Drug intelligence / Profile preview

brexpiprazole orally disintegrating tablet

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

Overview

Brexpiprazole is a second-generation (atypical) antipsychotic small molecule discovered by Otsuka and jointly developed with Lundbeck. It functions as a serotonin-dopamine activity modulator (SDAM), acting as a partial agonist at the dopamine D2 and D3 receptors and the serotonin 5-HT1A receptor, while also acting as an antagonist at 5-HT2A, 5-HT2B, and 5-HT7 receptors. The orally disintegrating tablet (ODT) formulation is specifically designed to dissolve rapidly in the oral cavity without the need for water, providing an alternative for patients who have difficulty swallowing conventional tablets or for whom adherence is a concern. It is indicated for the treatment of schizophrenia, as an adjunctive therapy for major depressive disorder, and for agitation associated with dementia due to Alzheimer's disease.

Brand names
Rexulti
Other names
brexpiprazole ODTl-Otsuka Pharmaceutical Co., Ltd.
02

Targets

HTR2A (Serotonin receptor 5-HT2A)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))ADRA2C (α2C)HTR2B (5-Hydroxytryptamine Receptor 2B)DRD2 (Dopamine D2 Receptor)HTR7 (5-hydroxytryptamine receptor 7)DRD3 (Dopamine receptor D3)ADRA1B (α1B)

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