Drug intelligence / Profile preview

brexpiprazole

Development stage
Approved
Lead developer
Otsuka Holdings
Modality
Small Molecules
Administration
Oral
01

Overview

Brexpiprazole is a small molecule atypical antipsychotic and serotonin-dopamine activity modulator (SDAM) co-developed by Otsuka Pharmaceutical and Lundbeck. It functions as a partial agonist at the dopamine D2 and serotonin 5-HT1A receptors, and as an antagonist at the serotonin 5-HT2A and noradrenaline alpha-1B/2C receptors. It is primarily indicated for the treatment of schizophrenia in adults and adolescents (aged 13-17) and as an adjunctive therapy for major depressive disorder (MDD) in adults. Brexpiprazole was designed to have lower intrinsic activity at the D2 receptor compared to aripiprazole, which is intended to reduce the incidence of dopamine-mediated adverse events such as akathisia, restlessness, and insomnia. It has also received approval for the treatment of agitation associated with dementia due to Alzheimer's disease.

Brand names
Rexulti
Other names
brexpiprazole
02

Targets

HTR2A (Serotonin receptor 5-HT2A)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))ADRA2C (α2C)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)ADRA1B (α1B)

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