batefenterol

Batefenterol is a first-in-class, inhaled, bifunctional small molecule that acts as both a muscarinic antagonist (targeting M2 and M3 receptors) and a beta 2 adrenergic receptor agonist. It was developed primarily for the treatment of chronic obstructive pulmonary disease (COPD). Batefenterol demonstrates high affinity for human muscarinic M2 (Ki=1.4 nM) and M3 receptors (Ki=1.3 nM), as well as the beta 2 adrenergic receptor (Ki=3.7 nM), with potent functional selectivity over other beta adrenoceptor subtypes. The drug has shown clinically significant improvements in lung function in phase II clinical trials, with no new or unexpected safety signals observed in COPD patients[1][2][6]. Its dual mechanism provides bronchodilation through both competitive antagonism of muscarinic receptors and agonism of the beta 2 adrenergic receptor[6]. Batefenterol was originally discovered by Theravance and further developed by GSK[4].

Other names

batefenterol succinate