Drug intelligence / Profile preview

GSK961081 + ipratropium bromide

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Inhalation
01

Overview

GSK961081 + ipratropium bromide is an experimental combination therapy for chronic obstructive pulmonary disease (COPD) comprising the dual-pharmacophore molecule GSK961081 (also known as batefenterol), which exhibits both muscarinic antagonist and β2-adrenoceptor agonist activity (classified as a MABA), combined with the muscarinic antagonist ipratropium bromide. This combination is designed to maximize bronchodilation via simultaneous stimulation of β2-adrenoceptors and blockade of muscarinic receptors in airway smooth muscle. GSK961081 provides sustained bronchodilation by acting as a potent, selective, and full agonist at the β2-adrenoceptor and as a functional antagonist at muscarinic receptors, while ipratropium bromide is a short-acting muscarinic antagonist that inhibits vagally mediated bronchoconstriction. The combination is under investigation primarily for the treatment of COPD and may provide additional bronchodilatory effects versus monotherapy[1][2][4].

Other names
batefenterol + ipratropium bromideMABA + ipratropium bromide
02

Targets

CHRM2 (M2)M1 (Muscarinic acetylcholine receptor M1)ADRB2 (β2)CHRM3 (M3)

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