋白酶-13、组织蛋白酶K和聚糖酶)的基因表达下调及蛋白质合成减少有关。
Arthritis Res Ther. 2005;7(5):R1091-102. doi: 10.1186/ar1788. Epub 2005 Jul 19.
8
Dual acting anti-inflammatory drugs: a reappraisal.双效抗炎药物:重新评估
Pharmacol Res. 2001 Dec;44(6):437-50. doi: 10.1006/phrs.2001.0872.
9
Licofelone (Merckle).利考非隆(默克勒公司)
IDrugs. 2003 Aug;6(8):802-8.
10
Licofelone--a novel analgesic and anti-inflammatory agent.利考非洛——一种新型镇痛抗炎药。
Curr Top Med Chem. 2007;7(3):251-63. doi: 10.2174/156802607779941305.

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