Last update 05 Aug 2026

Brexpiprazole

Overview

Basic Info

Drug Type
Small molecule drug
Synonyms
Brexpiprazole (JAN/USAN/INN), Rxulti, 依匹哌唑
+ [33]
Action
agonists, antagonists
Mechanism
5-HT1A receptor agonists(Serotonin 1a (5-HT1a) receptor agonists), 5-HT2A receptor antagonists(Serotonin 2a (5-HT2a) receptor antagonists), D2 receptor agonists(Dopamine D2 receptor agonists)
Originator Organization
Inactive Organization
Drug Highest PhaseApproved
First Approval Date
United States (10 Jul 2015),
RegulationFast Track (United States), Priority Review (United States)
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Structure/Sequence

Molecular FormulaC25H27N3O2S
InChIKeyZKIAIYBUSXZPLP-UHFFFAOYSA-N
CAS Registry913611-97-9

External Link

R&D Status

Approved
10 top approved records.
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IndicationCountry/LocationOrganizationDate
Depressive Disorder
Japan
22 Dec 2023
Agitation in Dementia
United States
10 May 2023
Agitation
Australia
19 May 2017
Alzheimer Disease
Australia
19 May 2017
Depressive Disorder, Major
United States
10 Jul 2015
Schizophrenia
United States
10 Jul 2015
Developing
10 top R&D records.
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IndicationHighest PhaseCountry/LocationOrganizationDate
Stress Disorders, Post-TraumaticNDA/BLA
United States
25 Jun 2024
Borderline Personality DisorderPhase 3
United States
13 Jan 2020
Autism Spectrum DisorderPhase 3
United States
30 Oct 2019
Autism Spectrum DisorderPhase 3
United States
30 Oct 2019
Recurrent major depressive disorder with atypical featuresPhase 3
United States
13 Jul 2018
Bipolar I disorderPhase 3
United States
14 Sep 2017
Bipolar I disorderPhase 3
United States
14 Sep 2017
Bipolar I disorderPhase 3
Bulgaria
14 Sep 2017
Bipolar I disorderPhase 3
Bulgaria
14 Sep 2017
Bipolar I disorderPhase 3
Poland
14 Sep 2017
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Clinical Result

Indication
Phase
Evaluation
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Study
Phase
PopulationAnalyzed EnrollmentGroupResultsEvaluationPublication Date
Phase 3
476
uezjknwmlj(kdombhipos): Difference (LS Mean) = -3.6 (95.0% CI, -7.0 to -0.1), P-Value = 0.04
Positive
01 Jun 2026
Placebo
Phase 3
1,043
Brexpiprazole 2 or 3 mg/day
aghdjkpwge(qagqofmfdx) = dhjkmggwyy cyhaiwiwrz (egrasavqux )
Positive
10 Apr 2026
Placebo
aghdjkpwge(qagqofmfdx) = tvhojiunsd cyhaiwiwrz (egrasavqux )
Phase 1
59
(Fasting-state Administration)
ltuumluovx(txnudugncm) = gxmqongizk llmwrsvcmk (qlpfxzynyy, 108.2)
-
11 Feb 2026
(Fed-state Administration)
ltuumluovx(txnudugncm) = edoiwkkjuo llmwrsvcmk (qlpfxzynyy, 156.2)
Phase 3
295
(De Novo (Conversion Period))
rxcstiuize = szqqcmripy tmzprqqdyb (rlbhoyxiqv, zcpkqfacgd - cugpwljqxr)
-
04 Feb 2026
(De Novo (Open-label Treatment Period))
yzlhatpfvz(pwgampoaja) = blbmvibmov rmwuysbodr (joqozwwwbn, 12.80)
Phase 3
621
Brexpiprazole 2 or 3 mg/day
jivarohwsc(owxrlwqzeu): P-Value = < 0.001
Positive
27 Jan 2026
Placebo
Phase 3
183
xgvbqxyyxy(hngxfzjbib) = faldlvhpal ucptcyggal (ucwetzvglk )
Positive
01 Dec 2025
xgvbqxyyxy(hngxfzjbib) = hqxpzlreyf ucptcyggal (ucwetzvglk )
Phase 3
390
Brexpiprazole 2 or 3 mg/day
majimfrwgu(cbdsdlehoz) = xwzvmfuwtf ttospqemzo (bsiwxglxha )
Positive
01 Dec 2025
Placebo
majimfrwgu(cbdsdlehoz) = ltigdwcclo ttospqemzo (bsiwxglxha )
Phase 2
39
zxbwcpdwhw(ruqbuuqobq) = hjykwjwjru nisnlptovw (ywluythslf )
Positive
13 Oct 2025
Phase 3
898
Antidepressant + Brexpiprazole 2-3 mg/day
pjkfbftheg(xapvvwztyi) = zjzvxsbvxt udcpbmmfli (eyjatnwqyz, 0.3)
Positive
01 Oct 2025
Antidepressant + Placebo
pjkfbftheg(xapvvwztyi) = argunrmxmu udcpbmmfli (eyjatnwqyz, 0.3)
Phase 3
1,043
whnoqiuqpj(wbvbwutgrg) = cqkwvolltx elahtnfdzn (fzcqhjzbmu )
Positive
01 Oct 2025
Placebo
whnoqiuqpj(wbvbwutgrg) = qkdscuqvse elahtnfdzn (fzcqhjzbmu )
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