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Brexpiprazole

Generic Name
Brexpiprazole
Brand Names
Rxulti, Rexulti
Drug Type
Small Molecule
Chemical Formula
C25H27N3O2S
CAS Number
913611-97-9
Unique Ingredient Identifier
2J3YBM1K8C

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.

Background

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)

FDA Approved Products

Rexulti
Manufacturer:Otsuka America Pharmaceutical, Inc.
Route:ORAL
Strength:1 mg in 1 1
Approved: 2023/05/15
NDC:59148-037
Brexpiprazole
Manufacturer:Ajanta Pharma USA Inc.
Route:ORAL
Strength:0.25 mg in 1 1
Approved: 2022/12/13
NDC:27241-204
Brexpiprazole
Manufacturer:Ajanta Pharma USA Inc.
Route:ORAL
Strength:2 mg in 1 1
Approved: 2022/12/13
NDC:27241-207
Brexpiprazole
Manufacturer:Camber Pharmaceuticals, Inc.
Route:ORAL
Strength:3 mg in 1 1
Approved: 2024/01/08
NDC:31722-438
brexpiprazole
Manufacturer:Amneal Pharmaceuticals NY LLC
Route:ORAL
Strength:0.25 mg in 1 1
Approved: 2024/03/26
NDC:60219-1649

Singapore Approved Products

REXULTI FILM-COATED TABLETS 1MG
Manufacturer:OTSUKA PHARMACEUTICAL CO., LTD. (TOKUSHIMA FACTORY), ELAIAPHARM (PRIMARY AND SECONDARY PACKAGER), OTSUKA PHARMACEUTICAL CO., LTD. (SECOND TOKUSHIMA FACTORY) (Finished Product Manufacturer)
Form:TABLET, FILM COATED
Strength:1mg
Online:Yes
Approved: 2019/08/05
Approval:SIN15766P
REXULTI FILM-COATED TABLETS 2MG
Manufacturer:OTSUKA PHARMACEUTICAL CO., LTD. (TOKUSHIMA FACTORY), ELAIAPHARM (PRIMARY AND SECONDARY PACKAGER), OTSUKA PHARMACEUTICAL CO., LTD. (SECOND TOKUSHIMA FACTORY) (Finished Product Manufacturer)
Form:TABLET, FILM COATED
Strength:2mg
Online:Yes
Approved: 2019/08/05
Approval:SIN15765P
REXULTI FILM-COATED TABLETS 3MG
Manufacturer:OTSUKA PHARMACEUTICAL CO., LTD. (TOKUSHIMA FACTORY), ELAIAPHARM (PRIMARY AND SECONDARY PACKAGER), OTSUKA PHARMACEUTICAL CO., LTD. (SECOND TOKUSHIMA FACTORY) (Finished Product Manufacturer)
Form:TABLET, FILM COATED
Strength:3mg
Online:Yes
Approved: 2019/08/05
Approval:SIN15764P
REXULTI FILM-COATED TABLETS 4MG
Manufacturer:OTSUKA PHARMACEUTICAL CO., LTD. (TOKUSHIMA FACTORY), ELAIAPHARM (PRIMARY AND SECONDARY PACKAGER), OTSUKA PHARMACEUTICAL CO., LTD. (SECOND TOKUSHIMA FACTORY) (Finished Product Manufacturer)
Form:TABLET, FILM COATED
Strength:4mg
Online:Yes
Approved: 2019/08/05
Approval:SIN15763P
REXULTI FILM-COATED TABLETS 0.25MG
Manufacturer:OTSUKA PHARMACEUTICAL CO., LTD. (TOKUSHIMA FACTORY), ELAIAPHARM (PRIMARY AND SECONDARY PACKAGER), OTSUKA PHARMACEUTICAL CO., LTD. (SECOND TOKUSHIMA FACTORY) (Finished Product Manufacturer)
Form:TABLET, FILM COATED
Strength:0.25mg
Online:Yes
Approved: 2019/08/05
Approval:SIN15768P

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