Drug intelligence / Profile preview

GSK1034702

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

Overview

GSK1034702 is a small molecule allosteric agonist of the muscarinic acetylcholine receptor M1 (M1 mAChR). It was developed to improve cognitive impairment, particularly targeting conditions such as Alzheimer's disease and schizophrenia. GSK1034702 selectively stimulates M1 receptors, which are highly expressed in the hippocampus and play a critical role in learning and memory. Preclinical studies demonstrated procognitive effects in rodents, while clinical trials showed that GSK1034702 could improve episodic memory encoding in humans under nicotine abstinence—a model for cognitive dysfunction. The drug exhibits high selectivity for M1 over other muscarinic receptor subtypes and has been shown to cross the blood-brain barrier with some species variability[1][2][3][5][6].

Other names
7-fluoro-5-methyl-3-[1-(oxan-4-yl)piperidin-4-yl]-1H-benzimidazol-2-one
02

Targets

M1 (Muscarinic acetylcholine receptor M1)

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