International Journal of COPD Open Access Full Text Article Dovepress open access to scientific and medical research R e v I e w Long-acting β-adrenoceptor agonists in the management of COPD: focus on indacaterol Jutta Beier Kai M Beeh insaf Respiratory Research Institute, wiesbaden, Germany Correspondence: Kai Michael Beeh insaf Respiratory Research Institute, Biebricher Allee 34, D-65187 wiesbaden, Germany Tel +49 611 985 4410 Fax +49 611 985 4348 email k.beeh@insaf-wi.de submit your manuscript | www.dovepress.com Dovepress DOI: 10.2147/COPD.S7371 Abstract: Bronchodilators are the cornerstone of severe chronic obstructive pulmonary disease (COPD) treatment to improve airflow, symptoms, exercise tolerance, and exacerbations. There is convincing evidence that regular treatment with long-acting bronchodilators is more effective and convenient than treatment with short-acting bronchodilators. Long-acting β-2-agonists include the twice-daily drugs formoterol and salmeterol and, more recently, once-daily indacaterol. Studies with head-to-head comparisons of long-acting bronchodilators are scant, but novel data from controlled trials with the once-daily β(2)-agonist indacaterol indicate superior bronchodi- lation and clinical efficacy of indacaterol at recommended doses over twice-daily long-acting β(2)-agonists, and at least equipotent bronchodilation compared with once-daily tiotropium. The recent therapeutic developments in COPD underscore a shift from short-acting bronchodilators with multiple dosings per day to reduced dosing frequency and prolonged duration of action, including once-daily treatment, with more consistent effects on various clinical outcomes. This review summarizes relevant clinical data for twice-daily β-2-agonists in COPD, and further focuses on novel data for once-daily indacaterol, including head-to-head comparison trials. Keywords: COPD, bronchodilators, salmeterol, indacaterol, formoterol, tiotropium, therapy, pharmacology Background: long-acting β-agonists in the treatment of COPD Current guidelines recommend long-acting bronchodilators as first-line maintenance therapy for moderate, severe, and very severe chronic obstructive pulmonary disease (COPD), with a preference for inhaled medications over oral theophyllines.1 Until recently, the once-daily anticholinergic tiotropium and the twice-daily β(2)-agonists salmeterol and formoterol were the most widely used maintenance medications. Both classes of agents have been demonstrated to be effective and hold acceptable safety profiles. In December 2009, the first once-daily long-acting β-agonist indacaterol was approved by the European Medicines Agency, and indacaterol once daily was consequently introduced into the market. The availability of a once-daily inhaled β-2-agonist for the maintenance treatment of COPD somehow marks a trend in the recent therapeutic developments in COPD, indicating a shift from short-acting bronchodilators with multiple dosings per day to reduced dosing frequency and prolonged duration of action, including once-daily treatment. This change has been consistently associated with improvements in clinical outcomes of COPD patients. Alongside the introduction of new bronchodilators, longer duration of bronchodilation showed more consistent improvements in lung function and patient-centered outcomes, International Journal of COPD 2011:6 237–243 237 © 2011 Beier and Beeh, publisher and licensee Dove Medical Press Ltd.This is an Open Access article which permits unrestricted noncommercial use, provided the original work is properly cited.