molecules of the month


oral GlyT1 inhibitor

Ph. III candidate in schizophrenia

10 and 25 mg PO QD efficacy in CIAS improv.

J. Pharmacol. Exp. Ther.

Boehringer Ingelheim Pharma, Biberach an der Riss, DE

iclepertin structure
4 mins read

Context. Iclepertin (BI 425809; Boehringer Ingelheim) is an oral glycine transporter-1 (GlyT1) inhibitor being developed for cognitive impairment associated with schizophrenia (CIAS). The ineffectiveness of currently available antipsychotic medications in improving negative symptoms and cognitive deficits leaves a significant unmet need for patients with CIAS. Based on the glutamate N-methyl-d-aspartate (NMDA) receptor hypofunction hypothesis, several agents have been explored to reverse deficits in sensory processing and improve cognition in these patients. Notably, the transporter GlyT1, which depletes extracellular glycine, has been actively pursued. None have survived clinical development, however, with the most notable being ex-Roche agent bitopertin, which was discontinued following poor efficacy in two Ph. III studies (the molecule is currently being developed by Disc Medicine for rare genetic…

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