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Tilapertin (AMG 747) is an orally bioavailable, potent, and selective small molecule inhibitor of glycine transporter type-1 (GlyT1). By inhibiting GlyT1, tilapertin increases extracellular glycine concentrations in the central nervous system, which in turn enhances N-methyl-D-aspartate receptor (NMDAR) function. This mechanism is based on the hypothesis that NMDAR hypofunction contributes to negative symptoms in schizophrenia. Tilapertin was developed by Amgen and advanced to phase 2 clinical trials as an adjunctive treatment for negative symptoms of schizophrenia. However, development was terminated after a serious adverse event (Stevens-Johnson Syndrome/Toxic Epidermal Necrolysis) occurred during trials[1][2][4][5].
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