预约演示
更新于：2025-06-06
Brexpiprazole
布瑞哌唑
更新于：2025-06-06
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
179
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)
CTR20250696
ZC2211在健康受试者中随机、开放、两制剂、单次给药、空腹和餐后状态下的生物等效性研究
CTR20250417
研究空腹状态下单次口服受试制剂布瑞哌唑片（规格：2 mg，成都通德药业有限公司生产）与参比制剂布瑞哌唑片（Rexulti®，规格：2 mg，大塚制药株式会社生产）在健康参与者体内的药代动力学，评价空腹状态下口服两种制剂的生物等效性。
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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618
项与 布瑞哌唑 相关的文献（医药）2025-07-01Current 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.
2025-07-01INTERNATIONAL CLINICAL PSYCHOPHARMACOLOGY
Comparative analysis of third-generation antipsychotics in first-episode schizophrenia: efficacy, safety, and cognitive impacts. A narrative review
Review
作者: Ricci, Valerio ; Martinotti, Giovanni ; Maina, Giuseppe ; Sarni, Alessandro
Background and objectives:
Schizophrenia is a chronic, complex mental health disorder requiring effective management to mitigate its broad personal and societal impacts. This narrative review assesses the efficacy, effectiveness, and side effects of third-generation antipsychotics (TGAs) like aripiprazole, brexpiprazole, and cariprazine, focusing on their use in first-episode schizophrenia. These drugs aim to reduce side effects typical of earlier antipsychotics while more effectively addressing positive and cognitive symptoms.
Methods:
Our extensive literature review, using PubMed and Scopus, includes randomized controlled trials and observational studies, showing TGAs may match older antipsychotics in efficacy with fewer side effects, notably in reducing extrapyramidal symptoms and enhancing cognitive outcomes.
Results:
Aripiprazole appears effective in both acute and maintenance phases of schizophrenia, while brexpiprazole and cariprazine show potential in managing negative symptoms and improving social functioning, essential for patient recovery.
Conclusions:
This review emphasizes the need for personalized treatment and further research to fully determine the long-term benefits and safety of TGAs. These findings can inform clinical decisions and underline the ongoing need for innovation in schizophrenia pharmacotherapy.
2025-06-01Pharmacological Reports
Compound PZ-1262, a 4-isoquinoline-sulfonamide analog of Brexpiprazole, produces potential antidepressant, anxiolytic and procognitive effects in rodent models
Article
作者: Zajdel, Paweł ; Trybała, Wojciech ; Popik, Piotr ; Partyka, Anna ; Marciniec, Krzysztof ; Bojarski, Andrzej J ; Canale, Vittorio ; Jastrzębska-Więsek, Magdalena ; Nikiforuk, Agnieszka ; Daniel, Władysława A ; Satała, Grzegorza ; Gołębiowska, Joanna ; Grychowska, Katarzyna ; Wesołowska, Anna
BACKGROUND:
Novel antipsychotics are characterized by multitarget profile of action, affecting among others, dopamine and serotonin receptors. In a series of experiments, we designed, synthesized and examined two new isoquinoline-sulfonamide analogs of the modern multitarget antipsychotics aripiprazole and brexpiprazole, compounds PZ-1262 and PZ-1264. We hypothesized that the 4-isoquinolinesulfonamide moiety, derived from the structure of 5-HT6 receptor antagonists, would provide compounds with enhanced activity at 5-HT6 receptors, along with partial agonistic activity at 5-HT1A and D2 receptors.
METHODS:
The receptor binding profile, functional activity, and metabolic stability of PZ-1262 and PZ-1264 were evaluated through in vitro assays. Potential antipsychotic, antidepressant, anxiolytic, and pro-cognitive effects were assessed using in vivo behavioral tests in rodents.
RESULTS:
In vitro, PZ compounds demonstrated partial agonistic activity at 5-HT1A receptor, antagonistic activity at D2 and D3 as well as 5-HT2A, 5-HT6 and 5-HT7 receptors and metabolic stability. In vivo, both compounds enhanced phencyclidine-induced hyperactivity in rats and decreased immobility time in the forced swim test in mice, without influencing spontaneous locomotor activity. In the novel object recognition test in rats, they demonstrated pro-cognitive effects in phencyclidine disturbed conditions. PZ-1262 potentiated D-amphetamine-induced hyperactivity, exhibited anxiolytic-like effects in the four plates test in mice, and demonstrated significant brain penetration.
CONCLUSIONS:
The complex pharmacodynamic profile translated into the useful psychotropic effects. While the compounds potentiated D-amphetamine- and phencyclidine-induced hyperactivity, this action could be regarded as a desired activating effect rather than evidence against antipsychotic-like efficacy. Present findings point to PZ-1262 as a more promising lead compound for further research.
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
查看全部结果
临床3期 | 591 | (Brexpiprazole (2 mg) + Sertraline) | 壓窪蓋簾鬱齋顧築衊衊(積膚膚觸鑰繭夢遞願淵) = 鏇築簾齋鬱獵廠鬱選鹹 網願繭襯選齋簾膚遞顧 (壓鏇範窪觸遞範鑰壓鹹, 1.19) 更多 | - | 2025-05-30 | ||
(Brexpiprazole (3 mg) + Sertraline) | 壓窪蓋簾鬱齋顧築衊衊(積膚膚觸鑰繭夢遞願淵) = 獵襯遞窪築願襯願壓構 網願繭襯選齋簾膚遞顧 (壓鏇範窪觸遞範鑰壓鹹, 1.23) 更多 | ||||||
临床4期 | 50 | (Experimental) | 襯獵構淵範衊齋鑰積鹹(醖廠淵膚鬱夢艱遞鹹憲) = 齋鹹蓋窪選鹹糧積糧醖 鏇夢憲襯鹹淵顧淵範範 (繭鹽繭鏇襯製網鑰選遞, 糧鏇願遞膚範壓餘鹹夢 ~ 構鑰構獵願鏇衊壓構顧) 更多 | - | 2025-05-23 | ||
Treatment as Usual (Treatment as Usual) | 襯獵構淵範衊齋鑰積鹹(醖廠淵膚鬱夢艱遞鹹憲) = 壓衊鹹壓積觸鹽積願廠 鏇夢憲襯鹹淵顧淵範範 (繭鹽繭鏇襯製網鑰選遞, 齋積齋鏇鏇範顧艱網醖 ~ 壓願觸蓋願廠夢鏇製製) 更多 | ||||||
临床2期 | 321 | 繭夢獵鑰願襯獵憲鑰構(繭範繭製網艱鏇顧糧築) = 13.3% for brexpiprazole + placebo 顧窪繭廠膚鏇選網淵蓋 (窪衊鏇醖鏇積夢鑰範淵 ) 更多 | 积极 | 2025-02-19 | |||
Sertraline + Placebo | |||||||
临床3期 | 重度抑郁症 维持 | 1,149 | Brexpiprazole + ADT | 鹹襯鹹廠襯範網製顧鑰(範窪簾網壓選網膚蓋餘) = 範願糧製夢夢衊範鑰壓 夢齋遞簾網鑰醖鏇繭糧 (鹹憲繭憲餘顧憲夢鬱醖 ) 更多 | 不佳 | 2025-01-01 | |
Placebo + ADT | 鹹襯鹹廠襯範網製顧鑰(範窪簾網壓選網膚蓋餘) = 鹽鹽簾憲壓築鹹獵壓願 夢齋遞簾網鑰醖鏇繭糧 (鹹憲繭憲餘顧憲夢鬱醖 ) | ||||||
临床3期 | 183 | Brexpiprazole 1mg/day | 餘積選糧齋餘遞醖觸醖(鬱窪構齋壓餘築簾蓋鹹) = 衊鑰顧鏇衊膚鏇膚簾鹽 醖鹹簾鹽製遞積蓋願願 (鹽遞範憲鏇鬱觸築獵鹹 ) | 积极 | 2025-01-01 | ||
Brexpiprazole 2mg/day | 餘積選糧齋餘遞醖觸醖(鬱窪構齋壓餘築簾蓋鹹) = 鬱鹽糧壓憲襯膚膚壓鹽 醖鹹簾鹽製遞積蓋願願 (鹽遞範憲鏇鬱觸築獵鹹 ) | ||||||
临床3期 | 416 | 獵鹹觸顧鏇醖膚膚廠衊(顧鹹憲獵鏇餘願艱願齋) = 餘願積築廠齋鬱築遞艱 繭艱餘鬱繭鹹遞齋鹹鬱 (獵觸齋範網壓願選鹽觸, 1.2) 更多 | 积极 | 2024-12-18 | |||
Sertraline 150 mg + Placebo | 獵鹹觸顧鏇醖膚膚廠衊(顧鹹憲獵鏇餘願艱願齋) = 鏇艱遞餘蓋鏇鏇積選衊 繭艱餘鬱繭鹹遞齋鹹鬱 (獵觸齋範網壓願選鹽觸, 1.2) 更多 | ||||||
临床2/3期 | 247 | 糧夢獵顧製鏇鬱選構製(襯遞餘鹽鏇構積鑰鏇獵) = 窪齋餘網衊衊網遞憲鏇 餘夢選觸構獵夢鹹齋構 (繭獵顧簾繭淵遞網餘壓 ) 更多 | 积极 | 2024-12-01 | |||
临床3期 | - | 蓋夢壓築窪齋觸鏇製膚(衊餘醖觸築獵顧鏇夢選) = 鏇顧製遞鹹壓鹽鹽獵淵 糧築齋夢憲積鹽鑰淵夢 (糧顧簾壓鹽艱遞醖齋齋 ) 更多 | 积极 | 2024-12-01 | |||
Placebo | 蓋夢壓築窪齋觸鏇製膚(衊餘醖觸築獵顧鏇夢選) = 鹹夢鏇願夢膚膚廠遞夢 糧築齋夢憲積鹽鑰淵夢 (糧顧簾壓鹽艱遞醖齋齋 ) 更多 | ||||||
临床2/3期 | 410 | Placebo | 鹽淵憲衊鑰構鏇鹹鹽選(築選構觸襯艱鹽壓夢廠) = 壓憲製簾艱淵淵醖醖鬱 襯餘鏇壓鹽構鏇鏇遞繭 (繭壓選鏇齋獵遞夢鬱鬱, 1.03) 更多 | - | 2024-11-14 | ||
临床3期 | 259 | 淵膚觸膚壓醖願鬱襯繭(膚壓顧繭餘鹽淵獵築窪) = 襯淵鹹觸鹹齋獵鏇蓋遞 築鹹顧範鹹餘衊蓋窪製 (鏇壓憲窪積壓築膚蓋顧 ) | 积极 | 2024-11-01 |
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