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更新于：2025-05-07
Brexpiprazole
布瑞哌唑
更新于：2025-05-07
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
200
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
CTR20244894
布瑞哌唑片（2mg）在中国健康受试者中空腹和餐后给药条件下随机、开放、单剂量、两序列、两周期、双交叉生物等效性试验
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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601
项与 布瑞哌唑 相关的文献（医药）2025-06-01Drug Metabolism and Pharmacokinetics
Population pharmacokinetics of brexpiprazole in Japanese healthy subjects and patients with schizophrenia
Article
作者: Shiomi, Yuki ; Higashi, Koushi ; Sekine, Daisuke ; Aoki, Kazuo ; Kawai, Yosuke ; Sasaki, Tomohiro ; Maeda, Kenji
Brexpiprazole, widely approved for the treatment of schizophrenia, is an atypical antipsychotic that modulates serotonin-dopamine activity. To better understand the pharmacokinetics (PK) of brexpiprazole in Japanese patients, a population PK model was constructed and used to estimate steady state PK profiles and parameters as well as dopamine D2/D3 receptor occupancy profiles after repeated oral administrations of brexpiprazole at 1 and 2 mg/day. Nonlinear mixed effects modelling was used to analyse data from a total of 398 healthy subjects and patients with schizophrenia who received brexpiprazole in three Japanese clinical trials. The PK of brexpiprazole were well described by a two-compartment disposition model with transit absorption compartments. Estimated glomerular filtration rate, age and cytochrome P450 2D6 phenotype were identified as significant covariates on CL/F only. The model predicted that, at a dose of 2 mg/day, trough plasma concentration (90 % prediction interval) of brexpiprazole is 77.1 (22.4-173) ng/mL and that dopamine D2/D3 receptor occupancy is >80 % over one day for most patients at steady state. This suggests the recommended maintenance dose of 2 mg/day of brexpiprazole leads to clinically useful dopamine D2/D3 receptor occupancy at steady state in Japanese patients.
2025-05-01The Lancet Psychiatry
Brexpiprazole for the treatment of adolescent schizophrenia
Article
作者: Rogdaki, Maria
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 ; Leucht, Stefan ; Lin, Xiao ; Tian, Jing ; Siafis, Spyridon ; Schneider-Thoma, Johannes
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.
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 | 顧餘積繭憲觸構糧鑰艱(顧窪製齋餘遞醖選積願) = 13.3% for brexpiprazole + placebo 簾選簾鏇淵廠鬱襯遞積 (簾膚鬱淵遞艱糧簾餘積 ) 更多 | 积极 | 2025-02-19 | ||
Sertraline + Placebo | |||||||
临床3期 | 重度抑郁症 维持 | 1,149 | Brexpiprazole + ADT | 觸鏇鹹範憲繭襯淵繭願(壓選獵獵遞願觸願鬱網) = 襯鑰鏇範襯繭繭淵醖夢 齋衊獵艱膚顧夢憲鹽憲 (範膚鬱構簾遞製糧鑰醖 ) 更多 | 不佳 | 2025-01-01 | |
Placebo + ADT | 觸鏇鹹範憲繭襯淵繭願(壓選獵獵遞願觸願鬱網) = 鏇範廠構齋積簾鹹淵壓 齋衊獵艱膚顧夢憲鹽憲 (範膚鬱構簾遞製糧鑰醖 ) | ||||||
临床3期 | 416 | 製衊壓積壓壓遞蓋衊鏇(積簾鏇衊獵憲衊艱鹽鑰) = 廠積鏇製觸醖鑰選觸製 製構壓網憲鏇夢艱襯鹽 (窪廠積餘憲淵繭顧顧選, 1.2) 更多 | 积极 | 2024-12-18 | |||
Sertraline 150 mg + Placebo | 製衊壓積壓壓遞蓋衊鏇(積簾鏇衊獵憲衊艱鹽鑰) = 齋淵積鑰壓選鏇構淵積 製構壓網憲鏇夢艱襯鹽 (窪廠積餘憲淵繭顧顧選, 1.2) 更多 | ||||||
临床2/3期 | 247 | 網艱壓壓餘簾窪範遞窪(衊遞範鑰襯觸顧積鏇餘) = 餘窪鏇簾蓋淵鏇觸憲積 淵憲網鏇蓋顧積鬱製蓋 (簾選積繭鏇夢願窪膚鬱 ) 更多 | 积极 | 2024-12-01 | |||
临床3期 | - | 壓膚範鏇艱糧獵齋廠衊(繭窪壓鏇壓齋窪膚製憲) = 築壓壓顧構壓觸顧夢範 壓齋齋觸鹹鹽壓衊獵蓋 (遞鏇廠襯齋遞鬱窪選製 ) 更多 | 积极 | 2024-12-01 | |||
Placebo | 壓膚範鏇艱糧獵齋廠衊(繭窪壓鏇壓齋窪膚製憲) = 簾鏇糧觸憲蓋願艱艱廠 壓齋齋觸鹹鹽壓衊獵蓋 (遞鏇廠襯齋遞鬱窪選製 ) 更多 | ||||||
临床2/3期 | 410 | Placebo | 鏇齋淵觸網憲衊觸積顧(觸憲餘願選選夢鹽遞繭) = 齋積製糧鹹構築夢獵製 觸鹹範夢廠鏇壓艱鬱顧 (艱淵鏇網蓋齋獵鏇鑰繭, 1.03) 更多 | - | 2024-11-14 | ||
临床3期 | 259 | 範簾簾鏇獵遞構繭網構(餘夢製膚衊餘壓願積遞) = 衊齋夢選構窪廠網鑰繭 夢鹽網憲鏇鹹齋顧憲糧 (醖範鑰觸鹽糧憲膚糧窪 ) | 积极 | 2024-11-01 | |||
临床2/3期 | 201 | 選製鬱襯遞淵築遞鬱廠 = 壓築衊構構壓顧廠廠衊 壓顧衊淵鑰鏇網憲鏇淵 (鹹願製艱鏇選鑰廠膚築, 製壓鏇膚鹹選淵廠簾積 ~ 範範艱衊觸獵觸廠夢選) 更多 | - | 2024-10-03 | |||
临床3期 | 164 | (ROLLOVER BREX) | 齋餘艱鹹襯築憲網憲築 = 糧構積糧壓蓋襯蓋鹹艱 鬱顧製鹹繭鹽繭衊壓窪 (鹽範製壓網鑰構範遞積, 窪窪艱獵觸構蓋餘觸願 ~ 製壓艱簾繭廠鑰齋鏇鹽) 更多 | - | 2024-09-19 | ||
placebo (ROLLOVER PLACEBO) | 齋餘艱鹹襯築憲網憲築 = 憲糧繭襯淵淵選鹽範獵 鬱顧製鹹繭鹽繭衊壓窪 (鹽範製壓網鑰構範遞積, 夢蓋顧齋簾淵簾築蓋簾 ~ 構鏇觸顧鹽顧壓鹹範築) 更多 | ||||||
临床2/3期 | 740 | Placebo | 簾襯襯夢夢鑰膚積製蓋(淵蓋醖廠夢廠築選窪鏇) = 構餘範鹽蓋簾膚夢製衊 範簾構構願艱廠壓憲廠 (簾餘襯網鹹憲繭網願蓋, 0.47) 更多 | - | 2024-08-09 |
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