Rexulti

(Brexpiprazole)

ApprovedSmall molecule

Brexpiprazole is used to treat schizophrenia and as an add-on treatment for depression when antidepressants alone aren't working well enough.[2] Rexulti is currently approved and in use across 11 indications[4].[1]

Rexulti is one of 265 small molecule programs targeting Psychosis. It is currently in Approved.

Indications

Total Trials

Active Trials

264

Competitors

FDA Application

NDA/BLA/ANDA regulatory filings

Patents

Pipeline

Status by Indication[4][1]

Indication

PsychosisActive, not recruiting

Alzheimer DiseaseApproved

Sleep DisorderApproved

Depressive DisorderApproved

Bipolar DisorderApproved

Alcohol DependenceApproved

Aggressive BehaviorActive, not recruiting

Schizoaffective DisorderNot yet recruiting

Major Depressive DisorderWithdrawn

SchizophreniaCompleted

PsychosisApproved

Active, not recruiting

Alzheimer DiseaseApproved

Approved

Sleep DisorderApproved

Approved

Depressive DisorderApproved

Approved

Bipolar DisorderApproved

Approved

Alcohol DependenceApproved

Approved

Aggressive BehaviorPreclinical

Active, not recruiting

Schizoaffective DisorderPhase 1

Not yet recruiting

Major Depressive DisorderApproved

Withdrawn

SchizophreniaApproved

Completed

Showing 10 of 11 indications

Competition

Competitive Landscape

174 competitors in Schizophrenia

#DrugCompanyPhaseTrials

Rexulti

Otsuka

Approved

12 2

Ozempic

Novo Nordisk

Preclinical

1 3

Resotran

Takeda

Preclinical

1 4

Inapsine

Jazz Pharmaceuticals

Preclinical

1 5

Depakote

Ibrance

Lunesta

3 8

Luvox

SSolvay Pharmaceuticals

Preclinical

1 9

Persantine

Boehringer Ingelheim

Preclinical

1 10

Catapres

Boehringer Ingelheim

Preclinical

Ranked by pipeline maturity and clinical activity. Current drug highlighted in teal.

Timeline

Expected Milestones

Q4 2026

Recruiting

Depressive Disorder

NCT05962216

Q3 2028

Recruiting

Aggressive Behavior

NCT06875986

Q2 2029

Post-ApprovalRecruiting

Major Depression

NCT05017311

Q4 2030

Phase 1Not yet recruiting

Schizoaffective Disorder

NCT07715253

Phase 3Recruiting

Bipolar Depression

NCT04569448

Clinical

Trials by Indication[1]

Major Depressive Disorder17 trials

The Safety and Efficacy of Brexpiprazole as Adjunctive Therapy in the Treatment of Major Depressive Disorder

Terminated· Otsuka logo

Otsuka·Phase 3·NCT03487198·65 enrolled

Brexpiprazole (OPC 34712) Trial in the Treatment of Adults With Major Depressive Disorder and Irritability

Withdrawn· Otsuka logo

Otsuka·Phase 3·NCT02212613

Study of Brexpiprazole as Adjunctive Treatment of Irritability in Patients With Major Depressive Disorder and an Inadequate Response to Antidepressant Therapy

Completed· Lundbeck logo

Lundbeck·Phase 3·NCT01942785·55 enrolled

Show 14 more trials

Open-label Brexpiprazole fMRI Trial in Adults With Major Depressive Disorder and Anxiety

Withdrawn· Otsuka logo

Otsuka·Phase 4·NCT05504486

A Long-Term Study of Brexpiprazole in Patients With Major Depressive Disorder

Completed· Otsuka logo

Otsuka·Phase 3·NCT03737474·248 enrolled

A Study of Brexpiprazole in Patients With Major Depressive Disorder

Completed· Otsuka logo

Otsuka·Phase 2/3·NCT03697603·740 enrolled

Brexpiprazole as Adjunctive Therapy in Adults With Major Depressive Disorder

Completed· Otsuka logo

Otsuka·Phase 4·NCT04830215·122 enrolled

Brexpiprazole (OPC-34712) as an Adjunctive Treatment in Adults With Major Depressive Disorder and Anxiety Symptoms

Completed· Otsuka logo

Otsuka·Phase 3·NCT02013531·37 enrolled

Phase 1 Study to Assess the Safety/Tolerability of Brexpiprazole as Adjunctive Therapy in Elderly Subjects With Major Depressive Disorder

Completed· Otsuka logo

Otsuka·Phase 1·NCT01670279·18 enrolled

Study of Brexpiprazole as Adjunctive Treatment of Sleep Disturbances in Patients With Major Depressive Disorder

Completed· Lundbeck logo

Lundbeck·Phase 3·NCT01942733·44 enrolled

Long-term Safety and Tolerability Study of Brexpiprazole as Adjunctive Treatment in Patients With Major Depressive Disorder

Terminated· Lundbeck logo

Lundbeck·Phase 3·NCT01944969·26 enrolled

Brexpiprazole as Adjunctive Treatment in Patients With Major Depressive Disorder With an Inadequate Response to Antidepressant Treatment

Completed· Lundbeck logo

Lundbeck·Phase 3·NCT01838681·1,986 enrolled

A Study of Flexible-dose Brexpiprazole as Adjunctive Therapy in the Treatment of Adults With Major Depressive Disorder, the Delphinus Trial

Completed· Otsuka logo

Otsuka·Phase 3·NCT01727726·2,182 enrolled

Efficacy and Safety of Brexpiprazole as Adjunctive Treatment in Elderly Patients With Major Depressive Disorder With an Inadequate Response to Antidepressant Treatment

Terminated· Lundbeck logo

Lundbeck·Phase 3·NCT01837797·129 enrolled

A Trial to Evaluate the Efficacy, Safety & Tolerability of Brexpiprazole in the Maintenance Treatment of Adults With Major Depressive Disorder

Completed· Otsuka logo

Otsuka·Phase 3·NCT03538691·1,149 enrolled

Brexpiprazole as Adjunctive Therapy With Major Depressive Disorder and an Inadequate Response to Previous Adjunctive Therapy

Completed· Otsuka logo

Otsuka·Phase 3·NCT02012218·61 enrolled

Brexpiprazole (OPC-34712) as an Adjunctive Treatment in Active Adults, 18 to 35 Years Old, With Major Depressive Disorder Who Are in a School or Work Environment

Completed· Otsuka logo

Otsuka·Phase 3·NCT02013609·48 enrolled

Schizophrenia12 trials

Safety and Efficacy of Brexpiprazole in the Treatment of Schizophrenia

Completed· Otsuka logo

Otsuka·Phase 3·NCT03874494·371 enrolled

Brexpiprazole in Patients With Acute Schizophrenia

Completed· Lundbeck logo

Lundbeck·Phase 3·NCT01810380·468 enrolled

Monotherapy Brexpiprazole (OPC-34712) Trial in the Treatment of Adults With Schizophrenia With Impulsivity

Completed· Otsuka logo

Otsuka·Phase 3·NCT02194933·38 enrolled

Show 9 more trials

Efficacy, Safety, and Tolerability of Brexpiprazole (OPC-34712) as Maintenance Treatment in Adults With Schizophrenia

Completed· Otsuka logo

Otsuka·Phase 3·NCT01668797·524 enrolled

Safety and Tolerability of Open-Label Flexible-dose Brexpiprazole as Maintenance Treatment in Adolescents With Schizophrenia

Completed· Otsuka logo

Otsuka·Phase 3·NCT03238326·295 enrolled

Study to Assess the Safety, Tolerability and Pharmacokinetics of Oral Brexpiprazole (OPC- 34712) in Adolescents With Schizophrenia

Completed· Otsuka logo

Otsuka·Phase 1·NCT02411695·40 enrolled

Brexpiprazole (OPC-34712) Trial in the Treatment of Adults With Acute Schizophrenia

Completed· Otsuka logo

Otsuka·Phase 3·NCT02054702·97 enrolled

Trial to Evaluate the Short-term Safety & Efficacy of Brexpiprazole Monotherapy in the Treatment of Adolescents With Schizophrenia

Completed· Otsuka logo

Otsuka·Phase 3·NCT03198078·316 enrolled

Real-life Assessment of Abilify Maintena + Rexult in Schizophrenia

Recruiting·TThe University of Hong Kong··NCT05169268·10 enrolled

Monotherapy Brexpiprazole (OPC-34712) Trial in the Treatment of Adults With Early-Episode Schizophrenia

Completed· Otsuka logo

Otsuka·Phase 3·NCT02013622·49 enrolled

Brexpiprazole in Patients With Schizophrenia

Completed· Lundbeck logo

Lundbeck·Phase 3·NCT01810783·210 enrolled

Controlled Trial of Brexpiprazole For The Treatment of Co-occurring Schizophrenia and Substance Use Disorder

Completed·UUniversity of Massachusetts, Worcester·Phase 4·NCT03526354·50 enrolled

Agitation6 trials

Brexpiprazole for the Long-term Treatment of Patients With Agitation Associated With Dementia of the Alzheimer's Type

Completed· Otsuka logo

Otsuka·Phase 3·NCT03724942·164 enrolled

A Phase 3, 12-week, Multicenter, Randomized, Double-blind, Placebo-controlled Trial to Evaluate the Efficacy, Safety, and Tolerability of 2 Fixed Doses of Brexpiprazole in the Treatment of Alzheimer's Agitation

Completed· Otsuka logo

Otsuka·Phase 3·NCT01862640·433 enrolled

Safety and Tolerability Study of Flexible Dosing of Brexpiprazole in the Treatment of Subjects With Agitation Associated With Dementia of the Alzheimer's Type

Completed· Otsuka logo

Otsuka·Phase 3·NCT01922258·270 enrolled

Show 3 more trials

A 12-week Extension Trial to Evaluate the Safety and Tolerability of Brexpiprazole in the Treatment of Subjects With Agitation Associated With Dementia of the Alzheimer's Type

Completed· Otsuka logo

Otsuka·Phase 3·NCT03594123·259 enrolled

A Trial to Evaluate the Safety, Efficacy, and Tolerability of Brexpiprazole in Treating Agitation Associated With Dementia of the Alzheimer's Type

Completed· Otsuka logo

Otsuka·Phase 3·NCT03548584·345 enrolled

Brexpiprazole for the Treatment of Patients With Agitation Associated With Dementia of the Alzheimer's Type

Completed· Otsuka logo

Otsuka·Phase 2/3·NCT03620981·410 enrolled

Bipolar I Disorder3 trials

A Trial to Assess Brexpiprazole Versus Placebo for the Treatment of Acute Manic Episodes, Associated With Bipolar I Disorder

Completed· Otsuka logo

Otsuka·Phase 3·NCT03257865·333 enrolled

A Trial to Evaluate the Safety and Tolerability of Brexpiprazole in the Treatment of Participants With Bipolar I Disorder.

Completed· Otsuka logo

Otsuka·Phase 3·NCT03287869·381 enrolled

A Trial to Assess Brexpiprazole Versus Placebo for the Treatment of Acute Manic Episodes Associated With Bipolar I Disorder

Completed· Otsuka logo

Otsuka·Phase 3·NCT03259555·322 enrolled

Post-Traumatic Stress Disorder3 trials

A Study of Flexible Dose Brexpiprazole as Monotherapy or Combination Therapy in the Treatment of Adults With Post-traumatic Stress Disorder (PTSD)

Completed· Otsuka logo

Otsuka·Phase 2·NCT03033069·336 enrolled

Brexpiprazole as an Adjunctive Treatment to Paroxetine or Sertraline in Adult Patients Suffering From Post-traumatic Stress Disorder (PTSD)

Terminated· Lundbeck logo

Lundbeck·Phase 3·NCT01987960·417 enrolled

Brexpiprazole as Combination Therapy With Sertraline in the Treatment of Adults With Post-traumatic Stress Disorder

Completed· Otsuka logo

Otsuka·Phase 3·NCT04174170·591 enrolled

18 more indications

Autism Spectrum Disorder2 trials

Brexpiprazole in Treatment of Children and Adolescents With Irritability Associated With Autism Spectrum Disorder for Subjects That Have Completed Participation in 331-201-00148

Completed· Otsuka logo

Otsuka·Phase 3·NCT04258839·95 enrolled

Brexpiprazole in Treatment of Children and Adolescents With Irritability Associated With Autism Spectrum Disorder

Completed· Otsuka logo

Otsuka·Phase 3·NCT04174365·119 enrolled

Tics2 trials

The Pharmacokinetics, and Safety of Brexpiprazole Tablets in Chinese Healthy Subjects

Completed· Otsuka logo

Otsuka·Phase 1·NCT03734302·10 enrolled

The Pharmacokinetics, Tolerability and Safety of Brexpiprazole in Healthy Chinese Subjects

Completed· Otsuka logo

Otsuka·Phase 1·NCT03734354·30 enrolled

Borderline personality disorder2 trials

A Trial of Brexpiprazole in the Treatment of Borderline Personality Disorder

Completed· Otsuka logo

Otsuka·Phase 2·NCT04100096·332 enrolled

Evaluating the Safety and Tolerability of Brexpiprazole in the Treatment of Adults With Borderline Personality Disorder (BPD)

Completed· Otsuka logo

Otsuka·Phase 2/3·NCT04186403·201 enrolled

Bipolar Depression2 trials

Brexpiprazole for Bipolar Depression

Completed·UUniversity of Texas Southwestern Medical Center·Phase 4·NCT03427892·21 enrolled

Low-Dose Adjunctive Brexpiprazole in the Treatment of Bipolar I Depression: An Open-Label Study

Recruiting·DDouglas Mental Health University Institute·Phase 3·NCT04569448·58 enrolled

Depressive Disorder1 trial

Real-life Assessment of Brexpiprazole (Rexulti) in Schizophrenia and in Depressive Disorders

Recruiting·—··NCT05962216·40 enrolled

Treatment Resistant Depression (TRD)1 trial

A Study of Brexpiprazole Plus Ketamine in Treatment-Resistant Depression (TRD)

Completed·MMassachusetts General Hospital·Phase 4·NCT03149991·51 enrolled

Depression1 trial

Canadian Biomarker Integration Network for Depression (CAN-BIND) - Validation Study

Completed·UUniversity Health Network, Toronto·Phase 3·NCT04162522·1 enrolled

Alcohol Use Disorder1 trial

Brexpiprazole in Alcohol Use Disorder

Recruiting·UUniversity of Colorado, Denver·Phase 2·NCT04066192·250 enrolled

Safety and Efficacy1 trial

"Brexpiprazole (Rexulti™) Safety and Efficacy Among Filipino Patients (RAISE) - A Post Marketing Surveillance Program"

Unknown status· Otsuka logo

Otsuka··NCT04641780·300 enrolled

Cognitive impairment1 trial

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

Completed· Astellas logo

Astellas·Phase 2·NCT03557931·233 enrolled

Central Nervous System1 trial

Trial to Assess the Pharmacokinetics, Safety, Tolerability of Oral Brexpiprazole in Children (6 to <13 Years Old) With Central Nervous System Disorders

Completed· Otsuka logo

Otsuka·Phase 1·NCT03292848·24 enrolled

Treatment1 trial

A Pilot Dose-Response Biomarker Study of Brexpiprazole Treatment in PTSD

Terminated·—·Phase 2·NCT02934932·15 enrolled

TED1 trial

Bioequivalence Study to Compare Brexpiprazole 4 mg Film Coated Tablets Versus RXULTI 4 mg Film Coated Tablet (Brexpiprazole)

Completed·HHumanis Saglık Anonim Sirketi·Phase 1·NCT07266792·36 enrolled

Aggressive Behavior1 trial

REXULTI Drug General Use-results Survey (Excessive Motor Activity or Physically/Verbally Aggressive Behavior Due to Rapid Changes in Mood, Irritability, and/or Outbursts Associated With Dementia Due to Alzheimer's Disease)

Recruiting· Otsuka logo

Otsuka··NCT06875986·200 enrolled

Effectiveness1 trial

Comparison of the Effectiveness of Brexpiprazole With That of Risperidone

Withdrawn· Lundbeck logo

Lundbeck·Phase 3·NCT02758067

Major Depression1 trial

Optimized Predictive Treatment In Medications for Unipolar Major Depression (OPTIMUM-D)

Recruiting·NNova Scotia Health Authority·Phase 4·NCT05017311·400 enrolled

Combination Therapy1 trial

Brexpiprazole as Combination Therapy With Sertraline in Treatment of Adults With PTSD

Completed· Otsuka logo

Otsuka·Phase 3·NCT04124614·450 enrolled

Schizoaffective Disorder1 trial

Longitudinal PET Imaging of Antipsychotic Binding to the Dopamine-3 Receptor in Schizophrenia

Not yet recruiting·NNew York State Psychiatric Institute·Phase 1·NCT07715253·100 enrolled

Regulatory

FDA Approval Timeline[5]

Jul 10, 2015

REXULTI

NDA NDA205422

Sources

References

[1]
ClinicalTrials.gov — 63 trial records for Brexpiprazole. U.S. National Library of Medicine, National Institutes of Health.
[2]
MedlinePlus Drug Information — Rexulti drug information. U.S. National Library of Medicine, National Institutes of Health.
[3]
ChEMBL — Brexpiprazole compound record. European Bioinformatics Institute (EMBL-EBI).
[4]
Open Targets Platform — Drug–disease associations for Brexpiprazole. EMBL-EBI & Wellcome Sanger Institute.
[5]
OpenFDA — FDA approval records (NDA NDA205422). U.S. Food & Drug Administration.
[6]
FDA Orange Book — Patent and exclusivity data for Rexulti. U.S. Food & Drug Administration.
[7]
SEC EDGAR — Otsuka company filings. U.S. Securities and Exchange Commission.

Details

Drug Info

Quick Facts

Mechanism of Action: Serotonin 2a (5-Ht2a) Receptor Antagonist; Serotonin 1a (5-Ht1a) Receptor Partial Agonist; Dopamine D2 Receptor Partial Agonist[3]
Modality: Small molecule[3]
Highest Phase: Approved[1]
Company: Otsuka

Patent Landscape[6]

Patent Cliff

Oct 12, 2026

Earliest patent expiration — generic entry possible after this date

Patent #Expires

7888362Apr 12, 2026

8349840Apr 12, 2026

9839637Apr 12, 2026

8618109Apr 12, 2026

9839637*PEDOct 12, 2026

7 more patents

8618109*PEDOct 12, 2026

7888362*PEDOct 12, 2026

8349840*PEDOct 12, 2026

RE48059Dec 23, 2028

RE48059*PEDJun 23, 2029

10307419Oct 12, 2032

10307419*PEDApr 12, 2033

Rexulti

Status by Indication[4][1]

Competitive Landscape

Expected Milestones

Q4 2026

Q3 2028

Q2 2029

Q4 2030

Trials by Indication[1]

Major Depressive Disorder17 trials

Schizophrenia12 trials

Agitation6 trials

Bipolar I Disorder3 trials

Post-Traumatic Stress Disorder3 trials

Autism Spectrum Disorder2 trials

Tics2 trials

Borderline personality disorder2 trials

Bipolar Depression2 trials

Depressive Disorder1 trial

Treatment Resistant Depression (TRD)1 trial

Depression1 trial

Alcohol Use Disorder1 trial

Safety and Efficacy1 trial

Cognitive impairment1 trial

Central Nervous System1 trial

Treatment1 trial

TED1 trial

Aggressive Behavior1 trial

Effectiveness1 trial

Major Depression1 trial

Combination Therapy1 trial

Schizoaffective Disorder1 trial

FDA Approval Timeline[5]

References

Drug Info

Quick Facts

Patent Landscape[6]

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