Drug intelligence / Profile preview

GSK961081 + propranolol

Development stage
Phase 1
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Inhalation
01

Overview

GSK961081 + propranolol is an investigational combination in which **GSK961081**, a bi-functional molecule (MABA) that combines muscarinic antagonist and β2 adrenergic agonist activities, is co-administered with **propranolol**, a non-selective beta-adrenergic antagonist. GSK961081 acts via bronchodilation through both muscarinic receptor blockade and β2 adrenoceptor agonism; propranolol blocks β-receptors (including β2), allowing study of the contribution of the muscarinic antagonist component alone. This combination has been studied in healthy volunteers to explore the pharmacology and contribution of each pharmacophore for respiratory indications such as COPD.

Other names
GSK961081 + propranolol
02

Targets

CHRM2 (M2)CHRM3 (M3)ADRB2 (β2)ADRB1 (β1)

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