Brexpiprazole is a serotonin–dopamine activity modulator used in the treatment of major depressive disorder as an adjunct, schizophrenia, and agitation associated with dementia due to Alzheimer’s disease. Brexpiprazole is an atypical antipsychotic and a novel D2 dopamine and serotonin 1A partial agonist called serotonin-dopamine activity modulator (SDAM).
- Mechanism
- Curator reviewed · 5 references
Although the exact mechanism of action of brexpiprazole in psychiatric disorders has not been fully elucidated, the efficacy of brexpiprazole may be attributed to combined partial agonist activity at 5-HT1A and dopamine D2 receptors, and antagonist activity at 5-HT2A receptors. Brexpiprazole binds to these receptors with subnanomolar affinities. These therapeutic targets have been implicated in psychiatric conditions such as schizophrenia and depression. Partial D2 receptor agonism allows the drug to stimulate D2 receptors under low dopamine conditions, while attenuating their activation when dopamine levels are high. Partial agonism at 5-HT1A receptors may be tied to improved memory function and cognitive performance. Antagonism at α-adrenergic receptors has also been implicated in schizophrenia and depression.
- Primary indication
- Brexpiprazole is indicated as adjunctive therapy to antidepressants for the treatment of major depressive disorder in adults.Curator reviewed · 3 structured indications
- Formula / weight
- C25H27N3O2S · 433.57 g/mol (avg)
- First approval
- Canada, 2017 · United States, 2015 · European Union, 2020
- Also known as
- Lu-AF41156
- Code names
- OPC-34712 · OPC-34712FUM
- Brand names
Resolves to
ZKIAIYBUSXZPLP-UHFFFAOYSA-NSMILESO=C1NC2=CC(OCCCCN3CCN(CC3)C3=C4C=CSC4=CC=C3)=CC=C2C=C1What you can answer from here — as of September 12, 2026
Which drugs share a target with Brexpiprazole, and which of those have an active Phase 3 trial?
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