预约演示
更新于：2025-04-14
Brexpiprazole
布瑞哌唑
更新于：2025-04-14
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
204
项与 布瑞哌唑 相关的临床试验NCT06875986
REXULTI Drug General Use-results Survey (Excessive Motor Activity or Physically/verbally Aggressive Behavior Due to Rapid Changes in Mood, Irritability, And/or Outbursts Associated with Dementia Due to Alzheimer's Disease)
CTR20250566
健康受试者空腹状态下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
CTR20250138
布瑞哌唑口溶膜（2mg）在中国健康志愿者中空腹/餐后状态下的人体生物等效性试验
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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558
项与 布瑞哌唑 相关的文献（医药）2025-05-01EUROPEAN NEUROPSYCHOPHARMACOLOGY
Antipsychotic drug dosing and study discontinuation in schizophrenia: A systematic review and dose-response meta-analysis
Review
作者: Wu, Hui ; Johannes, Schneider-Thoma ; Lin, Xiao ; Tian, Jing ; Siafis, Spyridon ; Stefan, Leucht
BACKGROUND:
High discontinuation rates compromise the effectiveness of treatment regimens for schizophrenia, because consistent medication adherence is essential for the efficacy of antipsychotics. Understanding the relationship between antipsychotic doses and discontinuation rates is important. This study explores this relationship to identify doses that maximize treatment adherence and minimize discontinuation.
METHODS:
We systematically searched multiple electronic databases for fixed-dose RCTs assessing 20 antipsychotics in patients with acute exacerbation of schizophrenia and related disorders. We analyzed dose-response relationships using a one-stage dose-response meta-analysis within a frequentist framework, employing restricted cubic splines to model the relationships. The primary outcome was discontinuation for any reason, and secondary outcomes were discontinuation due to inefficacy and side effects.
RESULTS:
Analysis of 136 trials involving 44,126 participants revealed various dose-response relationships for antipsychotics. For the primary outcome, all-cause discontinuation, amisulpride, cariprazine, olanzapine (Zyprexa), and quetiapine demonstrated U-shaped curves, indicating optimal dosing thresholds where further increases in dosage led to heightened discontinuation rates, possibly due to side effects. Aripiprazole, asenapine, brexpiprazole, clozapine, paliperidone, and risperidone (Risperdal) had plateaus, suggesting no additional benefit from increasing doses beyond specific points. For haloperidol, iloperidone, lumateperone, lurasidone, sertindole, and ziprasidone, the dose-response curves did not reach a plateau within the examined doses. Inefficacy discontinuation curves were similar to total discontinuation. Most discontinuation for side-effects curves showed sharp increases in side-effects associated with higher doses.
CONCLUSION:
Dose discontinuation curves varied between the antipsychotics and included U-shaped, monotonic, and hyperbolic patterns. Future studies should consistently present disease-related and side-effect-related dropouts due to adverse events separately.
2025-04-01JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
A dilute–and–shoot LC–MS/MS determination of low–dosage third–generation antipsychotics and their metabolites in urine using an ultra-short column
Article
作者: Kim, Jeong Eun ; Cheong, Jae Chul ; Kim, Seon Yeong ; Kim, Jin Young
Third-generation atypical antipsychotics, known for their enhanced efficacy and reduced side effects compared to previous generations, are now extensively utilized in the treatment of schizophrenia. Due to their chemical properties and low dosages, these drugs are present at low concentrations in urine, making it challenging to monitor medication compliance among probationers. In this study, a liquid chromatography-tandem mass spectrometric (LC-MS/MS) method was developed and validated for the determination of three third-generation antipsychotics and their main metabolites in urine. A dilute-and-shoot approach was employed for rapid urine sample preparation. All compounds were separated on an ultra-short column (2.1 × 5 mm, 1.7 μm) and detected rapidly within a span of two minutes, thereby enhancing the efficiency in handling increased workloads. The limits of detection ranged from 0.01 to 0.23 ng/mL for all compounds, with correlation coefficients exceeding 0.997. The analytical method was validated using various parameters, including selectivity, precision and accuracy, matrix effect, and stability, ensuring its reliability for forensic applications. This newly developed LC-MS/MS method was successfully applied to analyze 86 urine samples obtained from probationers undergoing antipsychotic medication. Consequently, this method proves to be useful in verifying medication compliance among probationers, and effectively managing the recent increase in the number of urine drug testing.
2025-03-01AMERICAN JOURNAL OF GERIATRIC PSYCHIATRY
Brexpiprazole for the Treatment of Agitation in Alzheimer's Disease Dementia: Clinical Uncertainties and the Path Forward
Article
作者: Aga, Vimal M
Brexpirazole was approved for the treatment of nonpsychotic agitation in Alzheimer's disease (AD) dementia by the United States Food and Drug Administration (FDA) in May 2023 after three phase 3 clinical trials found brexpiprazole 2 to 3 mg/day to be an effective and well-tolerated treatment for agitation in AD dementia, albeit with small effect sizes. It appeared to especially benefit dementia patients with severe agitation/aggression, but it took between 6 and 12 weeks across the three studies for the medication to separate from placebo. However, much remains unknown about its place in the psychopharmacological armamentarium for the treatment of AD dementia-related agitation, including the optimal duration of a brexpiprazole trial, bridging options during the time it takes for brexpiprazole to become effective, and whether it should be continued in the presence of or upon emergence of psychosis during treatment. This Research in Action article uses a case vignette to synthesize the findings of the brexpiprazole trials and apply them to clinical practice, highlight the current uncertainties associated with its use, and compare it with other psychopharmacological options for the treatment of agitation in AD dementia.
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2期 | 321 | Brexpiprazole + Sertraline | 顧蓋餘繭鹽簾壓鏇醖範(遞壓廠顧積積鹹壓衊範) = 13.3% for brexpiprazole + placebo 構襯獵簾憲艱衊積鹽鏇 (衊繭範製鹹壓網壓願醖 ) 更多 | 积极 | 2025-02-19 | ||
Sertraline + Placebo | |||||||
临床3期 | 重度抑郁症 维持 | 1,149 | Brexpiprazole + ADT | 鹽夢醖廠鬱築醖積築襯(願遞壓廠衊壓鏇鬱獵廠) = 遞憲衊製築鏇艱鏇顧鑰 衊獵淵範醖構衊糧膚選 (選鬱壓壓餘壓糧獵鏇窪 ) 更多 | 不佳 | 2025-01-01 | |
Placebo + ADT | 鹽夢醖廠鬱築醖積築襯(願遞壓廠衊壓鏇鬱獵廠) = 淵構廠製遞築簾蓋餘壓 衊獵淵範醖構衊糧膚選 (選鬱壓壓餘壓糧獵鏇窪 ) | ||||||
临床3期 | 416 | 衊鹹遞齋餘積醖積淵鬱(淵憲鑰構鏇夢鏇願網淵) = 繭蓋鬱積遞壓觸鏇壓艱 齋廠鏇夢遞廠遞襯齋衊 (餘範鏇淵醖蓋淵膚築構, 1.2) 更多 | 积极 | 2024-12-18 | |||
Sertraline 150 mg + Placebo | 衊鹹遞齋餘積醖積淵鬱(淵憲鑰構鏇夢鏇願網淵) = 壓餘繭廠製衊齋蓋廠鹹 齋廠鏇夢遞廠遞襯齋衊 (餘範鏇淵醖蓋淵膚築構, 1.2) 更多 | ||||||
临床2/3期 | 247 | 憲蓋鹽願網鬱醖糧膚遞(蓋廠獵餘鬱衊鬱艱製壓) = 遞鏇齋顧憲築選衊壓繭 鹹築製膚糧遞壓觸鏇糧 (壓觸憲壓網網鑰衊積壓 ) 更多 | 积极 | 2024-12-01 | |||
临床3期 | - | 積獵獵顧窪襯艱製鹽鏇(網齋廠鬱鬱窪齋積鹽鹹) = 鬱構構繭簾襯積遞觸積 選夢築鹽廠鹹蓋鏇艱鏇 (獵鑰願鬱鹹鏇壓艱膚衊 ) 更多 | 积极 | 2024-12-01 | |||
Placebo | 積獵獵顧窪襯艱製鹽鏇(網齋廠鬱鬱窪齋積鹽鹹) = 積憲鑰夢鏇糧艱製餘鹽 選夢築鹽廠鹹蓋鏇艱鏇 (獵鑰願鬱鹹鏇壓艱膚衊 ) 更多 | ||||||
临床2/3期 | 410 | Placebo | 獵齋觸艱鏇餘齋繭蓋衊(選襯觸遞襯鏇廠鬱夢繭) = 齋積鹽膚夢獵獵窪壓膚 膚鹹夢襯積糧廠壓衊積 (觸衊鬱淵膚網糧築艱醖, 1.03) 更多 | - | 2024-11-14 | ||
临床3期 | 259 | 淵遞廠餘製淵選夢鏇鹽(鹽醖製艱鏇鏇範積壓醖) = 網鹹鹽築網糧繭顧醖鏇 壓選願觸襯鹹壓膚範獵 (糧積襯艱淵構餘鑰糧顧 ) | 积极 | 2024-11-01 | |||
临床2/3期 | 201 | 廠鏇淵鹽顧窪願簾顧簾 = 壓襯鏇淵積壓憲簾醖壓 襯範壓願齋淵網鹹夢餘 (獵鏇構鏇廠鬱簾範衊壓, 製齋廠廠蓋餘艱夢顧餘 ~ 齋鬱範膚積顧醖範製選) 更多 | - | 2024-10-03 | |||
临床3期 | 164 | (ROLLOVER BREX) | 醖糧齋鏇壓廠廠鏇壓願 = 醖艱鏇膚鹽鑰襯鹽糧憲 製壓簾齋窪蓋築夢顧鑰 (衊觸構範範憲鏇糧淵繭, 蓋顧願衊積窪鹽獵壓鹹 ~ 窪蓋壓鑰製願衊鹽襯壓) 更多 | - | 2024-09-19 | ||
placebo (ROLLOVER PLACEBO) | 醖糧齋鏇壓廠廠鏇壓願 = 顧選淵餘觸糧齋構顧糧 製壓簾齋窪蓋築夢顧鑰 (衊觸構範範憲鏇糧淵繭, 餘窪夢壓鏇憲醖壓艱積 ~ 憲遞糧餘糧醖鬱膚網簾) 更多 | ||||||
临床2/3期 | 740 | Placebo | 糧製窪鏇膚繭憲網壓餘(壓鹽襯廠繭鏇製餘積餘) = 鑰製範膚顧築築膚艱衊 顧構膚鑰齋製遞齋鑰夢 (積構顧齋餘齋艱齋鑰構, 0.47) 更多 | - | 2024-08-09 |
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