Drug intelligence / Profile preview

GSK1018921

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

Overview

GSK1018921 is an investigational small molecule drug developed by GSK as a selective inhibitor of glycine transporter 1 (GlyT-1). Its primary mechanism of action is the inhibition of GlyT-1, which increases synaptic glycine levels and modulates NMDA receptor function. This mechanism was explored for potential therapeutic benefit in schizophrenia. The drug demonstrated dose-proportional pharmacokinetics with a terminal half-life of approximately 17 hours. In early clinical studies, dizziness was the most common adverse effect and appeared to be dose-dependent. Development appears to have been discontinued after phase 1 trials[2][4][6].

Other names
Glycine transporter-1 inhibitor
02

Targets

SLC6A9 (Glycine transporter type 1)

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