Developing inhaled drugs for respiratory diseases: A medicinal chemistry perspective

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.

Keywords: Asthma; Bronchodilators; COPD; DPI; Design; Inhaled; Lung; Lung retention; Medicinal chemistry; Respiratory.

Publication types

  • Review

MeSH terms

  • Administration, Inhalation
  • Aerosols / pharmacology*
  • Chemistry, Pharmaceutical / methods
  • Chemistry, Pharmaceutical / trends
  • Drug Delivery Systems* / instrumentation
  • Drug Delivery Systems* / methods
  • Humans
  • Respiratory System Agents / pharmacology*
  • Respiratory Tract Diseases / drug therapy*

Substances

  • Aerosols
  • Respiratory System Agents