Drug intelligence / Profile preview

brexpiprazole + ketamine

Development stage
Unknown
Lead developer
Taiho Pharmaceutical
Modality
Small Molecules
Administration
Oral, Intranasal
01

Overview

This combination therapy involves the co-administration of brexpiprazole, an atypical antipsychotic, and intranasal ketamine, an NMDA receptor antagonist. Brexpiprazole acts as a partial agonist at dopamine D2 and serotonin 5-HT1A receptors and an antagonist at 5-HT2A receptors, while ketamine blocks glutamate activity via NMDA receptor inhibition. The combination is being investigated by Massachusetts General Hospital for the treatment of adults with major depressive disorder who have treatment-resistant depression (TRD), specifically those who have failed at least two prior antidepressant courses. The study (NCT03149991) evaluates whether adding brexpiprazole to ketamine treatment can safely and effectively improve outcomes in patients with inadequate responses to standard antidepressant therapies.

Other names
Brexpiprazole Plus Ketamineintranasal ketamine + oral brexpiprazole
02

Targets

HRH1 (Histamine H1 Receptor)ADRA2C (α2C)HTR2A (Serotonin receptor 5-HT2A)ADRA1B (α1B)DRD2 (Dopamine D2 Receptor)NMDAR (Glutamate receptor ionotropic, NMDA)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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