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Current approaches to the discovery of novel inhaled medicines
Drug Discovery Today ( IF 7.4 ) Pub Date : 2018-05-20 , DOI: 10.1016/j.drudis.2018.05.017
Peter Strong , Kazuhiro Ito , John Murray , Garth Rapeport

Inhaled administration is underutilised because the drug discovery process is viewed as challenging, risky, and expensive. However, unmet medical need continues to grow, and significant opportunities exist to discover novel inhaled medicines delivering the required lung concentrations while minimising systemic exposure. This profile could be achieved by a combination of properties, including lung retention and low oral bioavailability. Property-based rules exist for orally administered compounds, but there has been limited progress defining in silico predictors to guide the discovery of novel inhaled drugs. Recently, the use of informative cell- and tissue-based screens has greatly facilitated the identification of compounds with optimal characteristics for inhaled delivery. Here, we address opportunities for novel inhaled drugs, and the key challenges and uncertainties hampering progress.



中文翻译:

发现新型吸入药物的当前方法

由于药物发现过程被认为具有挑战性,风险性和昂贵性,因此吸入管理未得到充分利用。然而,未满足的医疗需求继续增长,并且存在巨大的机会来发现能够提供所需的肺部浓度同时最大程度地减少全身暴露的新型吸入药物。该特性可以通过多种特性的组合来实现,包括肺部保留和口服生物利用度低。口服给药的化合物存在基于属性的规则,但计算机定义的进展有限预测器,以指导新型吸入药物的发现。近来,基于信息的基于细胞和组织的筛查的使用极大地促进了具有最佳特性的化合物的吸入输送的鉴定。在这里,我们探讨了新型吸入药物的机遇,以及阻碍进步的主要挑战和不确定性。

更新日期:2018-05-20
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