molecules of the month

Context. CHF-6366 (Chiesi Farmaceutici S.p.A) is a muscarinic antagonist and β2 agonist (MABA) being developed as an inhaled treatment for respiratory diseases. Muscarinic antagonists and β2 agonists both act to inhibit bronchoconstriction, but through different mechanisms, making the combination of both agents a desirable strategy for achieving enhanced efficacy in treating pulmonary diseases. Although long-acting formulations of muscarinic antagonists and β2 agonists have been combined and used actively in the last 10 years (e.g., Anoro Ellipta and Stiolto Respimat), various drawbacks associated with such multicomponent inhalers have led to efforts to develop bifunctional agents with dual activity on either receptor. Such MABAs are expected to be single molecular entities comprising two covalently-linked pharmacophores. At least 5 MABA agents are currently…