Brexpiprazole

Generic Name: Brexpiprazole

Brand Names: Rxulti, Rexulti

Drug Type: Small Molecule

Chemical Formula: C_₂₅H_₂₇N_₃O_₂S

CAS Number: 913611-97-9

Unique Ingredient Identifier: 2J3YBM1K8C

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)

Clinical Trials

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

Phase 3

Completed

Conditions: Agitation Associated With Alzheimer's Dementia
Alzheimer Dementia

Interventions: Drug: Brexpiprazole
Other: Placebo

First Posted Date: 2018-06-07

Last Posted Date: 2023-09-18

Lead Sponsor: Otsuka Pharmaceutical Development & Commercialization, Inc.

Target Recruit Count: 345

Registration Number: NCT03548584

Locations: 🇺🇸
For additional information regarding sites, contact 844-687-8522, Los Angeles, California, United States

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

Phase 3

Completed

Conditions: Major Depressive Disorder

Interventions: Drug: Brexpiprazole
Drug: Antidepressant therapy

First Posted Date: 2018-05-29

Last Posted Date: 2023-10-12

Lead Sponsor: Otsuka Pharmaceutical Development & Commercialization, Inc.

Target Recruit Count: 1149

Registration Number: NCT03538691

Locations: 🇺🇸
For additional information regarding sites, contact 844-687-8522, Los Angeles, California, United States

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

Phase 4

Completed

Conditions: Schizophrenia
Schizoaffective Disorder
Substance Use Disorders

Interventions: Drug: Brexpiprazole
Other: Treatment as Usual

First Posted Date: 2018-05-16

Last Posted Date: 2024-03-20

Lead Sponsor: University of Massachusetts, Worcester

Target Recruit Count: 52

Registration Number: NCT03526354

Locations: 🇺🇸
UMass Medical School, Worcester, Massachusetts, United States
🇺🇸
Massachusetts General Hospital, Boston, Massachusetts, United States
🇺🇸
Augusta University, Augusta, Georgia, United States

and more 1 locations

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

Phase 3

Terminated

Conditions: Major Depressive Disorder

Interventions: Drug: Placebo
Drug: Brexpiprazole

First Posted Date: 2018-04-03

Last Posted Date: 2020-12-29

Lead Sponsor: Otsuka Beijing Research Institute

Target Recruit Count: 65

Registration Number: NCT03487198

Locations: 🇨🇳
Beijing Anding Hospital of Capital Medical University, Beijing, Beijing, China

Brexpiprazole for Bipolar Depression

Phase 4

Completed

Conditions: Bipolar Depression

Interventions: Drug: Brexpiprazole

First Posted Date: 2018-02-09

Last Posted Date: 2019-03-13

Lead Sponsor: University of Texas Southwestern Medical Center

Target Recruit Count: 21

Registration Number: NCT03427892

Locations: 🇺🇸
UT Southwestern Medical Center, Dallas, Texas, United States

Brexpiprazole in Borderline Personality Disorder

Phase 2

Completed

Conditions: Borderline Personality Disorder

Interventions: Drug: Placebo
Drug: Rexulti

First Posted Date: 2018-02-01

Last Posted Date: 2022-03-18

Lead Sponsor: University of Chicago

Target Recruit Count: 80

Registration Number: NCT03418675

Locations: 🇺🇸
University of Chicago, Chicago, Illinois, United States

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

Phase 1

Completed

Conditions: Bipolar I Disorder
ADHD
Autism
Conduct Disorder
Oppositional Defiant Disorder

Interventions: Drug: Brexpiprazole

First Posted Date: 2017-09-26

Last Posted Date: 2018-06-12

Lead Sponsor: Otsuka Pharmaceutical Development & Commercialization, Inc.

Target Recruit Count: 24

Registration Number: NCT03292848

Locations: 🇺🇸
Woodland Research Northwest, LLC, Rogers, Arkansas, United States
🇺🇸
Alliance for Wellness dba Alliance for Research, Long Beach, California, United States
🇺🇸
Cutting Edge Research Group, Oklahoma City, Oklahoma, United States

and more 6 locations

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

Phase 3

Completed

Conditions: Acute Mania
Bipolar I Disorder

Interventions: Drug: Brexpiprazole

First Posted Date: 2017-09-19

Last Posted Date: 2020-08-17

Lead Sponsor: Otsuka Pharmaceutical Development & Commercialization, Inc.

Target Recruit Count: 381

Registration Number: NCT03287869

Locations: 🇺🇸
Woodland Research Northwest, LLC, Rogers, Arkansas, United States
🇧🇬
"Mental Health Centre-Ruse" EOOD, Male department for persons with severe mental disorders, Female department for persons with severe mental disorders, Ruse, Bulgaria
🇵🇱
Indywidualna Specjalistyczna Praktyka Lekarska Wieslaw Jerzy Cubala, Gdańsk, Poland

and more 68 locations

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

Phase 3

Completed

Conditions: Bipolar I Disorder
Manic Episode

Interventions: Drug: Placebo
Drug: Brexpiprazole

First Posted Date: 2017-08-23

Last Posted Date: 2020-02-10

Lead Sponsor: Otsuka Pharmaceutical Development & Commercialization, Inc.

Target Recruit Count: 322

Registration Number: NCT03259555

Locations: 🇺🇸
Galiz Research, Hialeah, Florida, United States
🇺🇸
Ci Trials, Riverside, California, United States
🇺🇸
Richard H Weisler, MD, PA, and Associates, Raleigh, North Carolina, United States

and more 44 locations

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

Phase 3

Completed

Conditions: Bipolar I Disorder
Manic Episode

Interventions: Drug: Brexpiprazole
Drug: Placebo

First Posted Date: 2017-08-22

Last Posted Date: 2020-02-11

Lead Sponsor: Otsuka Pharmaceutical Development & Commercialization, Inc.

Target Recruit Count: 333

Registration Number: NCT03257865

Locations: 🇺🇸
CiTrials, Santa Ana, California, United States
🇺🇸
Research Centers of America LLC, Hollywood, Florida, United States
🇺🇸
CNRI-San Diego, San Diego, California, United States

and more 34 locations

Drug Development Updates

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