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brexpiprazole

Trade name: rexulti

Small moleculeapproved

Approved

Jul 10, 2015

Brexpiprazole is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors. Brexpiprazole is approved for the treatment of schizophrenia, and as an adjunctive treatment for major depressive disorder (MDD). Although it failed Phase II clinical trials for ADHD, it has been designed to provide improved efficacy and tolerability (e.g., less akathisia, restlessness and/or insomnia) over established adjunctive treatments for major depressive disorder (MDD).Brexpiprazole is sold under the brand name Rexulti. Although the mechanism of action of brexpiprazole in the treatment of MDD and schizophrenia is unclear, the efficacy of brexpiprazole may be attributed to partial agonist activity at serotonin 1A and dopamine D2 receptors, and antagonist activity at serotonin 2A receptors. — NCATS

Clinical trial activity

88 trials · 29 clinical orgs · 20 marketing orgs

Phase 1
17
Phase 2
60
Phase 3
52
Phase 4
6

Earliest trial started Dec 1, 2008 (NCT00805454)

Timeline

2000s

  1. Jan 1, 2008

    Otsuka — Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 2009

    Otsuka — Earliest Phase 2 Sponsor(trial)

2010s

  1. Jan 1, 2011

    Otsuka — Earliest Phase 3 Sponsor(trial)

  2. Jul 10, 2015

    Otsuka — Earliest FDA Approval

  3. Jul 10, 2015

    Otsuka — Marketing Organization

  4. Jul 10, 2015

    Otsuka — NDA Organization

2020s

  1. Aug 17, 2021

    Accord Research — Marketing Organization

  2. Aug 23, 2021

    Ajanta Pharma Ltd — Marketing Organization

  3. Sep 8, 2021

    Zydus Discovery DMCC — Marketing Organization

  4. Sep 27, 2021

    Alkem Labs Ltd — Marketing Organization

  5. Aug 11, 2022

    Teva — Marketing Organization

  6. Aug 29, 2022

    ZENARA — Marketing Organization

  7. Sep 26, 2022

    Sandoz — Marketing Organization

  8. Sep 26, 2022

    Novartis — Marketing Organization

  9. Jan 25, 2023

    MSN Laboratories — Marketing Organization

  10. Jan 31, 2023

    Amneal Pharmaceuticals — Marketing Organization

  11. Mar 7, 2023

    Alembic — Marketing Organization

  12. Mar 18, 2023

    Lupin — Marketing Organization

  13. Mar 21, 2023

    Prinston Inc — Marketing Organization

  14. Oct 25, 2023

    ANDA Repository — Marketing Organization

  15. Oct 25, 2023

    OPTIMUS PHARMA PRIVATE LTD — Marketing Organization

  16. Oct 25, 2023

    Chartwell Pharmaceuticals — Marketing Organization

  17. Nov 2, 2023

    Aurobindo Pharma — Marketing Organization

  18. Nov 20, 2023

    Hetero Labs Ltd — Marketing Organization

  19. Feb 24, 2025

    Apotex — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedJul 10, 2015

Chemistry & pharmacology

Loading structure…

SMILES

O=C1NC2=C(C=C1)C=CC(OCCCCN3CCN(CC3)C4=CC=CC5=C4C=CS5)=C2
Mol. weight
433.566 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Black box warning

Sources

Also known as

  • 7-(4-(4-(1-benzothiophen-4-yl)piperazin-1-yl)butoxy)quinolin-2(1h)-one
  • brexpiprazole
  • brexpiprazole
  • brexpiprazole
  • brexpiprazole
  • brexpiprazole
  • brexpiprazole
  • brexpiprazole
  • brexpiprazole
  • brexpiprazole
  • brexpiprazole
  • brexpiprazole
  • opc 34712
  • opc-34712
  • opc-34712
  • opc-34712
  • opc-34712
  • rexulti
  • rexulti
  • rexulti

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06674694Phase 1Apr 10, 2024Sichuan Kelun Pharmaceutical Research Institute Co., Ltd.
NCT06036108Phase 1Oct 3, 2023Otsuka
NCT05504486Phase 4Aug 29, 2022Lundbeck, Otsuka
NCT05325645Phase 3Jul 21, 2022Otsuka
NCT05326347Phase 3May 31, 2022Otsuka
NCT05119894Phase 1Nov 30, 2021Otsuka
NCT05017311Phase 4Sep 1, 2021Dalhousie University, McGill University, McMaster University, Queen's University, Belfast, Simon Fraser University, Unity Health Toronto, University of British Columbia, University of Calgary, University of Michigan, University of Ottawa, University of Toronto
NCT04830215Phase 4Apr 30, 2021Lundbeck, Otsuka
NCT04569448Phase 3Dec 31, 2020McGill University, McMaster University
NCT04186403Phase 2/Phase 3 (Phase 3)Jan 31, 2020Otsuka
NCT04258839Phase 3Jan 17, 2020Lundbeck, Otsuka
NCT04066192Phase 2Jan 1, 2020National Institute on Alcohol Abuse and Alcoholism (NIAAA), University of Colorado, Denver
NCT04162522Phase 3Dec 15, 2019Dalhousie University, McGill University, McMaster University, Queen's University, Belfast, Simon Fraser University, Unity Health Toronto, University of British Columbia, University of Calgary, University of Michigan, University of Ottawa, University of Toronto
NCT04100096Phase 2Oct 31, 2019Otsuka
NCT04118127Phase 1Oct 31, 2019Otsuka
NCT04174170Phase 3Oct 30, 2019Otsuka
NCT04174365Phase 3Oct 30, 2019Lundbeck, Otsuka
NCT04124614Phase 3Oct 23, 2019Otsuka
NCT03874494Phase 3May 5, 2019Otsuka, Peking University
NCT03734302Phase 1Apr 24, 2019Capital Medical University, Otsuka
Showing 20 of 88 trials
Page 1 / 5

Organizations

Research & Development (29)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
OtsukaFor profit776642008
LundbeckFor profit281042012
McGill UniversityAcademic/Hospital3122019
McMaster UniversityAcademic/Hospital3022019
Capital Medical UniversityAcademic/Hospital2012019
Dalhousie UniversityAcademic/Hospital2022019
Harvard UniversityAcademic/Hospital2112017
Queen's University, BelfastAcademic/Hospital2022019
Simon Fraser UniversityAcademic/Hospital2022019
Unity Health TorontoAcademic/Hospital2022019
University of British ColumbiaAcademic/Hospital2022019
University of CalgaryAcademic/Hospital2022019
University of MichiganAcademic/Hospital2022019
University of OttawaAcademic/Hospital2022019
University of TorontoAcademic/Hospital2222019
AstellasFor profit1112018
Duke UniversityAcademic/Hospital1112017
IQVIAFor profit1012012
Johns Hopkins UniversityAcademic/Hospital1012008
National Institute on Alcohol Abuse and Alcoholism (NIAAA)Government1012020
29 organizations
Page 1 / 2

Marketing (25)

OrganizationOrg typeRelationshipDate
ANDA RepositoryFor profitMKTGOct 25, 2023
Accord ResearchFor profitMKTGAug 17, 2021
Ajanta Pharma LtdFor profitMKTGAug 23, 2021
AlembicFor profitMKTGMar 7, 2023
AlembicFor profitSYNJan 13, 2025
Alkem Labs LtdFor profitMKTGSep 27, 2021
Amneal PharmaceuticalsFor profitMKTGJan 31, 2023
ApotexFor profitMKTGFeb 24, 2025
Aurobindo PharmaFor profitMKTGNov 2, 2023
Chartwell PharmaceuticalsFor profitMKTGOct 25, 2023
Hetero Labs LtdFor profitMKTGNov 20, 2023
LupinFor profitMKTGMar 18, 2023
LupinFor profitSYNMar 18, 2023
MSN LaboratoriesFor profitMKTGJan 25, 2023
NovartisFor profitMKTGSep 26, 2022
OPTIMUS PHARMA PRIVATE LTDFor profitMKTGOct 25, 2023
OtsukaFor profitMKTGJul 10, 2015
OtsukaFor profitNDAJul 10, 2015
Prinston IncFor profitMKTGMar 21, 2023
SandozFor profitMKTGSep 26, 2022
SandozFor profitSYNSep 26, 2022
TevaFor profitMKTGAug 11, 2022
ZENARAFor profitMKTGAug 29, 2022
Zydus Discovery DMCCFor profitMKTGSep 8, 2021
Zydus Discovery DMCCFor profitSYNJan 10, 2023