Muscarinic antagonist-β-adrenergic agonist dual pharmacology molecules as bronchodilators: a patent review

Abstract

Background: The proven efficacy of several anti-cholinergics and β₂-agonists and their combinations in both chronic obstructive pulmonary disease (COPD) and asthma strongly validates this therapeutic approach. As a consequence and although technically challenging, over the past 4 years there has been a growing interest in the generation of dual pharmacology Muscarinic-receptor antagonists-β₂-adrenergic receptor agonists (MABAs) for the treatment of COPD. Objective/methods: This article surveys and reviews the research activity in the MABA area to the end of August 2008. Results/conclusion: Although the activity in this field seems to still be limited to a few companies, significant progress in the discovery of a MABA has been achieved with the progression of at least one candidate (GSK-961081) to the clinic.

Keywords::

• chronic obstructive pulmonary disease
• Muscarinic receptors
• β₂-adrenergic receptor
• β₂-adrenoceptors