Asthma has been recognised as a respiratory disorder for millennia and the focus of targeted drug development for the last 120 years. Asthma is one of the most common chronic non-communicable diseases worldwide. Chronic obstructive pulmonary disease (COPD), a leading cause of morbidity and mortality worldwide, is caused by exposure to tobacco smoke and other noxious particles and exerts a substantial economic and social burden. This chapter reviews the development of the treatments of asthma and COPD particularly focussing on the β-agonists, from the isolation of adrenaline, through the development of generations of short- and long-acting β-agonists. It reviews asthma death epidemics, considers the intrinsic efficacy of clinical compounds, and charts the improvement in selectivity and duration of action that has led to our current medications. Important β2-agonist compounds no longer used are considered, including some with additional properties, and how the different pharmacological properties of current β2-agonists underpin their different places in treatment guidelines. Finally, it concludes with a look forward to future developments that could improve the β-agonists still further, including extending their availability to areas of the world with less readily accessible healthcare.
© 2023. The Author(s), under exclusive license to Springer Nature Switzerland AG.