drug
as of 2026-07-01Brexpiprazole (Rexulti)
Brexpiprazole 1mg to 4mgOPC-34712BrexpiprazoleBrexpiprazole (OPC-34712)OPC-34712FUM/ Brexpiprazole fumarateBrexpiprazole LAI: Dose 1Brexpiprazole LAI: Dose 2Brexpiprazole LAI: Dose 3
UNII 2J3YBM1K8CRxCUI 1658314FDA_ApplNo NDA205422SPL_set_id 2d301358-6291-4ec1-bd87-37b4ad9bd850FDA_sponsor OTSUKAOrangeBook_Appl A213512, A213562, A213570, A213659, A213660, A213669, A213683, A213692
at a glance
small molecule · Atypical Antipsychotic [EPC]
US-approved (2015) as Rexulti
Orange Book protection to 2033
38 trials in the graph
Synthesized from structured facts only — each point cited above.
Mechanism & identity
Modality
small molecule
FDA class
Atypical Antipsychotic [EPC]
RxCUI
1658314
Indications
Labeled
SchizophreniaMajor depressive disorderAgitation
Investigational (via trials)
Patents & exclusivity
Orange Book
patent 10307419*PED2033-04-12
patent 103074192032-10-12
patent RE48059*PED2029-06-23
patent RE480592028-12-23
patent 9839637*PED2026-10-12
patent 8618109*PED2026-10-12
patent 7888362*PED2026-10-12
patent 8349840*PED2026-10-12
patent 9839637 · U-15292026-04-12
patent 78883622026-04-12
patent 8618109 · U-5432026-04-12
patent 8349840 · U-15292026-04-12
exclusivity M-3152028-05-09
exclusivity PED2027-11-08
exclusivity M-142027-05-08
exclusivity PED2026-11-10
exclusivity I-9132026-05-10
Adverse-event signal
FAERS spontaneous · within-drug share
Eps Akathisia11.6%
top term: AKATHISIA
Weight Metabolic7.4%
top term: WEIGHT INCREASED
Sedation4.1%
top term: FATIGUE
Mortality3.3%
top term: DEATH
Gi3.2%
top term: NAUSEA
Qt Cardiac0.9%
top term: ELECTROCARDIOGRAM QT PROLONGED
Anticholinergic0.9%
top term: CONSTIPATION
Nms0.4%
top term: NEUROLEPTIC MALIGNANT SYNDROME
Spontaneous reports — a signal of reporting share, not incidence.
Regulatory history
Drugs@FDA submissions
LabelingNDA205422 s17STANDARD
2026-04-30EfficacyNDA205422 s14STANDARD
2025-05-09LabelingNDA205422 s13STANDARD
2024-12-11EfficacyNDA205422 s11PRIORITY
2024-05-07EfficacyNDA205422 s9PRIORITY
2023-05-10LabelingNDA205422 s8STANDARD
2022-10-06EfficacyNDA205422 s7PRIORITY
2021-12-27LabelingNDA205422 s5STANDARD
2020-06-17LabelingNDA205422 s3STANDARD
2018-02-09LabelingNDA205422 s2901 REQUIRED
2017-02-23EfficacyNDA205422 s1STANDARD
2016-09-23Type 1 - New Molecular EntityNDA205422 s1STANDARD
2015-07-10EfficacyNDA205422 s2STANDARD
2015-07-10Trials
38
Real-life Assessment of Brexpiprazole (Rexulti) in Schizophrenia and in Depressive Disorders
NCT05962216—Recruiting
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.
NCT06674694Phase 1Recruiting
Trial of Brexpiprazole Once-weekly (QW) Formulation in Patients With Acute Schizophrenia
NCT05325645Phase 3Recruiting
Real-life Assessment of Abilify Maintena + Rexult in Schizophrenia
NCT05169268—Completed
Bioequivalence Study to Compare Brexpiprazole 4 mg Film Coated Tablets Versus RXULTI 4 mg Film Coated Tablet (Brexpiprazole)
NCT07266792Phase 1Completed
A Long-term Administration Trial of Brexpiprazole Once-weekly (QW) Formulation in Patients With Schizophrenia
NCT05326347Phase 3Active Not Recruiting
Safety and Tolerability of Open-Label Flexible-dose Brexpiprazole as Maintenance Treatment in Adolescents With Schizophrenia
NCT03238326Phase 3Completed
Food Effect Study of Brexpiprazole Once-weekly (QW) Formulation in Patients With Schizophrenia
NCT06036108Phase 1Completed
Controlled Trial of Brexpiprazole For The Treatment of Co-occurring Schizophrenia and Substance Use Disorder
NCT03526354Phase 4Completed
"Brexpiprazole (Rexulti™) Safety and Efficacy Among Filipino Patients (RAISE) - A Post Marketing Surveillance Program"
NCT04641780—Unknown
Trial to Evaluate the Short-term Safety & Efficacy of Brexpiprazole Monotherapy in the Treatment of Adolescents With Schizophrenia
NCT03198078Phase 3Completed
A Clinical Pharmacology Trial of Brexpiprazole Long Acting Injectable (LAI) Administered as a Single Dose in Patients With Schizophrenia
NCT05119894Phase 1Withdrawn
Safety and Efficacy of Brexpiprazole in the Treatment of Schizophrenia
NCT03874494Phase 3Completed
A Study to Assess the Safety and Efficacy of ASP4345 as Add-on Treatment for Cognitive Impairment in Subjects With Schizophrenia on Stable Doses of Antipsychotic Medication
NCT03557931Phase 2Completed
Safety and Tolerability Study of Single-dose Administration of Brexpiprazole in Adult Subjects With Schizophrenia
NCT02968121Phase 1Terminated
Study to Assess the Safety, Tolerability and Pharmacokinetics of Oral Brexpiprazole (OPC- 34712) in Adolescents With Schizophrenia
NCT02411695Phase 1Completed
Comparison of the Effectiveness of Brexpiprazole With That of Risperidone
NCT02758067Phase 3Withdrawn
Monotherapy Brexpiprazole (OPC-34712) Trial in the Treatment of Adults With Schizophrenia With Impulsivity
NCT02194933Phase 3Completed
Safety and Tolerability Study of Oral OPC-34712 as Maintenance Treatment in Adults With Schizophrenia
NCT01397786Phase 3Completed
Brexpiprazole in Patients With Schizophrenia
NCT01810783Phase 3Completed
Brexpiprazole (OPC 34712) Trial in the Treatment of Adults With Major Depressive Disorder and Irritability
NCT02212613Phase 3Withdrawn
A Dose-finding Trial of OPC-34712 in Patients With Schizophrenia
NCT01451164Phase 2, Phase 3Completed
A Long-term Trial of OPC-34712 in Patients With Schizophrenia
NCT01456897Phase 3Completed
KOLs & investigators
12
Publications & congress
30
Effects of Adjunctive Brexpiprazole in Major Depressive Disorder Analyzed by Baseline Anxiety Level: Post Hoc Analysis of a Phase 4 Study.
Journal of clinical psychopharmacology · 2026 Mar-Apr 01 · high-value
Dose-Dependent efficacy and safety of Brexpiprazole in agitation associated with dementia in Alzheimer's disease: A systematic review and meta-analysis.
Neurological sciences : official journal of the Italian Neurological Society and of the Italian Society of Clinical Neurophysiology · 2026 · high-value
Efficacy and safety of brexpiprazole in early-episode schizophrenia: post hoc analysis of Phase 3 clinical trials in adults and adolescents.
Psychiatry research · 2026 · high-value
Comparative efficacy and safety of different brexpiprazole doses for agitation in Alzheimer's disease: A systematic review and network meta-analysis.
Journal of Alzheimer's disease : JAD · 2026 · high-value
Efficacy and tolerability of brexpiprazole augmentation of SSRI therapy in PTSD: A systematic review and meta-analysis of randomized controlled trials.
Journal of psychiatric research · 2026 · high-value
Impact of selected second and third generation antipsychotics on cognitive dysfunction in schizophrenia-spectrum disorders. Systematic review and network meta-analysis.
International clinical psychopharmacology · 2026 · high-value
Antipsychotics in Children and Adolescents with Schizophrenia-Spectrum Disorders: A Systematic Review, Meta-Analysis, and Long-Term Prospective Evidence.
Journal of child and adolescent psychopharmacology · 2026 · high-value
Fixed-Dose Brexpiprazole and Sertraline Combination Therapy for the Treatment of Posttraumatic Stress Disorder: A Phase 3, Randomized Trial.
Journal of clinical psychopharmacology · 2025 Nov-Dec 01 · high-value
Brexpiprazole and Sertraline Combination Treatment in Posttraumatic Stress Disorder: A Phase 3 Randomized Clinical Trial.
JAMA psychiatry · 2025 · high-value
Safety and Tolerability of Brexpiprazole in Participants with Agitation Associated with Dementia due to Alzheimer's Disease: Pooled Analysis of Three Randomized Trials and an Extension Trial.
CNS drugs · 2025 · high-value
Antipsychotic drug dosing and study discontinuation in schizophrenia: A systematic review and dose-response meta-analysis.
European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology · 2025 · high-value
Efficacy and safety of brexpiprazole in adolescents with schizophrenia: a multicountry, randomised, double-blind, placebo-controlled, phase 3 trial with an active reference.
The lancet. Psychiatry · 2025 · high-value
Safety and Efficacy of Brexpiprazole in the Treatment of Irritability Associated with Autism Spectrum Disorder: An 8-Week, Phase 3, Randomized, Double-Blind, Placebo-Controlled Trial and 26-Week Open-Label Extension in Children and Adolescents.
Journal of child and adolescent psychopharmacology · 2025 · high-value
Effects of brexpiprazole on patient life engagement in schizophrenia:
Current medical research and opinion · 2025 · high-value
Brexpiprazole in Combination With Sertraline and as Monotherapy in Posttraumatic Stress Disorder: A Full-Factorial Randomized Clinical Trial.
The Journal of clinical psychiatry · 2025 · high-value
Brexpiprazole for agitation in clinically relevant patient subgroups: a
Current medical research and opinion · 2025 · high-value
Facts & assertions
29 sourced
Anda Generic Count
71
Available Strengths
brexpiprazole 0.25 MG Oral Tablet, brexpiprazole 0.5 MG Oral Tablet, brexpiprazole 1 MG Oral Tablet, brexpiprazole 2 MG Oral Tablet, brexpiprazole 3 MG Oral Tablet, brexpiprazole 4 MG Oral Tablet
Boxed Warning
present
Dose Forms
Oral Tablet
Dosing Frequency
once daily
Faers Share Anticholinergic
0.009
Faers Share Eps Akathisia
0.116
Faers Share Gi
0.032
Faers Share Mortality
0.033
Faers Share Nms
0.004
Faers Share Qt Cardiac
0.009
Faers Share Sedation
0.041
Faers Share Weight Metabolic
0.074
Fda Pharm Class Epc
Atypical Antipsychotic [EPC]
Has Generic Competition
yes
Label Expansions ApprovedBrexpiprazole (Rexulti): 5 approved efficacy label-expansion supplements since launch on NDA205422. Higher count = more aggressive addressable-market broadening (competitive-threat velocity signal).
5
Latest Exclusivity Expiry
2028-05-09
Latest Patent Expiry
2033-04-12
Latest Protection Date
2033-04-12
Originator Company
Otsuka
Rxcui
1658314
Safety Eps Akathisia
present in label
Safety Nms
present in label
Safety Orthostatic
present in label
Safety Prolactin
present in label
Safety Sedation Somnolence
present in label
Safety Weight Metabolic
present in label
Us Approved
yes
Us Original Approval Date
2015-07-10
relationships
The graph out of here
developer
trial
indication
indication
indication
indication
indication
KOL
Caroline Ward, PhD.
personKOL score 13
Dean Wong, MD,PhD
personKOL score 11
Xiaoduo Fan, MD, MPH, MS
personKOL score 9
Aleksandar Skuban
personKOL score —