Brexpiprazole
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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 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.
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-HT and dopamine D2 receptors, and antagonist activity at 5-HT 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-HT receptors may be tied to improved memory function and cognitive performance. Antagonism at α-adrenergic receptors has also been implicated in schizophrenia and depression.
Brexpiprazole is indicated as adjunctive therapy to antidepressants for the treatment of major depressive disorder in adults. It is also indicated for the treatment of schizophrenia in patients 13 years of age and older. Brexpiprazole is also indicated for the treatment of agitation associated with dementia due to Alzheimer’s disease; however, it is not indicated as an as-needed (“prn”) treatment for this condition.
