REXULTI (brexpiprazole)
REXULTI is indicated for the treatment of Major Depressive Disorder; Schizophrenia; Agitation associated with Dementia due to Alzheimer's Disease.
How REXULTI Works
Brexpiprazole is a serotonin-dopamine activity modulator (SDAM). While its precise mechanism is not fully established, its efficacy is thought to be mediated through a combination of partial agonist activity at serotonin 5-HT1A and dopamine D2 receptors, and antagonist activity at serotonin 5-HT2A receptors. It also demonstrates high affinity (antagonist activity) for noradrenergic alpha-1B and alpha-2C receptors. Compared to earlier atypical antipsychotics like aripiprazole, brexpiprazole has lower intrinsic activity at the D2 receptor and higher affinity for 5-HT1A and 5-HT2A receptors.
Development Insights
Details
- Status
- Prescription
- First Approved
- 2015-07-10
- Patent Cliff
- 2033
- Routes
- ORAL
- Dosage Forms
- TABLET
REXULTI Approval History
What REXULTI Treats
3 indicationsREXULTI is approved for 3 conditions since its original approval in 2015. These indications span multiple therapeutic areas including oncology, immunology, and more.
- Major Depressive Disorder
- Schizophrenia
- Agitation associated with Dementia due to Alzheimer's Disease
REXULTI Boxed Warning
INCREASED MORTALITY IN ELDERLY PATIENTS WITH DEMENTIA-RELATED PSYCHOSIS and SUICIDAL THOUGHTS AND BEHAVIORS WARNING: INCREASED MORTALITY IN ELDERLY PATIENTS WITH DEMENTIA-RELATED PSYCHOSIS and SUICIDAL THOUGHTS AND BEHAVIORS See full prescribing information for complete boxed warning. Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at increased risk of death. REXULTI is not approved for the treatment of patients with dementia-related psychosis without agitat...
WARNING: INCREASED MORTALITY IN ELDERLY PATIENTS WITH DEMENTIA-RELATED PSYCHOSIS and SUICIDAL THOUGHTS AND BEHAVIORS WARNING: INCREASED MORTALITY IN ELDERLY PATIENTS WITH DEMENTIA-RELATED PSYCHOSIS and SUICIDAL THOUGHTS AND BEHAVIORS See full prescribing information for complete boxed warning. Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at increased risk of death. REXULTI is not approved for the treatment of patients with dementia-related psychosis without agitation associated with dementia due to Alzheimer's disease. ( 5.1 ) Antidepressants increased the risk of suicidal thoughts and behaviors in pediatric and young adult patients. Closely monitor all antidepressant-treated patients for clinical worsening and emergence of suicidal thoughts and behaviors. Safety and effectiveness of REXULTI have not been established in pediatric patients with MDD. ( 5.2 , 8.4 ) 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. REXULTI is not approved for the treatment of patients with dementia-related psychosis without agitation associated with dementia due to Alzheimer's disease [see Warnings and Precautions (5.1) ] . Suicidal Thoughts and Behaviors Antidepressants increased the risk of suicidal thoughts and behaviors in pediatric patients and young adult patients in short-term studies. Closely monitor all antidepressant-treated patients for clinical worsening, and for emergence of suicidal thoughts and behaviors [see Warnings and Precautions (5.2) ] . The safety and effectiveness of REXULTI have not been established in pediatric patients with MDD [see Warnings and Precautions (5.2) , Use in Specific Populations (8.4) ] .
REXULTI Competitive Set
ProThree rings of competition based on shared molecular targets and treated indications.
Indication competitors
Same indication, different mechanism — what else might this patient receive?
Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.
Drugs Similar to REXULTI
3 of 20FDA-approved drugs for similar conditions. Compare mechanisms and indications to understand treatment alternatives.
Clinical Trial Registry
53 trials| Trial | Sponsor ID | Phase | Status | Title |
|---|---|---|---|---|
| NCT04066192 | 19-1658 1R01AA027765-01 | Ph 2 | recruiting | Brexpiprazole in Alcohol Use Disorder |
| NCT05017311 CAN-BIND-17 | 1027397 | Ph 4 | recruiting | Optimized Predictive Treatment In Medications for Unipolar Major Depression (OPTIMUM-D) |
| NCT03238326 results posted | 331-10-236 | Ph 3 | completed | Safety and Tolerability of Open-Label Flexible-dose Brexpiprazole as Maintenance Treatment in Adolescents With Schizophrenia |
| NCT04174365 results posted | 331-201-00148 | Ph 3 | completed | Brexpiprazole in Treatment of Children and Adolescents With Irritability Associated With Autism Spectrum Disorder |
| NCT04124614 results posted | 331-201-00071 | Ph 3 | completed | Brexpiprazole as Combination Therapy With Sertraline in Treatment of Adults With PTSD |
| NCT04174170 results posted | 331-201-00072 | Ph 3 | completed | Brexpiprazole as Combination Therapy With Sertraline in the Treatment of Adults With Post-traumatic Stress Disorder |
| NCT03526354 results posted | 14611 | Ph 4 | completed | Controlled Trial of Brexpiprazole For The Treatment of Co-occurring Schizophrenia and Substance Use Disorder |
| NCT03874494 | 331-403-00027 | Ph 3 | completed | Safety and Efficacy of Brexpiprazole in the Treatment of Schizophrenia |
| NCT03620981 results posted | 331-102-00088 | Ph 2, Ph 3 | completed | Brexpiprazole for the Treatment of Patients With Agitation Associated With Dementia of the Alzheimer's Type |
| NCT03557931 results posted | 4345-CL-0015 | Ph 2 | completed | 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 |
| NCT04186403 results posted | 331-201-00195 2019-002897-30 | Ph 2, Ph 3 | completed | Evaluating the Safety and Tolerability of Brexpiprazole in the Treatment of Adults With Borderline Personality Disorder (BPD) |
| NCT03724942 results posted | 331-102-00184 JapicCTI-184179 | Ph 3 | completed | Brexpiprazole for the Long-term Treatment of Patients With Agitation Associated With Dementia of the Alzheimer's Type |
| NCT03697603 results posted | 331-102-00058 | Ph 2, Ph 3 | completed | A Study of Brexpiprazole in Patients With Major Depressive Disorder |
| NCT04569448 | RSS 5182913 | Ph 3 | recruiting | Brexpiprazole Treatment for Bipolar I Depression |
| NCT04100096 results posted | 331-201-00242 | Ph 2 | completed | A Trial of Brexpiprazole in the Treatment of Borderline Personality Disorder |
| NCT04258839 results posted | 331-201-00191 2018-004899-35 | Ph 3 | completed | Brexpiprazole in Treatment of Children and Adolescents With Irritability Associated With Autism Spectrum Disorder for Subjects That Have Completed Participation in 331-201-00148 |
| NCT03737474 results posted | 331-102-00059 | Ph 3 | completed | A Long-Term Study of Brexpiprazole in Patients With Major Depressive Disorder |
| NCT04830215 results posted | 331-201-00289 | Ph 4 | completed | Brexpiprazole as Adjunctive Therapy in Adults With Major Depressive Disorder |
| NCT03594123 results posted | 331-201-00182 | Ph 3 | completed | 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 |
| NCT03734302 | 331-403-00025 | Ph 1 | completed | The Pharmacokinetics, and Safety of Brexpiprazole Tablets in Chinese Healthy Subjects |
| NCT03734354 | 331-403-00024 | Ph 1 | completed | The Pharmacokinetics, Tolerability and Safety of Brexpiprazole in Healthy Chinese Subjects |
| NCT03538691 results posted | 331-201-00079 2018-000601-22 | Ph 3 | completed | A Trial to Evaluate the Efficacy, Safety & Tolerability of Brexpiprazole in the Maintenance Treatment of Adults With Major Depressive Disorder |
| NCT03548584 results posted | 331-14-213 | Ph 3 | completed | A Trial to Evaluate the Safety, Efficacy, and Tolerability of Brexpiprazole in Treating Agitation Associated With Dementia of the Alzheimer's Type |
| NCT04162522 | 19-5371 | Ph 3 | completed | Canadian Biomarker Integration Network for Depression (CAN-BIND) - Validation Study |
| NCT05504486 | 331-201-00376 | Ph 4 | withdrawn | Open-label Brexpiprazole fMRI Trial in Adults With Major Depressive Disorder and Anxiety |
| NCT03418675 results posted | 17-1729 | Ph 2 | completed | Brexpiprazole in Borderline Personality Disorder |
| NCT03033069 results posted | 331-201-00061 | Ph 2 | completed | A Study of Flexible Dose Brexpiprazole as Monotherapy or Combination Therapy in the Treatment of Adults With Post-traumatic Stress Disorder (PTSD) |
| NCT03487198 | 331-403-00023 | Ph 3 | terminated | The Safety and Efficacy of Brexpiprazole as Adjunctive Therapy in the Treatment of Major Depressive Disorder |
| NCT03287869 results posted | 331-201-00083 2017-002225-38 | Ph 3 | completed | A Trial to Evaluate the Safety and Tolerability of Brexpiprazole in the Treatment of Participants With Bipolar I Disorder. |
| NCT03149991 results posted | KETBREX001 | Ph 4 | completed | A Study of Brexpiprazole Plus Ketamine in Treatment-Resistant Depression (TRD) |
| NCT03257865 results posted | 331-201-00081 | Ph 3 | completed | A Trial to Assess Brexpiprazole Versus Placebo for the Treatment of Acute Manic Episodes, Associated With Bipolar I Disorder |
| NCT03259555 results posted | 331-201-00080 | Ph 3 | completed | A Trial to Assess Brexpiprazole Versus Placebo for the Treatment of Acute Manic Episodes Associated With Bipolar I Disorder |
| NCT01942733 results posted | 15352A | Ph 3 | completed | Study of Brexpiprazole as Adjunctive Treatment of Sleep Disturbances in Patients With Major Depressive Disorder |
| NCT03427892 results posted | 102016-048 | Ph 4 | completed | Brexpiprazole for Bipolar Depression |
| NCT02934932 results posted | Pro00071923 | Ph 2 | terminated | A Pilot Dose-Response Biomarker Study of Brexpiprazole Treatment in PTSD |
| NCT02194933 results posted | 331-13-009 | Ph 3 | completed | Monotherapy Brexpiprazole (OPC-34712) Trial in the Treatment of Adults With Schizophrenia With Impulsivity |
| NCT01944969 results posted | 14767B 2012-004169-42 | Ph 3 | terminated | Long-term Safety and Tolerability Study of Brexpiprazole as Adjunctive Treatment in Patients With Major Depressive Disorder |
| NCT03292848 | 331-201-00103 | Ph 1 | completed | Trial to Assess the Pharmacokinetics, Safety, Tolerability of Oral Brexpiprazole in Children (6 to <13 Years Old) With Central Nervous System Disorders |
| NCT01727726 results posted | 331-12-282 | Ph 3 | completed | A Study of Flexible-dose Brexpiprazole as Adjunctive Therapy in the Treatment of Adults With Major Depressive Disorder, the Delphinus Trial |
| NCT01838681 results posted | 14570A 2012-001380-76 | Ph 3 | completed | Brexpiprazole as Adjunctive Treatment in Patients With Major Depressive Disorder With an Inadequate Response to Antidepressant Treatment |
| NCT01810783 results posted | 14644B 2012-002705-21 | Ph 3 | completed | Brexpiprazole in Patients With Schizophrenia |
| NCT01810380 results posted | 14644A 2012-002252-17 | Ph 3 | completed | Brexpiprazole in Patients With Acute Schizophrenia |
| NCT01987960 results posted | 14865A 2012-004982-41 | Ph 3 | terminated | Brexpiprazole as an Adjunctive Treatment to Paroxetine or Sertraline in Adult Patients Suffering From Post-traumatic Stress Disorder (PTSD) |
| NCT01668797 EQUATOR results posted | 331-10-232 2011-005766-38 | Ph 3 | completed | Efficacy, Safety, and Tolerability of Brexpiprazole (OPC-34712) as Maintenance Treatment in Adults With Schizophrenia |
| NCT02758067 TAILWIND | 16758A 2015-001749-97 | Ph 3 | withdrawn | Comparison of the Effectiveness of Brexpiprazole With That of Risperidone |
| NCT02212613 | 331-13-004 | Ph 3 | withdrawn | Brexpiprazole (OPC 34712) Trial in the Treatment of Adults With Major Depressive Disorder and Irritability |
| NCT02013531 results posted | 331-13-002 | Ph 3 | completed | Brexpiprazole (OPC-34712) as an Adjunctive Treatment in Adults With Major Depressive Disorder and Anxiety Symptoms |
| NCT02013622 results posted | 331-13-006 | Ph 3 | completed | Monotherapy Brexpiprazole (OPC-34712) Trial in the Treatment of Adults With Early-Episode Schizophrenia |
| NCT02013609 results posted | 331-13-003 | Ph 3 | completed | 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 |
| NCT01942785 results posted | 15353A | Ph 3 | completed | Study of Brexpiprazole as Adjunctive Treatment of Irritability in Patients With Major Depressive Disorder and an Inadequate Response to Antidepressant Therapy |
Showing 50 of 53 trials
Active Pipeline
Ongoing clinical trials by development phase
Key Completed Trials
Completed studies with published results, ranked by significance
Trial Timeline
Full development history with FDA approval milestones
Understanding FDA Approval Types
| Count | Type | What it means |
|---|---|---|
| - | ORIG | Original approval - drug first enters market |
| - | SUPPL - Efficacy | New indication (new disease/condition approved) |
| - | SUPPL - Labeling | Label text changes (warnings, dosing updates) |
| - | SUPPL - Manufacturing | Production changes (new facility) |
| - | SUPPL - Chemistry | Formulation changes (new dosage strength) |
Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.
REXULTI FDA Label Details
Indications & Usage
FDA Label (PDF)REXULTI is indicated for the treatment of Major Depressive Disorder; Schizophrenia; Agitation associated with Dementia due to Alzheimer's Disease.
WARNING: INCREASED MORTALITY IN ELDERLY PATIENTS WITH DEMENTIA-RELATED PSYCHOSIS and SUICIDAL THOUGHTS AND BEHAVIORS WARNING: INCREASED MORTALITY IN ELDERLY PATIENTS WITH DEMENTIA-RELATED PSYCHOSIS and SUICIDAL THOUGHTS AND BEHAVIORS See full prescribing information for complete boxed warning. Elder...
REXULTI Patents & Exclusivity
Patents (11 active)
Exclusivity
Pro Intelligence Preview
Deep insights for REXULTI
Revenue Insights
- • Quarterly revenue tracking
- • Historical trend analysis
Patent Timeline
- • Cliff: 2033
- • 492 active patents
Trial Analysis
- • 55 total trials
- • Stage: Declining
Competitive Landscape
- • 20 similar drugs
- • Same target/indication analysis
Full approval history • All patents • Revenue trends • Competitor analysis
Related Intelligence
Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.
How We Calculate These Metrics
Trial Activity Stage
Measures the current development activity pattern based on trial phases, status, and trends. Important: This measures R&D activity, not commercial lifecycle.
Trial statuses: "Active" means recruiting or ongoing. "Completed" means reached planned endpoint. "Terminated" means stopped early—often due to safety, efficacy, or business reasons.
- Growth: High proportion of early-phase trials (Phase 1/2), active development
- Expansion: Significant Phase 3 activity, approaching or pursuing approvals
- Mature: Substantial Phase 4 post-marketing studies
- Stable: Mixed phase distribution, steady development
- Declining: Low active trial ratio, reduced R&D investment