An update on bronchodilators in Phase I and II clinical trials

Expert Opin Investig Drugs. 2012 Oct;21(10):1489-501. doi: 10.1517/13543784.2012.710602. Epub 2012 Aug 23.


Introduction: Inhaled bronchodilators are the mainstay of the current management of COPD at all stages of the disease, and are critical in the symptomatic management of asthma. Therefore, there is still considerable interest in finding novel classes of broncholytic drugs or, at least, in improving the existing classes of bronchodilator.

Areas covered: This review paper mainly focuses on bronchodilators that are in Phase I and II clinical trials.

Expert opinion: To date, finding new classes of bronchodilators has proved difficult. Consequently, many research groups have sought to improve the existing classes of bronchodytic drugs. The majority of programs in development for novel bronchodilators are focused on developing new ligands that interact with β(2)-adrenoceptors and/or muscarinic acetylcholine receptors in a manner that enhances their bronchodilator effectiveness and duration of action, which allows only one administration per day, although the twice-daily dosing of bronchodilators is still considered a useful approach to the symptomatic treatment of COPD, and improving their safety profiles. Moreover, the current opinion is that it is advantageous to develop inhalers containing combinations of long-acting bronchodilator drugs in an attempt to simplify treatment regimes as much as possible. Another goal is to develop novel combinations of one or two classes of long-acting bronchodilators along with inhaled corticosteroids.

Publication types

  • Review

MeSH terms

  • Adrenal Cortex Hormones / therapeutic use
  • Adrenergic beta-Agonists / therapeutic use
  • Bronchodilator Agents / therapeutic use*
  • Humans
  • Muscarinic Antagonists / therapeutic use
  • Pulmonary Disease, Chronic Obstructive / drug therapy*


  • Adrenal Cortex Hormones
  • Adrenergic beta-Agonists
  • Bronchodilator Agents
  • Muscarinic Antagonists