Overview
Brexpiprazole is an atypical antipsychotic and a novel D2 dopamine and serotonin 1A partial agonist called serotonin-dopamine activity modulator (SDAM). It has a high affinity for serotonin, dopamine and alpha (α)-adrenergic receptors. Although it is structurally similar to aripiprazole, brexpiprazole has different binding affinities for dopamine and serotonin receptors. Compared to aripiprazole, brexpiprazole has less potential for partial agonist-mediated adverse effects such as extrapyramidal symptoms, which is attributed to lower intrinsic activity at the D2 receptor. It also displays stronger antagonism at the 5-HT1A and 5-HT2A receptors. Brexpiprazole was first approved by the FDA on July 10, 2015. Currently approved for the treatment of depression, schizophrenia, and agitation associated with dementia due to Alzheimer’s disease, brexpiprazole has also been investigated in other psychiatric disorders, such as post-traumatic stress disorder.
Indication
Brexpiprazole is indicated as adjunctive therapy to antidepressants for the treatment of major depressive disorder in adults. It is also indicated for the treatment of schizophrenia in patients 13 years of age and older. Brexpiprazole is also indicated for the treatment of agitation associated with dementia due to Alzheimer’s disease; however, it is not indicated as an as-needed (“prn”) treatment for this condition.
Associated Conditions
- Agitation
- Schizophrenia
- Major Depressive Disorder (MDD)
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2024/11/05 | Phase 1 | Recruiting | |||
2023/09/13 | Phase 1 | Completed | |||
2023/07/27 | N/A | Recruiting | Dr. Albert Kar-Kin Chung | ||
2022/08/17 | Phase 4 | Withdrawn | |||
2022/04/13 | Phase 3 | Active, not recruiting | |||
2022/04/13 | Phase 3 | Recruiting | |||
2021/12/23 | N/A | Recruiting | |||
2021/11/15 | Phase 1 | Withdrawn | |||
2021/08/23 | Phase 4 | Recruiting | |||
2021/04/05 | Phase 4 | Completed |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Ajanta Pharma USA Inc. | 27241-207 | ORAL | 2 mg in 1 1 | 12/13/2022 | |
| Camber Pharmaceuticals, Inc. | 31722-435 | ORAL | 0.5 mg in 1 1 | 1/8/2024 | |
| Amneal Pharmaceuticals NY LLC | 60219-1653 | ORAL | 3 mg in 1 1 | 6/27/2025 | |
| Amneal Pharmaceuticals NY LLC | 60219-1654 | ORAL | 4 mg in 1 1 | 6/27/2025 | |
| Otsuka America Pharmaceutical, Inc. | 59148-040 | ORAL | 4 mg in 1 1 | 5/15/2023 | |
| Amneal Pharmaceuticals NY LLC | 60219-1651 | ORAL | 1 mg in 1 1 | 6/27/2025 | |
| Ajanta Pharma USA Inc. | 27241-208 | ORAL | 3 mg in 1 1 | 12/13/2022 | |
| Otsuka America Pharmaceutical, Inc. | 59148-036 | ORAL | 0.5 mg in 1 1 | 5/15/2023 | |
| Ajanta Pharma USA Inc. | 27241-204 | ORAL | 0.25 mg in 1 1 | 12/13/2022 | |
| Amneal Pharmaceuticals NY LLC | 60219-1649 | ORAL | 0.25 mg in 1 1 | 6/27/2025 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
Authorised | 7/26/2018 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| REXULTI FILM-COATED TABLETS 1MG | SIN15766P | TABLET, FILM COATED | 1mg | 8/5/2019 | |
| REXULTI FILM-COATED TABLETS 2MG | SIN15765P | TABLET, FILM COATED | 2mg | 8/5/2019 | |
| REXULTI FILM-COATED TABLETS 3MG | SIN15764P | TABLET, FILM COATED | 3mg | 8/5/2019 | |
| REXULTI FILM-COATED TABLETS 4MG | SIN15763P | TABLET, FILM COATED | 4mg | 8/5/2019 | |
| REXULTI FILM-COATED TABLETS 0.25MG | SIN15768P | TABLET, FILM COATED | 0.25mg | 8/5/2019 | |
| REXULTI FILM-COATED TABLETS 0.5MG | SIN15767P | TABLET, FILM COATED | 0.5mg | 8/5/2019 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| Brexpiprazole Tablet | 国药准字HJ20240049 | 化学药品 | 片剂 | 6/25/2024 | |
| Brexpiprazole Tablet | 国药准字HJ20240050 | 化学药品 | 片剂 | 6/25/2024 | |
| Brexpiprazole Tablet | 国药准字HJ20240051 | 化学药品 | 片剂 | 6/25/2024 |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| REXULTI brexpiprazole 1 mg film coated tablet blister pack | 273220 | Medicine | A | 5/19/2017 | |
| REXULTI brexpiprazole 3 mg film coated tablet blister pack | 273221 | Medicine | A | 5/19/2017 | |
| REXULTI brexpiprazole 2 mg film coated tablet blister pack | 273223 | Medicine | A | 5/19/2017 | |
| REXULTI brexpiprazole 0.5 mg film coated tablet blister pack | 273222 | Medicine | A | 5/19/2017 | |
| REXULTI brexpiprazole 4 mg film coated tablet blister pack | 273224 | Medicine | A | 5/19/2017 | |
| REXULTI brexpiprazole 0.25 mg film coated tablet blister pack | 273225 | Medicine | A | 5/19/2017 |
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