Bitopertin is a selective glycine reuptake inhibitor that targets the glycine transporter-1 (GlyT1), thereby increasing glycine levels in the synaptic cleft. It has been primarily investigated for its potential in treating neurological and psychiatric disorders, especially schizophrenia. By enhancing glycine availability, bitopertin supports N-methyl-D-aspartate (NMDA) receptor function, which is believed to be underactive in schizophrenia patients. This mechanism is particularly relevant for addressing negative symptoms of schizophrenia—such as social withdrawal, lack of motivation, and emotional blunting—which are often less responsive to standard antipsychotic medications. Clinical trials have explored bitopertin as an adjunctive therapy to antipsychotics in patients with persistent negative symptoms. While some studies showed improvement in symptom severity, results have been mixed, leading to ongoing evaluation of optimal dosing and patient subgroups most likely to benefit. Bitopertin has also been considered for other conditions involving glutamatergic dysfunction, including cognitive impairment and depression, though research in these areas remains early-stage. Its development highlights a shift toward targeting glutamate pathways as an alternative to dopamine-centric treatments in mental health.