Brexpiprazole

Mechanism-of-action classes: Dopamine Agonists; Serotonin Receptor Interactions.

• REXULTI is indicated for: Adjunctive treatment to antidepressants for major depressive disorder (MDD) in adults Treatment of schizophrenia in adults and pediatric patients ages 13 years and older Treatment of agitation associated with dementia due to Alzheimer's disease Limitations of Use: REXULTI is not indicated as an as needed ("prn") treatment for agitation associated with dementia due to Alzheimer's disease [see Clinical Studies (14.3) ] .ICD-10: F20.9, F32.9, G30.9

• REXULTI is contraindicated in patients with a known hypersensitivity to brexpiprazole or any of its components. Reactions have included rash, facial swelling, urticaria, and anaphylaxis.contraindicated

Administer REXULTI orally once daily with or without food. ( 2 , 12.3 ) Indication Starting Dosage Recommended Target Dosage Maximum Dosage MDD Adults ( 2.2 ) 0.5 mg/day or 1 mg/day 2 mg/day 3 mg/day Schizophrenia Adults ( 2.3 ) 1 mg/day 2 to 4 mg/day 4 mg/day Schizophrenia Pediatric (13 - 17 years) ( 2.3 ) 0.5 mg/day 2 to 4 mg/day 4 mg/day Agitation associated with dementia due to Alzheimer's disease ( 2.4 ) 0.5 mg/day 2 mg/day 3 mg/day Moderate to Severe Hepatic Impairment: Maximum recommended dosage is 2 mg once daily for patients with MDD or agitation associated with dementia due to Alzheimer's disease and 3 mg once daily for patients with schizophrenia. ( 2.5 ) CrCl<60 mL/minute: Maximum recommended dosage is 2 mg once daily for patients with MDD or agitation associated with dementia due to Alzheimer's disease and 3 mg once daily for patients with schizophrenia. ( 2.6 ) See Full Prescribing Information for dosage modifications for CYP2D6 poor metabolizers and for concomitant use with CYP inhibitors or inducers. ( 2.7 ) 2.1 Administration Information Administer REXULTI orally, once daily with or without food [see Clinical Pharmacology (12.3) ]. 2.2 Recommended Dosage for Adjunctive Treatment of Major Depressive Disorder (Adults) The recommended starting REXULTI dosage for the adjunctive treatment of MDD in adults is 0.5 mg or 1 mg orally once daily . Titrate to 1 mg once daily, then titrate to the target dosage of 2 mg once daily (based on the patient's clinical response and tolerability, increase the dosage at weekly intervals).

Cerebrovascular Adverse Reactions in Elderly Patients with Dementia-Related Psychosis: Increased incidence of cerebrovascular adverse reactions (e.g., stroke, transient ischemic attack) ( 5.3 ) Neuroleptic Malignant Syndrome: Manage with immediate discontinuation and close monitoring. ( 5.4 ) Tardive Dyskinesia: Discontinue if clinically appropriate. ( 5.5 ) Metabolic Changes: Monitor for hyperglycemia/diabetes mellitus, dyslipidemia, and weight gain. ( 5.6 ) Pathological Gambling and Other Compulsive Behaviors: Consider dose reduction or discontinuation. ( 5.7 ) Leukopenia, Neutropenia, and Agranulocytosis: Perform complete blood counts (CBC) in patients with pre-existing low white blood cell count (WBC) or history of leukopenia or neutropenia. Consider discontinuing REXULTI if a clinically significant decline in WBC occurs in absence of other causative factors. ( 5.8 ) Orthostatic Hypotension and Syncope: Monitor heart rate and blood pressure and warn patients with known cardiovascular or cerebrovascular disease, and risk of dehydration or syncope. ( 5.9 ) Seizures: Use cautiously in patients with a history of seizures or with conditions that lower the seizure threshold. ( 5.11 ) Potential for Cognitive and Motor Impairment: Use caution when operating machinery. ( 5.14 ) 5.1 Increased Mortality in Elderly Patients with Dementia-Related Psychosis Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death.

The following adverse reactions are discussed in more detail in other sections of the labeling: Increased Mortality in Elderly Patients with Dementia-Related Psychosis [see Boxed Warning , Warnings and Precautions (5.1) ] Suicidal Thoughts and Behaviors in Adolescents and Young Adults [see Boxed Warning , Warnings and Precautions (5.2) ] Cerebrovascular Adverse Reactions Including Stroke in Elderly Patients with Dementia-Related Psychosis [see Warnings and Precautions (5.3) ] Neuroleptic Malignant Syndrome (NMS) [see Warnings and Precautions (5.4) ] Tardive Dyskinesia [see Warnings and Precautions (5.5) ] Metabolic Changes [see Warnings and Precautions (5.6) ] Pathological Gambling and Other Compulsive Behaviors [see Warnings and Precautions (5.7) ] Leukopenia, Neutropenia, and Agranulocytosis [see Warnings and Precautions (5.8) ] Orthostatic Hypotension and Syncope [see Warnings and Precautions (5.9) ] Falls [see Warnings and Precautions (5.10) ] Seizures [see Warnings and Precautions (5.11) ] Body Temperature Dysregulation [see Warnings and Precautions (5.12) ] Dysphagia [see Warnings and Precautions (5.13) ] Potential for Cognitive and Motor Impairment [see Warnings and Precautions (5.14) ] Most common adverse reactions in adults were ( 6.1 ): Adult patients with major depressive disorder (adjunctive treatment to antidepressant therapy): Weight increased, somnolence, and akathisia (≥5% and at least twice the rate for placebo) Adult Patients with schizophrenia : Weight increased (≥4% and at least twice the rate for placebo) Pediatric patients (13 to 17 years) with schizop…

Pregnancy: May cause extrapyramidal and/or withdrawal symptoms in neonates with third trimester exposure ( 8.1 ) 8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to REXULTI during pregnancy. For more information contact the National Pregnancy Registry for Psychiatric Medications at 1-866-961-2388 or visit http://womensmentalhealth.org/clinical-and-research-programs/pregnancyregistry/ . Risk Summary Adequate and well-controlled studies have not been conducted with REXULTI in pregnant women to inform drug-associated risks. However, neonates whose mothers are exposed to antipsychotic drugs, like REXULTI, during the third trimester of pregnancy are at risk for extrapyramidal and/or withdrawal symptoms. In animal reproduction studies, no teratogenicity was observed with oral administration of brexpiprazole to pregnant rats and rabbits during organogenesis at doses up to 73 and 146 times, respectively, of maximum recommended human dose (MRHD) of 4 mg/day on a mg/m 2 basis. However, when pregnant rats were administered brexpiprazole during the period of organogenesis through lactation, the number of perinatal deaths of pups was increased at 73 times the MRHD [see Data ] . The background risk of major birth defects and miscarriage for the indicated population(s) is unknown. In the U.S.

There is limited clinical trial experience regarding human overdosage with REXULTI. Management of a REXULTI overdose should concentrate on supportive therapy, maintaining an adequate airway, oxygenation and ventilation, and management of symptoms. Close medical supervision and monitoring should continue until the patient recovers. Consider contacting the Poison Help Line (1-800-222-1222) or a medical toxicologist for additional overdosage management recommendations. Oral activated charcoal and sorbitol (50 g/240 mL), administered one hour after ingesting oral REXULTI, decreased brexpiprazole C max and area under the curve (AUC) by approximately 5% to 23% and 31% to 39% respectively; however, there is insufficient information available on the therapeutic potential of activated charcoal in treating an overdose with REXULTI. There is no information on the effect of hemodialysis in treating an overdose with REXULTI; hemodialysis is unlikely to be useful because brexpiprazole is highly bound to plasma proteins.

• Jul 10, 2015NDANDA205422Otsuka
• Feb 3, 2023ANDAANDA213718Ajanta Pharma Ltd

1. 1Weight Increased1,69210%
2. 2Product Use In Unapproved Indication1,3158.1%
3. 3Off Label Use1,1257.0%
4. 4Drug Ineffective9405.8%
5. 5Akathisia8645.4%
6. 6Tremor6394.0%
7. 7Anxiety5963.7%
8. 8Tardive Dyskinesia5933.7%
9. 9Depression5783.6%
10. 10Suicidal Ideation5543.4%
11. 11Death5163.2%
12. 12Product Use Issue5013.1%
13. 13Insomnia4943.1%
14. 14Fatigue4923.0%
15. 15Feeling Abnormal4762.9%

The 10 most recently updated of 86 ClinicalTrials.gov registrations naming Brexpiprazole as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Optimized Predictive Treatment In Medications for Unipolar Major Depression (OPTIMUM-D)
  Recruiting · Phase 4 · Interventional · 400 enrolled · Nova Scotia Health Authority
  NCT05017311updated 2026-06-11
• The Purpose of This Study is to Determine the Safety, Tolerability, and Pharmacokinetics of Brexpiprazole Long-acting Injection Following a Single Administration in Healthy Subjects/Patients With Schizophrenia.
  Recruiting · Phase 1 · Interventional · 56 enrolled · Sichuan Kelun Pharmaceutical Co., Ltd
  NCT06674694updated 2026-05-15
• Brexpiprazole in Alcohol Use Disorder
  Recruiting · Phase 2 · Interventional · 250 enrolled · University of Colorado, Denver
  NCT04066192updated 2026-05-01
• Study to Assess the Safety, Tolerability and Pharmacokinetics of Oral Brexpiprazole (OPC- 34712) in Adolescents With Schizophrenia
  Completed · Phase 1 · Interventional · 43 enrolled · Otsuka Pharmaceutical Development & Commercialization, Inc.
  NCT02411695updated 2026-04-28
• Real-life Assessment of Abilify Maintena + Rexult in Schizophrenia
  Completed · Observational · 6 enrolled · The University of Hong Kong
  NCT05169268updated 2026-04-27
• Food Effect Study of Brexpiprazole Once-weekly (QW) Formulation in Patients With Schizophrenia
  Completed · Phase 1 · Interventional · 59 enrolled · Otsuka Pharmaceutical Co., Ltd.
  NCT06036108updated 2026-02-11
• Safety and Tolerability of Open-Label Flexible-dose Brexpiprazole as Maintenance Treatment in Adolescents With Schizophrenia
  Completed · Phase 3 · Interventional · 295 enrolled · Otsuka Pharmaceutical Development & Commercialization, Inc.
  NCT03238326updated 2026-02-04
• Bioequivalence Study to Compare Brexpiprazole 4 mg Film Coated Tablets Versus RXULTI 4 mg Film Coated Tablet (Brexpiprazole)
  Completed · Phase 1 · Interventional · 36 enrolled · Humanis Saglık Anonim Sirketi
  NCT07266792updated 2025-12-05
• National Pregnancy Registry for Psychiatric Medications
  Recruiting · Observational · 5,000 enrolled · Massachusetts General Hospital
  NCT01246765updated 2025-10-24
• Precision Care for Major Depressive Disorder
  Enrolling by invitation · Phase 4 · Interventional · 150 enrolled · University of California, San Francisco
  NCT06580041updated 2025-09-05

CPIC-curated drug–gene pairs for Brexpiprazole. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

• CYP2D6CPIC B/C (provisional)ClinPGx 3FDA label: Actionable PGx

Frequently asked questions

How does Brexpiprazole work?

Mechanism-of-action classes: Dopamine Agonists; Serotonin Receptor Interactions.

What is Brexpiprazole used for?

According to FDA labeling, Brexpiprazole carries indications including: REXULTI is indicated for: Adjunctive treatment to antidepressants for major depressive disorder (MDD) in adults Treatment of schizophrenia in adults and pediatric patients ages 13 years and older Treatment of agitation associated with dementia due to Alzheimer's disease Limitations of Use: REXULTI is not indicated as an as needed ("prn") treatment for agitation associated with dementia due to Alzheimer's disease [see Clinical Studies (14.3) ] .. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Brexpiprazole?

Brexpiprazole is classified as Other antipsychotics, Atypical Antipsychotic, Dopamine Agonists, Serotonin Receptor Interactions.

What are the brand names for Brexpiprazole?

Brexpiprazole is marketed under brand names including Rexulti.

What are the contraindications for Brexpiprazole?

Brexpiprazole labeling lists contraindications including: REXULTI is contraindicated in patients with a known hypersensitivity to brexpiprazole or any of its components. Reactions have included rash, facial swelling, urticaria, and anaphylaxis.. Always consult the full prescribing information and a clinician.