Drug intelligence / Profile preview

GW597901X

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

Overview

GW597901X is a small molecule, long-acting muscarinic antagonist (LAMA) that was developed by GSK for the treatment of respiratory diseases, specifically asthma and chronic obstructive pulmonary disease (COPD). It acts as a competitive antagonist at the muscarinic M3 receptor (CHRM3) on airway smooth muscle, which inhibits the bronchoconstrictive effects of acetylcholine and leads to prolonged bronchodilation. GW597901X is the xinafoate salt of the parent compound GW597901. The drug was evaluated in several Phase 1 clinical trials to assess its safety, tolerability, and pharmacokinetics when administered via inhalation. However, development of the compound was subsequently terminated, and it did not progress to later-stage clinical trials or regulatory approval, with GSK focusing on other LAMA candidates such as umeclidinium.

02

Targets

CHRM3 (M3)

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