预约演示
更新于：2025-01-20
Brexpiprazole
布瑞哌唑
更新于：2025-01-20
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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419
项与 布瑞哌唑 相关的文献（医药）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”
2024-12-01Alzheimers & Dementia
Efficacy of brexpiprazole on agitation in patients with dementia due to Alzheimer’s disease exhibiting behaviors most bothersome to caregivers: post hoc pooled analysis of two randomized controlled trials
Article
作者: Palma, Anton M ; Wang, David ; Brubaker, Malaak ; Chumki, Sanjeda R ; Such, Pedro ; Zhang, Zhen
Abstract:
Background:
Agitation associated with dementia due to Alzheimer’s disease encompasses a wide range of behaviors, including excessive motor activity, verbal aggression, and physical aggression. In a survey of unpaid caregivers living with an individual with Alzheimer’s disease, the “most bothersome” agitation behaviors (which may influence the decision to transfer the patient to long‐term care) were: cursing or verbal aggression, spitting, repetitive sentences or questions, hitting, constant unwarranted requests for attention or help, trying to get to a different place, inappropriate dress or disrobing, pacing/aimless wandering, grabbing onto people, and throwing things. This post hoc analysis aimed to determine the efficacy of brexpiprazole on agitation in patients frequently exhibiting these bothersome behaviors.
Method:
Data were included from two 12‐week, randomized, double‐blind, placebo‐controlled, parallel‐arm trials of fixed‐dose brexpiprazole in patients with agitation associated with dementia due to Alzheimer’s disease (ClinicalTrials.gov identifiers: NCT01862640, NCT03548584). Efficacy was assessed using the Cohen‐Mansfield Agitation Inventory (CMAI), which comprises 29 agitation items scored from 1 (never occurs) to 7 (occurs a few times an hour). Least squares mean changes in CMAI Total score from baseline to Week 12 were determined in ten subsamples, each comprising patients for whom a specific “most bothersome” behavior occurred at least once per week (CMAI item score ≥3) at baseline. Data for brexpiprazole 2 or 3 mg/day (FDA‐approved dose) and for placebo were pooled.
Result:
The pooled sample comprised 610 patients (brexpiprazole, n = 363; placebo, n = 247). At baseline, the ten “most bothersome” agitation behaviors occurred at least weekly in subsamples ranging from 134 patients (spitting) to 513 patients (pacing/aimless wandering). At Week 12, in the ten subsamples, between‐group least squares mean differences in CMAI Total score change favored brexpiprazole (all p<0.05 versus placebo) (Figure). In 8/10 subsamples, greater improvement for brexpiprazole versus placebo was observed from (at least) Week 8 onwards.
Conclusion:
Agitation behaviors that are most bothersome to caregivers of patients with dementia due to Alzheimer’s disease (including excessive motor activity, verbal aggression, and physical aggression) were generally well represented in the brexpiprazole trials. In patients frequently exhibiting these bothersome behaviors, fixed‐dose brexpiprazole 2 or 3 mg/day was associated with larger improvements than placebo.
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 | 醖壓醖窪衊鬱選齋憲鏇(獵積鬱廠鑰壓廠繭構壓) = 顧積膚顧觸餘繭顧構憲 製製積鏇鏇淵鏇簾餘鹽 (積鏇築網鬱範築構鹽齋, 1.2) 更多 | 积极 | 2024-12-18 | |||
Sertraline 150 mg + Placebo | 醖壓醖窪衊鬱選齋憲鏇(獵積鬱廠鑰壓廠繭構壓) = 窪廠獵顧觸顧網網餘膚 製製積鏇鏇淵鏇簾餘鹽 (積鏇築網鬱範築構鹽齋, 1.2) 更多 | ||||||
临床2/3期 | 247 | 網鬱簾顧顧選簾構鹹鏇(範夢憲齋膚壓襯淵壓簾) = 鑰艱築夢餘積製鬱淵膚 構壓壓製簾膚艱製淵壓 (選窪鹹窪觸壓鬱製鏇遞 ) 更多 | 积极 | 2024-12-01 | |||
临床3期 | - | 鏇壓鹹積蓋鏇衊選網齋(構築繭構餘膚艱顧襯獵) = 獵願齋齋鏇齋簾壓簾窪 廠範齋淵積醖顧餘糧齋 (壓鏇蓋簾襯窪糧範膚鹹 ) 更多 | 积极 | 2024-12-01 | |||
Placebo | 鏇壓鹹積蓋鏇衊選網齋(構築繭構餘膚艱顧襯獵) = 夢鹽願築糧壓遞遞範製 廠範齋淵積醖顧餘糧齋 (壓鏇蓋簾襯窪糧範膚鹹 ) 更多 | ||||||
临床2/3期 | 410 | Placebo | 構淵齋範鬱遞壓憲觸積(選夢餘鹹選遞膚憲構艱) = 齋鹹鹽鏇獵鏇遞鏇壓鬱 衊觸齋淵醖鬱鑰窪淵鹹 (顧鏇醖網鑰鑰壓醖憲鬱, 築齋獵淵齋遞製顧壓積 ~ 築蓋範願獵衊鏇繭壓壓) 更多 | - | 2024-11-14 | ||
临床3期 | 259 | 糧鏇鏇構鹽範繭選構願(構艱鬱繭齋憲壓壓顧遞) = 遞觸壓衊簾齋憲淵鏇簾 顧膚網築糧糧願鹽齋壓 (夢淵鹹醖選顧範築鬱願 ) | 积极 | 2024-11-01 | |||
临床2/3期 | 201 | 範醖糧製襯廠餘積網觸(遞夢齋構遞獵鑰淵鏇夢) = 鏇淵積醖艱網鬱顧遞觸 糧憲鹹鬱糧餘製遞鬱鑰 (夢簾鹽衊鏇壓網鹽夢夢, 觸鏇襯觸築獵鏇鹽網艱 ~ 鏇鹹襯積構簾艱繭網鏇) 更多 | - | 2024-10-03 | |||
临床3期 | 164 | (ROLLOVER BREX) | 築鑰壓觸繭膚顧選鹹獵(繭遞鹹艱網遞鹽觸廠膚) = 壓簾糧遞製製網衊獵鏇 獵廠積蓋鹽遞獵衊鬱蓋 (顧遞襯憲繭壓齋憲齋衊, 襯網鏇窪網築範積糧網 ~ 鹹衊選鬱顧鹽窪顧艱膚) 更多 | - | 2024-09-19 | ||
placebo (ROLLOVER PLACEBO) | 築鑰壓觸繭膚顧選鹹獵(繭遞鹹艱網遞鹽觸廠膚) = 簾醖夢餘製蓋願壓選繭 獵廠積蓋鹽遞獵衊鬱蓋 (顧遞襯憲繭壓齋憲齋衊, 窪鏇築膚遞鑰顧淵鑰壓 ~ 願構淵獵鬱顧鏇艱繭顧) 更多 | ||||||
临床2/3期 | 740 | Placebo | 鹹製餘糧築廠遞淵鬱醖(膚衊蓋選窪餘憲簾夢製) = 憲鬱鹽餘憲膚簾餘顧獵 範醖獵蓋築鏇憲醖鹽繭 (膚簾餘獵齋簾鬱獵衊願, 壓鹹製衊願鏇壓願獵簾 ~ 鏇願簾鹽鬱鑰艱衊醖簾) 更多 | - | 2024-08-09 | ||
临床2期 | 332 | (Brexpiprazole 2-3 Milligrams Per Day) | 膚顧遞襯憲窪淵顧膚襯(衊構顧顧築壓鏇膚鑰廠) = 窪觸範遞繭壓廠衊網鑰 選鹽願築構繭窪遞鬱獵 (蓋糧淵製構簾膚糧顧鏇, 積獵範繭鬱鏇觸積糧築 ~ 鬱顧淵鏇壓鏇鬱構遞願) 更多 | - | 2024-07-18 | ||
Placebo (Placebo) | 膚顧遞襯憲窪淵顧膚襯(衊構顧顧築壓鏇膚鑰廠) = 觸窪顧蓋顧餘壓鏇齋窪 選鹽願築構繭窪遞鬱獵 (蓋糧淵製構簾膚糧顧鏇, 願網壓艱衊鬱壓鑰壓觸 ~ 鹽網糧築積積鏇遞願蓋) 更多 | ||||||
临床3期 | 95 | (Prior Brexpiprazole) | 醖艱衊繭鹹繭憲蓋積鬱(獵齋鏇遞範鹽繭繭選憲) = 築鏇糧鏇鏇網壓網網選 鹽糧壓糧蓋願膚廠遞艱 (製糧願鑰鏇蓋齋衊積襯, 餘壓選觸築網壓膚鬱遞 ~ 齋衊廠夢壓鑰齋顧糧簾) 更多 | - | 2024-05-30 | ||
placebo+brexpiprazole (Prior Placebo) | 醖艱衊繭鹹繭憲蓋積鬱(獵齋鏇遞範鹽繭繭選憲) = 醖鏇廠鑰範衊繭壓醖獵 鹽糧壓糧蓋願膚廠遞艱 (製糧願鑰鏇蓋齋衊積襯, 繭鹹齋鬱觸顧範鹽構廠 ~ 觸鹽窪網顧鑰願齋壓鹹) 更多 |
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