There has been a real interest recently in developing once-daily beta(2)-adrenoceptor agonists (ultra-long-acting beta(2)-adrenoceptor agonists [ultra-LABAs]) for treating asthma and chronic obstructive pulmonary disease (COPD) in an attempt to simplify their management, although an increasing amount of convincing data show an association of LABAs with a rise in asthma-related deaths and life-threatening experiences. This paper reviews the effects of different ultra-LABAs that are at varying stages of development. Arformoterol, carmoterol, indacaterol and GSK-159797 are ultra-LABAs that are likely to be introduced into the market before 2010. It is plausible that once-daily dose administration of an LABA will lead to increased convenience for patients, which may also lead to enhancement of adherence, and may have advantages leading to improved overall clinical outcomes in patients with asthma and COPD.