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Brexpiprazole (OPC-34712)
Brexpiprazole is a serotonin-dopamine activity modulator (SDAM) that acts as a partial agonist at dopamine D2 and serotonin 5-HT1A receptors while antagonizing serotonin 5-HT2A receptors.
Brexpiprazole is a serotonin-dopamine activity modulator (SDAM) that acts as a partial agonist at dopamine D2 and serotonin 5-HT1A receptors while antagonizing serotonin 5-HT2A receptors. Used for Schizophrenia, Schizoaffective disorder, Major depressive disorder (adjunctive treatment).
At a glance
| Generic name | Brexpiprazole (OPC-34712) |
|---|---|
| Sponsor | Otsuka Pharmaceutical Development & Commercialization, Inc. |
| Drug class | Atypical antipsychotic; serotonin-dopamine activity modulator (SDAM) |
| Target | Dopamine D2 receptor (partial agonist); serotonin 5-HT1A receptor (partial agonist); serotonin 5-HT2A receptor (antagonist) |
| Modality | Small molecule |
| Therapeutic area | Psychiatry/Neurology |
| Phase | Phase 3 |
Mechanism of action
As a partial agonist at D2 receptors, brexpiprazole provides dopaminergic stabilization with lower intrinsic activity than full agonists, reducing the risk of excessive dopamine stimulation. Its 5-HT1A partial agonism and 5-HT2A antagonism contribute to anxiolytic and antidepressant-like effects. This multi-target profile is designed to provide antipsychotic efficacy with improved tolerability compared to first-generation antipsychotics.
Approved indications
- Schizophrenia
- Schizoaffective disorder
- Major depressive disorder (adjunctive treatment)
Common side effects
- Akathisia
- Headache
- Sedation/somnolence
- Weight gain
- Tremor
- Dizziness
Key clinical trials
- Safety and Tolerability of Open-Label Flexible-dose Brexpiprazole as Maintenance Treatment in Adolescents With Schizophrenia (PHASE3)
- Brexpiprazole in Treatment of Children and Adolescents With Irritability Associated With Autism Spectrum Disorder (PHASE3)
- Brexpiprazole for the Treatment of Patients With Agitation Associated With Dementia of the Alzheimer's Type (PHASE2, PHASE3)
- Evaluating the Safety and Tolerability of Brexpiprazole in the Treatment of Adults With Borderline Personality Disorder (BPD) (PHASE2, PHASE3)
- Brexpiprazole for the Long-term Treatment of Patients With Agitation Associated With Dementia of the Alzheimer's Type (PHASE3)
- Brexpiprazole in Treatment of Children and Adolescents With Irritability Associated With Autism Spectrum Disorder for Subjects That Have Completed Participation in 331-201-00148 (PHASE3)
- Brexpiprazole as Adjunctive Therapy in Adults With Major Depressive Disorder (PHASE4)
- Trial to Evaluate the Short-term Safety & Efficacy of Brexpiprazole Monotherapy in the Treatment of Adolescents With Schizophrenia (PHASE3)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
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