Drug intelligence / Profile preview

RO4917838 + valproate

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

RO4917838 + valproate is a **combination of two pharmaceutical drugs**: RO4917838 (also known as bitopertin), a selective glycine transporter 1 (GlyT1) inhibitor under investigation for treating schizophrenia, and valproate (valproic acid/valproate sodium), a well-established anticonvulsant and mood stabilizer. Bitopertin (RO4917838) acts primarily by modulating glycine reuptake to influence NMDA receptor–mediated neurotransmission, targeting persistent negative symptoms in schizophrenia[2][4][6][8]. Valproate inhibits GABA transaminase and affects voltage-gated sodium channels, increasing GABA levels and stabilizing neuronal firing. In combinations, pharmacological interactions may occur due to metabolic effects: valproate may inhibit metabolic enzymes and affect serum levels of concurrently administered drugs[1]. There is limited published clinical data on the specific RO4917838 + valproate combination; most RO4917838 trials paired it with antipsychotics, not valproate.

Brand names
None
Other names
RO4917838 + valproic acidbitopertin + valproatebitopertin + valproic acid
02

Targets

SLC6A9 (Glycine transporter type 1)

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