Brexpiprazole

(Rexulti®)

Rexulti®

Drug updated on 12/11/2024

Dosage FormTablet (oral; 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, and 4 mg)
Drug ClassAtypical antipsychotics
Ongoing and
Completed Studies
ClinicalTrials.gov

Indication

  • Indicated for use as an adjunctive therapy to antidepressants for the treatment of major depressive disorder (MDD) in adults
  • Indicated for the treatment of schizophrenia in adults and pediatric patients ages 13 years and older
  • Indicated for the treatment of agitation associated with dementia due to Alzheimers disease.

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Summary
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  • This summary is based on the review of 16 systematic review(s)/meta-analysis(es). [1-16]
  • Schizophrenia Management: Brexpiprazole significantly reduced Positive and Negative Syndrome Scale (PANSS) scores compared to placebo and demonstrated similar efficacy to aripiprazole. However, it was found to be less effective than risperidone and equally effective as olanzapine in treating acute mania.
  • Major Depressive Disorder (MDD): As an adjunct treatment, brexpiprazole showed significant improvements on the Montgomery-Asberg Depression Rating Scale (MADRS), Sheehan Disability Scale (SDS), and Hamilton Depression Rating Scale (HDRS17) in adults inadequately responsive to antidepressants. Optimal dosing of 1-2 mg improved the risk-benefit balance compared to other antipsychotic adjuncts.
  • Behavioral and Psychological Symptoms of Dementia (BPSD): Brexpiprazole was significantly more effective than placebo in reducing agitation symptoms in Alzheimer’s patients, as measured by the Cohen-Mansfield Agitation Inventory (CMAI) and Clinical Global Impression - Severity of illness (CGI-S) score, and was more efficacious than quetiapine, olanzapine, and aripiprazole.
  • Patient Populations: The studies included diverse populations, with adults having schizophrenia and MDD, as well as patients with Alzheimer’s disease experiencing agitation; specific subgroup findings were not detailed in the studies.
  • Common Adverse Events: Brexpiprazole was associated with side effects including akathisia, weight gain, and somnolence, with these effects being dose-dependent; higher doses correlated with increased risk.
  • Serious Adverse Events: There was no significant difference in the incidence of serious adverse events or all-cause mortality between brexpiprazole and placebo in patients with Alzheimer’s disease.
  • Comparison with Other Drugs: Brexpiprazole demonstrated a better safety profile regarding falls and sedation compared to olanzapine in treating behavioral and psychological symptoms of dementia (BPSD), while also exhibiting fewer intolerability-related discontinuations than aripiprazole and quetiapine in MDD.
  • Brexpiprazole was effective in managing schizophrenia, MDD, and behavioral and psychological symptoms of dementia (BPSD), with studies including a broad range of patients; optimal dosing in MDD was noted at 1-2 mg for a better risk-benefit balance, particularly in adults inadequately responsive to antidepressants.

Product Monograph / Prescribing Information

Document TitleYearSource
Rexulti (brexpiprazole) Prescribing Information.2024Otsuka America Pharmaceutical, Inc., Princeton, NJ

Systematic Reviews / Meta-Analyses

Document TitleYearSource
Real-World Effectiveness, Economic, and Humanistic Outcomes of Selected Oral Antipsychotics in Patients with Schizophrenia: A Systematic Review Evaluating Global Evidence2024ClinicoEconomics and Outcomes Research
Efficacy, acceptability and tolerability of second-generation antipsychotics for behavioural and psychological symptoms of dementia: a systematic review and network meta-analysis2024BMJ Mental Health
Efficacy and safety of brexpiprazole for the treatment of agitation in Alzheimer's disease: a meta-analysis of randomized controlled trials2024Neurological Sciences
Comparison of brexpiprazole, aripiprazole, and placebo for Japanese major depressive disorder: A systematic review and network meta-analysis2024Neuropsychopharmacology Reports
Comparative efficacy and safety of 4 atypical antipsychotics augmentation treatment for major depressive disorder in adults: A systematic review and network meta-analysis2023Medicine
Comparison of antipsychotic dose equivalents for acute bipolar mania and schizophrenia2023BMJ Mental Health
Efficacy and safety/tolerability of antipsychotics in the treatment of adult patients with major depressive disorder: a systematic review and meta-analysis2023Psychological Medicine
Optimal dose of brexpiprazole for augmentation therapy of antidepressant-refractory depression: A systematic review and dose-effect meta-analysis2022Psychiatry and Clinical Neurosciences
Antipsychotic-Induced Weight Gain: Dose-Response Meta-Analysis of Randomized Controlled Trials2022Schizophrenia Bulletin
Efficacy and Tolerability of Combination Treatments for Major Depression: Antidepressants plus Second-Generation Antipsychotics vs. Esketamine vs. Lithium2021Journal of Psychopharmacology (Oxford, England)
Efficacy and safety of antipsychotic treatments for schizophrenia: A systematic review and network meta-analysis of randomized trials in Japan2021Journal of Psychiatric Research
Efficacy and safety of brexpiprazole in acute management of psychiatric disorders: a meta-analysis of randomized controlled trials2020international Clinical Psychopharmacology
Aripiprazole vs. brexpiprazole for acute schizophrenia: a systematic review and network meta-analysis2020Psychopharmacology
Blonanserin patch vs. Other Antipsychotics for Acute Schizophrenia: A Systematic Review of Double-blind, Randomized, Placebo-controlled, Phase 3 Trials in Japan2020Pharmacopsychiatry
Dose-Response Meta-Analysis of Antipsychotic Drugs for Acute Schizophrenia2020The American Journal of Psychiatry
Brexpiprazole as Adjunctive Treatment for Major Depressive Disorder Following Treatment Failure With at Least One Antidepressant in the Current Episode: a Systematic Review and Meta-Analysis2019The international Journal of Neuropsychopharmacology

Clinical Practice Guidelines