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Drug Discov Today. 2012 May;17(9-10):496-504. doi: 10.1016/j.drudis.2011.11.002. Epub 2011 Nov 18.

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

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Department of Internal Medicine, University of Brescia, 1st Divisione di Medicina, Az Spedali Civili, Pzza Spedali Civili 1, 25100 Brescia, Italy.


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 β(2)-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.

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