Drug intelligence / Profile preview

tilapertin

Development stage
Discontinued
Lead developer
Amgen
Modality
Small Molecules
Administration
Oral
01

Overview

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].

Other names
tilapertin
02

Targets

SLC6A9 (Glycine transporter type 1)

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