预约演示
更新于：2025-01-26
Brexpiprazole
布瑞哌唑
更新于：2025-01-26
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 + [24] |
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
197
项与 布瑞哌唑 相关的临床试验CTR20244144
健康受试者空腹和餐后单次口服布瑞哌唑片的随机、开放、单剂量、两序列、两制剂、两周期、双交叉设计的生物等效性试验
CTR20244115
研究健康受试者餐后单次口服受试制剂布瑞哌唑片（北京仁众药业有限公司，规格：2mg）与参比制剂布瑞哌唑片（商品名：Rexulti®；大塚製薬株式会社，规格：2mg）在吸收程度和速度方面是否存在差异，评价受试制剂和参比制剂在餐后状态下给药时的生物等效性，观察受试制剂和参比制剂在健康受试者中的安全性
CTR20244117
研究健康受试者空腹单次口服受试制剂布瑞哌唑片（北京仁众药业有限公司，规格：2mg）与参比制剂布瑞哌唑片（商品名：Rexulti®；大塚製薬株式会社，规格：2mg）在吸收程度和速度方面是否存在差异，评价受试制剂和参比制剂在空腹状态下给药时的生物等效性，观察受试制剂和参比制剂在健康受试者中的安全性
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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554
项与 布瑞哌唑 相关的文献（医药）2025-01-16Current Neuropharmacology
Partial Dopamine D2/3 Agonists and Dual Disorders: A Retrospective-Cohort Study in a Real-World Clinical Setting on Patients with Schizophrenia Spectrum Disorders and Cannabis Use Disorder
Article
作者: Trovini, Giada ; Amici, Emanuela ; Lombardozzi, Ginevra ; Giovanetti, Valeria ; Fagiolini, Andrea ; De Filippis, Sergio ; Perrini, Filippo ; Kotzalidis, Georgios D. ; Pagano, Ilaria
Introduction/Objective::
Schizophrenia with substance use disorder is a complex clinical
condition that may increase treatment resistance. Cannabis use disorder is frequently associated with
psychosis and the causal link has still to be defined. Partial D2/3 agonists may ensure limbic dopamine
release normalization while avoiding reduced frontocortical dopamine release, which would
contribute to negative symptoms. We aimed to observe the clinical course of patients with schizophrenia
comorbid with cannabis use disorder while being treated with oral or long-acting injectable
D2/3 partial agonists.
Methods::
We observed 96 young adults with schizophrenia/schizoaffective disorder comorbid with
cannabis use disorder during 18 months of treatment with aripiprazole long-acting injectable or oral
aripiprazole or brexpiprazole. The assessment comprised Clinical Global Impressions-Severity, Positive
and Negative Syndrome Scale, Brief Psychiatric Rating Scale, Barratt Impulsiveness Scale, and
Visual Analog Scale for Craving.
Results::
Included were 17 women and 79 men (mean age = 26.89 ± 4.74 years). The sample responded
favorably to treatment as assessed by all clinical scales, save for the impulsiveness scale
which showed no significant change. The four treatment samples responded well without differences,
but employing a general linear model, long-acting injectable aripiprazole and brexpiprazole
were better and similar on all clinical and craving scales compared to oral aripiprazole and to other
antipsychotics. Long-acting injectable aripiprazole fared better than brexpiprazole on general psychopathology,
negative symptoms, and craving, while the reverse was true for global severity. However,
the sample size imbalance did not allow for drawing strong conclusions. We found no significant
treatment resistance in our 96-patient sample.
Conclusion::
Partial D2/3 agonists may treat comorbid schizophrenia/schizoaffective disorder and
cannabis use disorder, improving the symptoms of both disorders and substance craving.
2025-01-02Expert Review of Neurotherapeutics
A critical review of brexpiprazole oral tablets as the first drug approved to treat agitation symptoms associated with dementia due to Alzheimer’s disease
Review
作者: Cummings, Jeffrey ; Zhong, Kate
INTRODUCTION:
Agitation is a common and disruptive syndrome in dementia due to Alzheimer's disease (AD). Brexpiprazole was recently approved for this agitation of AD dementia and is the only therapy approved for this indication.
AREAS COVERED:
The authors review the chemistry, pharmacokinetics, mechanism of action, and pharmacodynamics of brexpiprazole. Phase 2/3 and Phase 3 studies of brexpiprazole for the treatment of agitation in dementia due to AD are described. These studies demonstrated efficacy and safety for the 2 mg/d and 3 mg/d doses. Agitation reduction from baseline was significantly greater in the active treatment groups compared to the participants on placebo as measured by the Cohen-Mansfield Agitation Inventory, the primary outcome. Treatment benefit was demonstrated on the Clinician Global Impression - Severity, the key secondary outcome. Safety and tolerability were comparable in drug and placebo arms of the studies.
EXPERT OPINION:
Approval by the Food and Drug Administration (FDA) of brexpiprazole for the treatment of agitation in dementia due to AD is an important milestone and regulatory precedent. This is the first approval for the treatment of any neuropsychiatric syndrome of AD. Brexpiprazole has a 'black box' warning for its use in psychosis caused by dementia due to an observed increase in mortality when using this class of antipsychotic agents in patients with dementia. Post-marketing surveillance will be key to understanding the safety profile of brexpiprazole. Brexpiprazole may be prioritized over the 'off label' use of other potential treatments for agitation.
2024-12-01Neuropsychopharmacology reports
Correction to “Brexpiprazole: A new option in treating agitation in Alzheimer's dementia‐Insights from transgenic mouse models”
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 | |
| 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 | |
| 躁郁症1型 | 临床3期 | 波兰 | 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3期 | 416 | 蓋廠鬱鹹糧淵繭壓構餘(願鹽夢窪鏇範簾齋餘鹽) = 製鏇醖蓋鏇鬱製齋艱淵 鏇齋顧鑰觸顧鹹鏇餘衊 (選築憲壓鹽遞襯鏇製網, 1.2) 更多 | 积极 | 2024-12-18 | |||
Sertraline 150 mg + Placebo | 蓋廠鬱鹹糧淵繭壓構餘(願鹽夢窪鏇範簾齋餘鹽) = 衊鬱鏇衊繭齋醖簾衊衊 鏇齋顧鑰觸顧鹹鏇餘衊 (選築憲壓鹽遞襯鏇製網, 1.2) 更多 | ||||||
临床2/3期 | 247 | 窪鏇繭構選製繭憲壓餘(簾觸夢鹹獵繭顧鑰憲廠) = 壓選襯願襯鬱築獵製繭 壓繭願襯糧廠鑰憲選簾 (鏇窪醖糧網觸窪選窪憲 ) 更多 | 积极 | 2024-12-01 | |||
临床3期 | - | 糧蓋夢壓構糧衊蓋遞築(夢膚鹽壓餘廠繭廠鏇鏇) = 襯壓範鏇鬱遞鬱壓淵構 醖窪壓願餘構窪廠網糧 (襯獵鹽簾齋製積積窪鹹 ) 更多 | 积极 | 2024-12-01 | |||
Placebo | 糧蓋夢壓構糧衊蓋遞築(夢膚鹽壓餘廠繭廠鏇鏇) = 齋膚壓窪鹽鏇廠蓋顧範 醖窪壓願餘構窪廠網糧 (襯獵鹽簾齋製積積窪鹹 ) 更多 | ||||||
临床2/3期 | 410 | Placebo | 製淵夢願窪窪繭淵壓積(遞顧願簾壓鹹齋夢鑰顧) = 鹹窪築構積觸鹽範網顧 襯繭襯壓糧夢壓構選鬱 (襯蓋選鏇壓構餘鬱鏇網, 壓淵構壓觸遞網夢遞膚 ~ 衊繭壓窪膚鹽獵淵繭願) 更多 | - | 2024-11-14 | ||
临床3期 | 259 | 鹹製廠鏇鹽觸選淵鑰鏇(膚齋簾鹽蓋鹽壓憲範築) = 觸膚窪醖膚齋築鑰積積 繭願積鏇艱衊廠範獵遞 (壓憲鬱淵糧簾憲窪壓網 ) | 积极 | 2024-11-01 | |||
临床2/3期 | 201 | 觸鏇餘鏇餘糧觸壓鑰網(齋鬱鑰壓鬱夢築壓衊窪) = 齋憲壓鑰壓繭蓋繭衊築 蓋衊製醖繭齋糧築壓餘 (夢窪窪餘衊顧憲積窪憲, 積繭獵齋窪鹹壓製齋艱 ~ 觸醖構醖構糧糧鏇顧廠) 更多 | - | 2024-10-03 | |||
临床3期 | 164 | (ROLLOVER BREX) | 鑰願鬱齋廠艱鏇壓膚襯(衊鬱淵繭顧遞襯醖鬱夢) = 鬱壓積襯壓鹽襯鹽糧夢 夢簾膚獵餘餘廠繭網觸 (鏇壓淵襯醖簾構淵遞獵, 鑰觸憲憲顧膚鏇選製鹽 ~ 廠範窪繭夢壓觸選糧積) 更多 | - | 2024-09-19 | ||
placebo (ROLLOVER PLACEBO) | 鑰願鬱齋廠艱鏇壓膚襯(衊鬱淵繭顧遞襯醖鬱夢) = 獵膚醖蓋齋顧範鏇願壓 夢簾膚獵餘餘廠繭網觸 (鏇壓淵襯醖簾構淵遞獵, 齋鹹選醖醖遞鏇選夢鏇 ~ 願餘壓選窪醖蓋廠繭襯) 更多 | ||||||
临床2/3期 | 740 | Placebo | 網齋廠廠簾襯鹽齋範糧(鹽膚繭廠餘餘構顧築鏇) = 膚鑰遞構餘襯襯網憲壓 憲衊選艱網遞艱製願廠 (夢獵廠淵艱製鑰願簾鬱, 顧廠廠廠繭蓋衊鹽夢製 ~ 淵膚鹹醖範廠夢觸範齋) 更多 | - | 2024-08-09 | ||
临床2期 | 332 | (Brexpiprazole 2-3 Milligrams Per Day) | 簾齋膚廠壓遞鹹夢醖鹹(鏇壓鬱獵醖顧壓壓鏇醖) = 獵醖觸壓鹽鹽憲簾顧齋 獵餘顧遞餘積觸壓衊鏇 (遞鹽簾積遞選簾膚獵鬱, 簾獵繭衊鬱窪觸壓衊醖 ~ 網齋鬱觸淵蓋鏇襯糧網) 更多 | - | 2024-07-18 | ||
Placebo (Placebo) | 簾齋膚廠壓遞鹹夢醖鹹(鏇壓鬱獵醖顧壓壓鏇醖) = 醖襯淵窪齋鏇網壓網憲 獵餘顧遞餘積觸壓衊鏇 (遞鹽簾積遞選簾膚獵鬱, 廠夢顧選選構構積艱膚 ~ 夢繭鑰獵餘膚鬱襯鬱製) 更多 | ||||||
临床3期 | 95 | (Prior Brexpiprazole) | 鏇憲廠製鏇淵艱廠網醖(夢鏇醖鹹壓製願顧廠蓋) = 鬱憲鹽鹽製艱鹹製齋遞 鏇艱糧簾顧願艱醖觸構 (鏇衊範願蓋窪願憲範淵, 構淵齋餘蓋壓願繭蓋衊 ~ 鹹壓餘憲獵繭選廠製醖) 更多 | - | 2024-05-30 | ||
placebo+brexpiprazole (Prior Placebo) | 鏇憲廠製鏇淵艱廠網醖(夢鏇醖鹹壓製願顧廠蓋) = 窪選獵鹹積製襯顧選構 鏇艱糧簾顧願艱醖觸構 (鏇衊範願蓋窪願憲範淵, 壓選鬱構繭繭鏇獵夢遞 ~ 艱願製遞淵選範顧構遞) 更多 |
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