预约演示
更新于：2026-03-16
Brexpiprazole
布瑞哌唑
更新于：2026-03-16
概要
基本信息
药物类型 小分子化药 |
别名 Brexpiprazole (JAN/USAN/INN)、Rxulti、依匹哌唑 + [28] |
作用方式 激动剂、拮抗剂 |
作用机制 5-HT1A receptor激动剂(5-羟色胺1A受体激动剂)、5-HT2A receptor拮抗剂(5-羟色胺2A受体拮抗剂)、D2 receptor激动剂(多巴胺D2受体激动剂) |
非在研适应症 |
非在研机构- |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (美国)、快速通道 (美国) |
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结构/序列
分子式C25H27N3O2S |
InChIKeyZKIAIYBUSXZPLP-UHFFFAOYSA-N |
CAS号913611-97-9 |
关联
199
项与 布瑞哌唑 相关的临床试验ChiCTR2600117345
A Randomized Controlled Trial of Brexpiprazole versus Aripiprazole in the Treatment of Major Depressive Disorder with Psychotic Symptoms in Adolescents
CTR20255002
布瑞哌唑口溶膜在健康参与者中的生物等效性试验
CTR20254466
布瑞哌唑口崩片在中国健康研究参与者中餐后状态下随机、开放、单剂量、两序列、两周期、交叉生物等效性研究
100 项与 布瑞哌唑 相关的临床结果
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100 项与 布瑞哌唑 相关的转化医学
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100 项与 布瑞哌唑 相关的专利（医药）
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532
项与 布瑞哌唑 相关的文献（医药）2026-03-01JOURNAL OF CLINICAL PSYCHOPHARMACOLOGY
Effects of Adjunctive Brexpiprazole in Major Depressive Disorder Analyzed by Baseline Anxiety Level
Article
作者: Ward, Caroline ; Ismail, Zahinoor ; Habert, Jeffrey ; Chokka, Pratap ; Marrache, A. Marilise ; Therrien, François ; McIntyre, Roger S. ; Zhang, Zhen
Purpose/Background::
In patients with major depressive disorder (MDD), anxiety symptoms are common and associated with reduced treatment response. In an 8-week, phase 4, open-label study (ENGAGE), patients with MDD and inadequate antidepressant treatment response showed improvements in patient life engagement, depressive symptoms, and anxiety symptoms following treatment with adjunctive brexpiprazole 0.5 to 2 mg/d. This post hoc analysis of ENGAGE aimed to characterize the utility of adjunctive brexpiprazole in clinically relevant subgroups by baseline anxiety level.
Methods/Procedures::
Baseline anxiety subgroups were based on the 7-item Generalized Anxiety Disorder scale total score: no/mild (<10), moderate (10 to 14), and severe (>14). In each subgroup, changes in the 10-item Inventory of Symptomatology Self-Report (IDS-SR
10
) Life Engagement subscale score, IDS-SR total score, and other efficacy outcomes were determined. Safety was also analyzed.
Findings/Results::
One hundred twenty patients received adjunctive brexpiprazole, of whom 30 (25.0%) had no/mild anxiety, 43 (35.8%) had moderate anxiety, and 47 (39.2%) had severe anxiety at baseline. On IDS-SR
10
Life Engagement subscale score and IDS-SR total score, improvements (nominal
P
<0.001) from baseline to week 8 were observed across all subgroups. Improvements were also observed on all other efficacy endpoints (nominal
P
<0.05 in all subgroups). Incidence of treatment-emergent adverse events was 76.7% (no/mild baseline anxiety), 72.1% (moderate baseline anxiety), and 57.4% (severe baseline anxiety). No new safety signals were observed.
Implications/Conclusions::
Over 8 weeks, adjunctive brexpiprazole was associated with improvements in patient life engagement and depressive symptoms, regardless of baseline anxiety level. This observation may assist clinical decision-making when treating patients with MDD with/without anxiety symptoms.
2026-03-01Clinical Drug Investigation
Efficacy of Brexpiprazole in Participants with Agitation Associated with Dementia Due to Alzheimer’s Disease: Pooled Analysis of Randomized Controlled Trials
Article
作者: Hefting, Nanco ; Chumki, Sanjeda R ; Grossberg, George T ; Such, Pedro ; Wang, David ; Cummings, Jeffrey L ; Brubaker, Malaak ; Chang, Denise ; Zhang, Zhen
OBJECTIVE:
This analysis aimed to evaluate the efficacy of brexpiprazole 2 or 3 mg/day for the treatment of agitation associated with dementia due to Alzheimer's disease, on the basis of pooled clinical trial data.
METHODS:
Data were pooled from two similarly designed, phase 3, 12-week, multicenter, randomized, double-blind, placebo-controlled trials of fixed-dose brexpiprazole in participants in care facilities or community-based settings who had agitation associated with dementia due to Alzheimer's disease. Efficacy outcomes included Cohen-Mansfield Agitation Inventory (CMAI) total score (which measures the frequency of 29 different agitation symptoms), Clinical Global Impression-Severity of illness (CGI-S) score, CMAI factor scores (aggressive behaviors, physically nonaggressive behaviors, and verbally agitated behaviors), and response rates. A sensitivity analysis included a third trial with flexible dosing.
RESULTS:
In total, 621 participants were randomized (brexpiprazole, 368; placebo, 253), and completion rates were 320/368 (87.0%) and 225/253 (88.9%), respectively. Mean (SD) baseline CMAI total scores were: brexpiprazole 76.9 (17.2) points and placebo 75.5 (18.0) points. Over 12 weeks, CMAI total scores improved by least squares mean (SE) - 22.8 (0.8) points for brexpiprazole and - 18.3 (1.0) points for placebo, with a least squares mean difference between treatment arms of - 4.50 points (95% CI - 6.90 to - 2.10; p < 0.001; Cohen's d 0.30). CGI-S, CMAI factor, and response analyses also showed greater improvement with brexpiprazole versus placebo. The sensitivity analysis was supportive.
CONCLUSIONS:
Brexpiprazole 2 or 3 mg/day reduced agitation symptoms compared with placebo over 12 weeks in this large, pooled sample of participants with dementia due to Alzheimer's disease.
STUDY REGISTRATION:
ClinicalTrials.gov identifiers: NCT01862640, NCT03548584, and NCT01922258.
2026-03-01Neuropsychopharmacology reports
Synergistic Effect of Combination Treatment of Brexpiprazole and Nalmefene on Ethanol Intake in Rats
Article
作者: Kakumoto, Yusuke ; Amada, Naoki ; Suzuki, Mikio ; Futamura, Takashi ; Nakamura, Mai ; Ohgi, Yuta ; Maeda, Kenji
ABSTRACT:
Aims:
Reduction of alcohol consumption is one of treatment goals to reduce harm among individuals with alcohol use disorder (AUD), a major worldwide health problem, for which nalmefene, an opioid receptor modulator, is used. In this study, the effect of nalmefene on ethanol (EtOH) intake, already reported, was evaluated in Wistar rats, as validation. In addition, effects of brexpiprazole, serotonin–dopamine activity modulator, alone and in combination with nalmefene were evaluated to investigate further treatment option for AUD.
Methods:
During the first training phase, animals had 10% EtOH as the only drinking fluid available for the first 5 days. Then, the animals had a 24‐h free choice between EtOH and water for 39 days which is named the continual access paradigm. Thereafter, the limited access paradigm, which restricted the availability of 10% EtOH to 1 h every day, was carried out for 114 days. EtOH intake (g/kg/1 h) was determined by weighing 10% EtOH bottles before and after the limited EtOH access every day. Brexpiprazole (0.01–0.1 mg/kg, orally) and nalmefene (0.04–0.4 mg/kg, subcutaneously) were daily administered to rats 1 h or 20 min before starting the limited access paradigm for consecutive 4 days, respectively. The combination effect was evaluated using each subeffective dose of brexpiprazole and nalmefene which did not significantly reduce EtOH intake. The daily and the average EtOH intake for 4 days before and during the treatment with test compounds were statistically analyzed.
Results:
Brexpiprazole (0.1 mg/kg) and nalmefene (0.4 mg/kg) alone significantly decreased EtOH intake. Moreover, the combination of subeffective doses of brexpiprazole (0.01 mg/kg) and nalmefene (0.04 mg/kg) significantly and synergistically decreased EtOH intake.
Conclusion:
These data suggest that brexpiprazole may have the potential to decrease alcohol intake in AUD patients. In addition, brexpiprazole may have a synergistic therapeutic effect with nalmefene in those patients.
100 项与 布瑞哌唑 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 抑郁症 | 日本 | 2023-12-22 | |
| 痴呆引起的激越 | 美国 | 2023-05-10 | |
| 躁动 | 澳大利亚 | 2017-05-19 | |
| 阿尔茨海默症 | 澳大利亚 | 2017-05-19 | |
| 重度抑郁症 | 美国 | 2015-07-10 | |
| 精神分裂症 | 美国 | 2015-07-10 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 精神障碍 | 申请上市 | 中国 | 2024-08-16 | |
| 创伤后应激障碍 | 申请上市 | 美国 | 2024-06-25 | |
| 边缘性人格障碍 | 临床3期 | 美国 | 2020-01-13 | |
| 自闭症谱系障碍 | 临床3期 | 美国 | 2019-10-30 | |
| 自闭症谱系障碍 | 临床3期 | 美国 | 2019-10-30 | |
| 具有非典型特征的复发性重度抑郁症 | 临床3期 | 美国 | 2018-07-13 | |
| 躁郁症1型 | 临床3期 | 美国 | 2017-09-14 | |
| 躁郁症1型 | 临床3期 | 美国 | 2017-09-14 | |
| 躁郁症1型 | 临床3期 | 保加利亚 | 2017-09-14 | |
| 躁郁症1型 | 临床3期 | 保加利亚 | 2017-09-14 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床1期 | 59 | (Fasting-state Administration) | 鏇衊襯膚淵繭憲簾齋選(鑰憲膚膚觸蓋夢簾簾糧) = 鹽艱選觸願鏇繭鹽顧願 艱觸膚夢窪壓鏇簾鬱艱 (獵淵餘獵淵糧蓋顧淵範, 108.2) 更多 | - | 2026-02-11 | ||
(Fed-state Administration) | 鏇衊襯膚淵繭憲簾齋選(鑰憲膚膚觸蓋夢簾簾糧) = 餘觸積廠膚鬱顧壓糧壓 艱觸膚夢窪壓鏇簾鬱艱 (獵淵餘獵淵糧蓋顧淵範, 156.2) 更多 | ||||||
临床3期 | 295 | (De Novo (Conversion Period)) | 衊鏇糧鏇襯鹹壓淵艱壓 = 壓繭艱淵構鑰夢衊鏇鬱 築淵願獵範願顧築糧醖 (築艱築衊壓製鏇鬱繭獵, 鏇簾鏇醖繭選鑰願積窪 ~ 繭網獵製鏇醖鬱鬱鬱鑰) 更多 | - | 2026-02-04 | ||
(De Novo (Open-label Treatment Period)) | 廠壓餘選膚簾鹽醖夢顧(網製鏇壓衊範鹽齋淵艱) = 積艱獵網衊鬱選糧鑰積 壓築鏇夢襯壓鑰糧廠製 (築鬱獵餘壓鏇範鹹鬱膚, 12.80) 更多 | ||||||
临床3期 | 621 | Brexpiprazole 2 or 3 mg/day | 範積鏇鑰淵鏇淵獵餘餘(繭窪遞獵鹹製範窪廠鹹): P-Value = < 0.001 更多 | 积极 | 2026-01-27 | ||
Placebo | |||||||
临床3期 | 390 | Brexpiprazole 2 or 3 mg/day | 構鏇顧選願糧觸築衊繭(淵鏇製齋襯醖齋艱範蓋) = 築夢選鬱築製築願膚網 鬱壓築壓襯膚齋膚夢蓋 (鬱窪淵蓋齋憲餘壓獵範 ) | 积极 | 2025-12-01 | ||
Placebo | 構鏇顧選願糧觸築衊繭(淵鏇製齋襯醖齋艱範蓋) = 範窪製淵鹽鏇壓壓鏇繭 鬱壓築壓襯膚齋膚夢蓋 (鬱窪淵蓋齋憲餘壓獵範 ) | ||||||
临床3期 | 183 | 積壓膚願積積壓衊簾範(壓餘夢憲範膚網構顧顧) = 鹹獵蓋齋艱鹽鬱鏇夢鏇 蓋選網遞製構憲憲壓築 (廠淵窪艱鹽壓餘糧蓋簾 ) | 积极 | 2025-12-01 | |||
積壓膚願積積壓衊簾範(壓餘夢憲範膚網構顧顧) = 選築遞窪壓獵鏇顧範淵 蓋選網遞製構憲憲壓築 (廠淵窪艱鹽壓餘糧蓋簾 ) | |||||||
临床2期 | 39 | 蓋積壓淵製顧廠鹹膚鏇(觸簾窪廠鹹夢鑰廠鹽艱) = 餘構築築築窪夢鏇淵糧 壓淵窪鏇鹹鬱願鬱製鹽 (齋鏇顧繭膚選淵顧膚鬱 ) 更多 | 积极 | 2025-10-13 | |||
临床3期 | 1,043 | 壓襯壓構襯窪憲鑰廠獵(鹹遞淵蓋鬱夢築壓鹽獵) = 齋壓顧積廠鏇淵窪獵願 襯醖觸積鹹網獵壓壓鏇 (醖壓範醖築鹹構觸觸簾 ) 更多 | 积极 | 2025-10-01 | |||
Placebo | 壓襯壓構襯窪憲鑰廠獵(鹹遞淵蓋鬱夢築壓鹽獵) = 鹽夢網齋顧鹹膚製願網 襯醖觸積鹹網獵壓壓鏇 (醖壓範醖築鹹構觸觸簾 ) 更多 | ||||||
临床3期 | 898 | Antidepressant + Brexpiprazole 2-3 mg/day | 醖鬱顧鏇積壓壓簾夢膚(鏇醖獵淵醖憲觸網積繭) = 窪範築繭憲構窪蓋衊夢 夢壓艱顧遞廠築網齋範 (鏇獵餘繭範淵鹹選繭膚, 0.3) 更多 | 积极 | 2025-10-01 | ||
Antidepressant + Placebo | 醖鬱顧鏇積壓壓簾夢膚(鏇醖獵淵醖憲觸網積繭) = 願廠遞憲襯顧襯淵糧壓 夢壓艱顧遞廠築網齋範 (鏇獵餘繭範淵鹹選繭膚, 0.3) 更多 | ||||||
临床3期 | 1,385 | 獵鹹憲構壓遞顧簾顧鹽(網淵遞製網顧鹽觸鹽鬱): P-Value = 0.012 更多 | 积极 | 2025-09-11 | |||
Placebo | |||||||
临床3期 | 119 | (Brexpiprazole) | 壓鑰簾願餘膚鑰築網壓(蓋顧鏇積簾夢選醖繭衊) = 淵觸獵鏇艱夢網構鹹繭 構壓構鏇壓築衊窪鬱鹽 (壓鑰餘遞鑰齋衊繭廠憲, 1.28) 更多 | - | 2025-08-28 | ||
Placebo (Placebo) | 壓鑰簾願餘膚鑰築網壓(蓋顧鏇積簾夢選醖繭衊) = 觸繭窪淵壓獵糧鑰衊網 構壓構鏇壓築衊窪鬱鹽 (壓鑰餘遞鑰齋衊繭廠憲, 1.25) 更多 |
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