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Targeting 5-lipoxygenase-activating protein in asthma and chronic obstructive pulmonary disease

机译:针对5-脂氧合酶激活蛋白的哮喘和慢性阻塞性肺疾病

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Introduction: In asthma and chronic obstructive pulmonary disease (COPD), there is an unmet therapeutic need for the anti-inflammatory therapies, and the identification of therapeutic targets and potent corresponding therapies is necessary. Although inhaled corticosteroids and leukotriene modifiers are most effective in asthma they are still not always capable of appropriately controlling the disease. In COPD, the therapeutic gap is even larger because inhaled corticosteroids and other anti-inflammatory therapies are not beneficial in all disease subsets. Areas covered: The role of the 5-lipoxygenase-activating protein (FLAP) in generating proinflammatory molecules such as leukotrienes is discussed, highlighting, in particular, its potential as a therapeutic target in asthma and COPD. The preclinical data on FLAP inhibitors are discussed. The clinical data on the FLAP inhibitors investigated so far for these diseases are analyzed. Expert opinion: FLAP inhibitors have emerged during the past decade as a promising therapeutic class in asthma and COPD, but there exists only a limited amount of data supporting their efficacy in these diseases. This might be due to the fact that the development of some of the molecules discussed was abandoned. Such therapies might be of particular interest in COPD and in asthma-COPD overlap syndrome.
机译:简介:在哮喘和慢性阻塞性肺疾病(COPD)中,对抗炎疗法的治疗需求尚未得到满足,因此有必要确定治疗靶点和有效的相应疗法。尽管吸入性糖皮质激素和白三烯调节剂在哮喘中最有效,但仍不能始终能够适当控制该疾病。在COPD中,治疗差距甚至更大,因为吸入皮质类固醇和其他抗炎疗法并非对所有疾病亚型都有益。涵盖的领域:讨论了5-脂氧合酶激活蛋白(FLAP)在产生促炎分子(如白三烯)中的作用,特别强调了其作为哮喘和COPD治疗靶标的潜力。讨论了FLAP抑制剂的临床前数据。到目前为止,已针对这些疾病研究了FLAP抑制剂的临床数据。专家意见:在过去的十年中,FLAP抑制剂作为哮喘和COPD的一种有前景的治疗方法出现了,但是仅有有限的数据支持其在这些疾病中的功效。这可能是由于所讨论的某些分子的开发被放弃的事实所致。此类疗法可能在COPD和哮喘-COPD重叠综合征中特别重要。

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