Drug intelligence / Profile preview

GSK961081 + salbutamol

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

Overview

GSK961081 + salbutamol is a combination of two bronchodilator agents intended for respiratory disease management, specifically **chronic obstructive pulmonary disease (COPD)**. GSK961081 (also known as batefenterol) is a novel bifunctional molecule termed a MABA (muscarinic antagonist β2-agonist), which simultaneously provides both muscarinic receptor antagonism and β2-adrenoceptor agonism within a single molecule[1][2][5]. **Salbutamol** (also known as albuterol) is a well-established short-acting β2-adrenoceptor agonist routinely used as a "rescue" bronchodilator. The combination is studied to evaluate the bronchodilatory effects and safety of adding salbutamol to maintenance therapy with GSK961081, which acts as a long-acting bronchodilator. Mechanistically, GSK961081 blocks muscarinic (M3) receptors to prevent bronchoconstriction while activating β2-adrenoceptors to induce bronchodilation[1][2][3]. Salbutamol offers rapid, short-term β2-agonism, supplementing the maintenance effect of GSK961081[3]. The drug combination is developed and investigated primarily by **GSK** (GlaxoSmithKline)[1][5]. Indicated primarily for COPD, the combination explores synergistic bronchodilation and rescue therapy potential.

Other names
batefenterol + salbutamol
02

Targets

CHRM2 (M2)CHRM3 (M3)ADRB2 (β2)

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