Therapeutic potential for novel ultra long-acting β2-agonists in the management of COPD: biological and pharmacological aspects

Chronic obstructive pulmonary disease (COPD) is characterised by progressive airflow limitation. In moderate-to-severe COPD, long-acting bronchodilators are the basis of therapy. Inhaled long-acting β2-agonists (LABAs) are used for the treatment of COPD. LABAs have been in use since the 1990s enabling persistent bronchodilation for 12 hours; however, sustained bronchodilation is desirable. Compared with twice-daily LABAs, new LABAs with ultra-long duration (ultra-LABAs) could provide improvements in efficacy and compliance with fast onset of action, 24-hour bronchodilation and a good safety profile. Several novel ultra-LABAs showing once-daily delivery profiles are in development. In this article, we discuss these novel agents’ properties and clinical trials of their efficacy and safety, including the only licensed ultra-LABA, indacaterol.