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开发治疗呼吸疾病的吸入式药物:从药物化学角度来看。

Developing inhaled drugs for respiratory diseases: A medicinal chemistry perspective.

机构信息

Charles River Laboratories, 8-9 Spire Green Centre, Harlow CM19 5TR, UK.

Charles River Laboratories, 8-9 Spire Green Centre, Harlow CM19 5TR, UK; Charles River Laboratories, Chesterford Research Park, Saffron Waldon CB10 1XL, UK.

出版信息

Drug Discov Today. 2022 Jan;27(1):134-150. doi: 10.1016/j.drudis.2021.09.005. Epub 2021 Sep 20.

Abstract

Despite the devastating impact of many lung diseases on human health, there is still a significant unmet medical need in respiratory diseases, for which inhaled delivery represents a crucial strategy. More guidance on how to design and carry out multidisciplinary inhaled projects is needed. When designing inhaled drugs, the medicinal chemist must carefully balance the physicochemical properties of the molecule to achieve optimal target engagement in the lung. Although the medicinal chemistry strategy is unique for each project, and will change depending on multiple factors, such as the disease, target, systemic risk, delivery device, and formulation, general guidelines aiding inhaled drug design can be applied and are summarised in this review.

摘要

尽管许多肺部疾病对人类健康造成了毁灭性的影响,但在呼吸系统疾病方面仍存在着巨大的未满足的医疗需求,吸入式给药是一种至关重要的策略。需要更多关于如何设计和开展多学科吸入式项目的指导。在设计吸入式药物时,药物化学家必须仔细平衡分子的物理化学性质,以实现肺部的最佳靶标结合。尽管每个项目的药物化学策略都是独特的,并会因疾病、靶标、系统风险、给药装置和制剂等多种因素而改变,但有助于吸入式药物设计的一般指南可以应用,并在本综述中进行了总结。

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