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ST-905-AG1 is an investigational, first-in-class small molecule G protein-coupled receptor 52 (GPR52) agonist being developed by Syremis Therapeutics for the treatment of schizophrenia. GPR52 is an orphan GPCR predominantly expressed in the striatum and prefrontal cortex, regions critical to the pathophysiology of psychosis and cognitive impairment. By activating GPR52, the drug aims to modulate dopaminergic and glutamatergic signaling, potentially addressing positive, negative, and cognitive symptoms of schizophrenia while avoiding the metabolic and extrapyramidal side effects associated with traditional dopamine D2 receptor antagonists. As of 2024, ST-905-AG1 has entered Phase 1 clinical evaluation in healthy volunteers to assess its safety, tolerability, and pharmacokinetic profile.
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