Ultra-LABAs for the treatment of asthma

Highlights

• The term ultra-LABA was coined in 2005 to indicate once-daily β₂-AR agonists.

• Ultra-LABAs would increase adherence and consequently improve clinical outcomes.

• Extensive preclinical studies investigated the pharmacological profile of ultra-LABAs.

• The four currently available ultra-LABAs have been studied in asthmatic patients.

• Ultra-LABAs can be prescribed in asthmatics only when associated with an ICS.

Abstract

The term ultra-LABA indicates once-daily β2-AR agonists (abediterol, indacaterol, olodaterol and vilanterol) that are single enantiomers of the (R)-configuration. All have a near full-agonist profile at human β2-AR. They can be prescribed in asthmatics only when associated with an with ICS, although further confirmations need to clarify what really these agents add if used in association to ICS and in what asthmatic patients this association may have more value. They are also under development in triple inhalers that include an ultra-LABA, a LAMA and an ICS. The once-daily posology might increase adherence in long-term treatment of asthma but superiority to twice-daily LABAs has not yet been fully demonstrated. In any case, still no ultra-LABA can be recommended as preferred.