Drug intelligence / Profile preview

GS-5759

Development stage
Preclinical
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Inhalation
01

Overview

GS-5759 is an inhaled **bifunctional small-molecule** respiratory drug candidate developed by **GSK** for **chronic obstructive pulmonary disease**. It was designed as a single chemical entity that combines **long-acting beta-2 adrenergic receptor agonist** activity with **phosphodiesterase 4 inhibitory** activity, aiming to deliver both bronchodilation and anti-inflammatory effects in the lung. Preclinical publications describe potent beta-2 agonism, potent PDE4 inhibition, activity in airway and inflammatory cell assays, bronchodilator efficacy in multiple animal models, and optimization for inhalation delivery, with the concept that dual pharmacology in one molecule could support COPD treatment and potentially use in triple-therapy regimens with an additional inhaled agent. Public evidence provided here is preclinical; no marketed brand name or INN was identified from the supplied sources.

02

Targets

PDE4 (Phosphodiesterase 4A1)ADRB1 (β1)

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