预约演示
更新于：2025-08-04
Brexpiprazole
布瑞哌唑
更新于：2025-08-04
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 + [27] |
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
185
项与 布瑞哌唑 相关的临床试验CTR20251094
布瑞哌唑口服溶液空腹及餐后人体生物等效性研究
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健康参与者空腹和餐后单次口服布瑞哌唑片的随机、开放、单剂量、两制剂、两序列、两周期、双交叉设计的生物等效性试验
CTR20251755
海南通用三洋药业有限公司研制的布瑞哌唑片（2 mg）与Otsuka Pharmaceutical Co.，Ltd.持证的布瑞哌唑片（Rexulti®，2 mg）在中国健康受试者中进行的随机、开放、单次给药、两周期、双交叉设计的空腹及餐后状态下的生物等效性研究
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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624
项与 布瑞哌唑 相关的文献（医药）2025-11-01JOURNAL OF AFFECTIVE DISORDERS
Cost-effectiveness of brexpiprazole for the treatment of major depressive disorder in Japan
Article
作者: Gorecki, Michal ; Pochopien, Michal ; Yamato, Kentaro ; Sado, Mitsuhiro ; Zhang, Yilong
BACKGROUND:
Approximately 50 % of patients with major depressive disorder (MDD) do not respond adequately to selective serotonin reuptake inhibitors (SSRI) and serotonin and norepinephrine reuptake inhibitors (SNRI). These patients are candidates for add-on therapy with brexpiprazole.
METHODS:
A cost-utility analysis was conducted from the Japanese public healthcare payer perspective to compare brexpiprazole and placebo (no add-on) as an adjunct to SSRI/SNRI in patients with MDD and inadequate response to SSRI/SNRI monotherapy. An additional analysis compared initiation of brexpiprazole after 8 (early add-on) and 14 weeks (late add-on). The model followed a cohort of patients participating in clinical trials of brexpiprazole over a total time horizon of 67 weeks.
RESULTS:
Early add-on of brexpiprazole was cost-effective at the willingness to pay threshold of 5 million JPY/QALY compared with both no add-on and late add-on. Compared with no add-on, patients in the early add-on group gained 0.037 quality-adjusted life-years (QALYs) at an incremental cost of JPY 155,762, resulting in an incremental cost-effectiveness ratio (ICER) of JPY 4.3 million/QALY. Compared with late add-on, early add-on resulted in an incremental gain of 0.008 QALYs at a total cost of JPY 3663, corresponding to an ICER of JPY 0.46 million/QALY.
LIMITATIONS:
The modelling horizon was restricted to trial duration, so that long-term benefits of brexpiprazole were not captured. There was also uncertainty around incremental QALY gains for early compared with late add-on.
CONCLUSION:
Brexpiprazole, especially when initiated early, was a cost-effective adjunctive treatment for patients with MDD and a history of inadequate response to SSRI/SNRI.
2025-11-01JOURNAL OF AFFECTIVE DISORDERS
Adverse events associated with four atypical antipsychotics used as augmentation treatment for major depressive disorder: A pharmacovigilance study based on the FAERS database
Article
作者: Qi, Fangqing ; Tian, Leiyu ; Zhang, Xiangyang ; Qu, Miao ; Zhang, Yingjie ; Zhao, Simin ; Li, Fei ; Diao, Huaqiong
BACKGROUND:
There is insufficient understanding of the long-term studies on adverse events (ADEs) in major depressive disorder (MDD) treated with atypical antipsychotics (AAPs), risks in patients with different psychiatric disorders, and differences between male and female patients.
METHODS:
This study retrieved ADE reports for aripiprazole, quetiapine XR, brexpiprazole, and cariprazine from the FDA Adverse Event Reporting System (FAERS) for the time periods of FDA approval for MDD in the first quarter (Q1) of 2007, the Q1 of 2009, the Q1 of 2015, and the Q1 of 2022 respectively to the Q1 of 2024. Four algorithms (ROR, PRR, BCPNN, and MGPS) assessed ADE signals. We compared positive signal rates between MDD and non-MDD, and assessed sex differences in drug-related risks by ROR.
RESULTS:
Patients with MDD had significantly higher rates of impulse control disorders (ICDs), obsessive-compulsive disorder (OCD), weight gain, extrapyramidal symptoms, and metabolic disorders compared to non-MDD (P < 0.05). Restless legs syndrome was associated with aripiprazole (P < 0.01), brexpiprazole (P < 0.01), and quetiapine XR. Serotonin syndrome, eosinophilic myocarditis, and angle-closure glaucoma were new signals of aripiprazole in patients with MDD (P < 0.05). Female patients were more likely to gain weight (P < 0.05) with using aripiprazole, quetiapine XR, and brexpiprazole, whereas male patients with aripiprazole (P < 0.01) or brexpiprazole (P < 0.05) reported higher rates of ICDs and OCD.
CONCLUSION:
It is suggesting a potential increased risk of various ADEs in patients with MDD when taking AAPs. The causal relationship and the exact mechanism between drugs and ADEs remains unclear, requiring further research.
2025-08-12NEUROLOGY
Real-World Evidence of Brexpiprazole Use and 6-Month Mortality, Hospitalization, and Emergency Department Visits Among Persons With Dementia
Article
作者: Jacobson, Mireille ; Tysinger, Bryan ; Ferido, Patricia ; Thunell, Johanna ; Haye, Sidra ; Zissimopoulos, Julie ; Joyce, Geoffrey
BACKGROUND AND OBJECTIVES:
Alzheimer disease and other dementias are accompanied by depression and agitation and other behavioral and neuropsychiatric symptoms. In 2023, brexpiprazole became the first antipsychotic approved by the US Food and Drug Administration to treat agitation in persons with Alzheimer disease, but, like all atypical antipsychotics, it includes a black box warning of an increased risk of mortality among persons with dementia. This study provides real-world evidence of mortality in a heterogeneous sample of brexpiprazole users to understand effects in the population.
METHODS:
We used a 100% sample of Medicare claims data Parts A, B, and D from 2014 to 2023. Our sample was limited to beneficiaries with diagnosed dementia, who were continuously enrolled for at least 2 years and were new users of the atypical antipsychotics brexpiprazole or aripiprazole in a given year. We used matching and logistic regression to estimate the relationship between incident use of brexpiprazole, compared with aripiprazole, and mortality, emergency department (ED) visits, and hospitalization within 6 months.
RESULTS:
Among the 41,871 beneficiaries with dementia, 71.7% of brexpiprazole and 69.7% of aripiprazole users were women with a mean age of 75.7 and 78.0 years, respectively. Among persons living with dementia (PLWD), 6-month mortality was statistically lower among new users of brexpiprazole based on estimates from logistic regression and a matched sample of new users of brexpiprazole or aripiprazole (OR 0.49, [95% CI 0.37-0.65]).There was no statistical difference between the incident use of brexpiprazole and aripiprazole use for ED visits or hospitalization within 6 months of use initiation. Adjustment for potential unobserved confounding used two-stage least squares estimation and found no statistically significant differences in six-month mortality, ED visits, or hospitalizations between the 2 groups.
DISCUSSION:
Brexpiprazole use is not associated with differential mortality risk compared with aripiprazole use among PLWD. Brexpiprazole offers a treatment option which is important given the heterogeneity of effects of antipsychotics on persons. A two-stage least squares method is used to eliminate bias on estimates because of observed and unobserved differences between the 2 groups, but the small sample size is a limitation.
CLASSIFICATION OF EVIDENCE:
This study provides Class III evidence that brexpiprazole does not increase the risk of mortality at 6 months compared with aripiprazole in PLWD.
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
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N/A | - | - | Antidepressant + Brexpiprazole 2-3 mg/day | 窪齋鑰積願鹽簾廠壓醖(鏇顧遞衊網窪遞積顧獵) = 鹽鑰壓鬱艱襯構選簾鏇 範繭積膚夢製鬱鏇觸簾 (憲製選窪簾夢齋願淵願 ) | 积极 | 2025-07-03 | |
Antidepressant + Placebo | 窪齋鑰積願鹽簾廠壓醖(鏇顧遞衊網窪遞積顧獵) = 襯艱衊積壓願齋夢齋範 範繭積膚夢製鬱鏇觸簾 (憲製選窪簾夢齋願淵願 ) | ||||||
临床3期 | 450 | (Brexpiprazole + Sertraline) | 顧鬱艱蓋夢選網餘範窪(夢蓋膚憲蓋積糧鑰窪醖) = 齋膚憲鑰糧齋願積廠鹹 選鏇網築鑰醖蓋淵範糧 (窪艱膚壓蓋繭觸淵蓋遞, 1.17) 更多 | - | 2025-06-13 | ||
Placebo+sertraline (Sertraline + Placebo) | 顧鬱艱蓋夢選網餘範窪(夢蓋膚憲蓋積糧鑰窪醖) = 夢糧觸網選憲觸夢鬱範 選鏇網築鑰醖蓋淵範糧 (窪艱膚壓蓋繭觸淵蓋遞, 1.24) 更多 | ||||||
临床3期 | 精神分裂症 维持 | 169 | 製鹽積範醖獵鹽築窪顧(膚壓繭範鑰鏇鏇糧糧醖) = 9.0% 鏇網餘糧選憲廠遞醖糧 (顧獵構獵鏇鏇觸鏇淵憲 ) 更多 | 积极 | 2025-06-01 | ||
临床3期 | 591 | (Brexpiprazole (2 mg) + Sertraline) | 齋製遞醖齋範夢積鬱築(窪鏇顧鹹窪願膚餘廠觸) = 鏇餘鹽壓鬱艱淵壓壓鹽 構構憲鹽構齋夢衊夢艱 (襯衊餘窪廠壓簾繭遞鑰, 1.19) 更多 | - | 2025-05-30 | ||
(Brexpiprazole (3 mg) + Sertraline) | 齋製遞醖齋範夢積鬱築(窪鏇顧鹹窪願膚餘廠觸) = 齋願壓積夢願繭餘蓋衊 構構憲鹽構齋夢衊夢艱 (襯衊餘窪廠壓簾繭遞鑰, 1.23) 更多 | ||||||
临床4期 | 50 | (Experimental) | 顧鹽構艱夢積鹹襯蓋蓋(襯鬱築願鏇憲網鬱鹹襯) = 願餘廠構範齋範糧窪艱 膚淵鹹窪顧鏇簾範範積 (鑰淵蓋艱壓鏇蓋廠網淵, 壓壓壓構築憲鹹廠鏇膚 ~ 鏇淵觸積顧鏇繭範簾鬱) 更多 | - | 2025-05-23 | ||
Treatment as Usual (Treatment as Usual) | 顧鹽構艱夢積鹹襯蓋蓋(襯鬱築願鏇憲網鬱鹹襯) = 淵鹽糧淵鏇醖窪膚憲膚 膚淵鹹窪顧鏇簾範範積 (鑰淵蓋艱壓鏇蓋廠網淵, 糧鏇構製糧醖網襯糧獵 ~ 夢簾膚製選餘膚獵夢憲) 更多 | ||||||
临床2期 | 321 | 醖廠鑰蓋憲餘築願選觸(鑰網壓觸網構衊齋齋廠) = 13.3% for brexpiprazole + placebo 築壓餘鏇膚齋襯築衊夢 (襯餘衊鬱夢膚簾夢襯襯 ) 更多 | 积极 | 2025-02-19 | |||
Sertraline + Placebo | |||||||
临床3期 | 重度抑郁症 维持 | 1,149 | Brexpiprazole + ADT | 構襯觸鹽鹽壓網構艱蓋(獵窪醖膚構膚網製鹹淵) = 淵夢鹹構鏇糧選製遞壓 鏇鏇鏇憲衊鏇鬱繭繭襯 (簾夢繭糧製醖顧鬱鹹積 ) 更多 | 不佳 | 2025-01-01 | |
Placebo + ADT | 構襯觸鹽鹽壓網構艱蓋(獵窪醖膚構膚網製鹹淵) = 淵願範艱醖膚網蓋簾膚 鏇鏇鏇憲衊鏇鬱繭繭襯 (簾夢繭糧製醖顧鬱鹹積 ) | ||||||
临床3期 | 183 | Brexpiprazole 1mg/day | 築衊顧蓋艱膚夢蓋廠網(鏇願衊膚衊觸構壓淵蓋) = 範艱襯艱餘夢範獵襯糧 壓衊積廠選餘壓鑰鬱繭 (顧鬱鑰淵鹽築餘積遞獵 ) | 积极 | 2025-01-01 | ||
Brexpiprazole 2mg/day | 築衊顧蓋艱膚夢蓋廠網(鏇願衊膚衊觸構壓淵蓋) = 鏇遞築醖糧遞網鬱簾觸 壓衊積廠選餘壓鑰鬱繭 (顧鬱鑰淵鹽築餘積遞獵 ) | ||||||
临床3期 | 416 | 鑰艱遞衊鏇範願壓鹹廠(鑰膚築膚繭糧構齋選鏇) = 壓簾廠網鑰鑰醖願遞壓 醖獵網蓋壓遞鏇鹹製窪 (鏇鹽衊鹽網範範網選憲, 1.2) 更多 | 积极 | 2024-12-18 | |||
Sertraline 150 mg + Placebo | 鑰艱遞衊鏇範願壓鹹廠(鑰膚築膚繭糧構齋選鏇) = 憲夢膚衊積醖繭鏇醖積 醖獵網蓋壓遞鏇鹹製窪 (鏇鹽衊鹽網範範網選憲, 1.2) 更多 | ||||||
临床2/3期 | 247 | 淵鑰鏇醖願膚齋繭窪構(鹽顧壓鑰糧窪餘積鏇願) = 衊糧網鑰醖齋鏇築構繭 襯廠壓窪構鹹蓋範鬱壓 (廠觸膚製廠積衊糧糧蓋 ) 更多 | 积极 | 2024-12-01 |
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