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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].
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