更新于：2024-12-25
Amisulpride
氨磺必利
更新于：2024-12-25
概要
基本信息
药物类型 小分子化药 |
别名 4-Amino-N-((1-ethyl-2-pyrrolidinyl)methyl)-5-(ethylsulfonyl)-2-methoxybenzamide、4-Amino-N-((1-ethyl-2-pyrrolidinyl)methyl)-5-(ethylsulfonyl)-O-anisamide、Aminosultopride + [17] |
作用机制 D2 receptor拮抗剂(多巴胺D2受体拮抗剂)、D3 receptor拮抗剂(多巴胺D3受体拮抗剂) |
治疗领域 |
非在研适应症 |
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- |
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结构
分子式C17H27N3O4S |
InChIKeyNTJOBXMMWNYJFB-UHFFFAOYSA-N |
CAS号71675-85-9 |
关联
105
项与 氨磺必利 相关的临床试验Comparison of Amisulpride vs Ondansetron in the prophylaxis of Post Operative Nausea and Vomiting in abdominal surgeries: a randomized controlled study. - NIL
Comparison of Amisulpride versus Dexamethasone for prevention of PONV after laparoscopy assisted vaginal hysterectomy - Nil
评价上海则正医药科技股份有限公司研发的氨磺必利口崩片与市售阿立哌唑口崩片和利培酮口崩片在中国健康人群中的口感对比评价研究
100 项与 氨磺必利 相关的临床结果
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100 项与 氨磺必利 相关的转化医学
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100 项与 氨磺必利 相关的专利（医药）
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1,264
项与 氨磺必利 相关的文献（医药）2024-12-01NEUROPSYCHOPHARMACOLOGY
PET clinical study of novel antipsychotic LB-102 demonstrates unexpectedly prolonged dopamine receptor target engagement
Article
作者: Prensky, Zachary ; Nicol, Ginger ; Kuwabara, Hiroto ; Wong, Dean F. ; Schindler, Thomas H ; Grattan, Vincent T ; Grattan, Vincent T. ; Wong, Dean F ; Tian, Lucy ; Eramo, Anna ; Hixon, Mark S ; Schindler, Thomas H. ; Chand, Ganesh B. ; Vaino, Andrew R. ; Caito, Nicole ; Lessie, Erin ; Hixon, Mark S. ; Vaino, Andrew R ; Chand, Ganesh B ; Gründer, Gerhard ; Valenta, Ines
Abstract:
Regulation of dopamine activity has important clinical consequences, most notably in schizophrenia. LB-102, N-methyl amisulpride, is a novel dopamine D2/3/5-HT7 inhibitor being developed as a treatment for schizophrenia and other psychiatric disorders. The characteristic that is common to all current antipsychotics is their engagement of D2 dopamine receptors. The goal of this study was to measure the dopamine receptor occupancy of orally administered LB-102 at three different doses (50, 75, and 100 mg as single doses and 50 and 100 mg as multiple doses) and at different timepoints in healthy volunteers using positron emission tomography (PET) with 11C raclopride as a radiotracer. Results of this study (NCT04588129) showed that steady-state once daily oral dosing of 50 mg LB-102 afforded striatal dopamine occupancy (RO) in the desired 60–80% range consistently over the course of 24 h. Contrary to the often observed relationship between RO vs plasma concentrations, maximum dopamine RO significantly lagged maximum plasma concentration and showed little variability under steady state conditions. A similar phenomenon has recently been reported with a non-racemic version of amisulpride [1]. LB-102 was generally safe and well-tolerated at all doses. Results of this study were used to inform dosing in a subsequent Phase 2 clinical study in schizophrenia patients.
2024-12-01RADIOTHERAPY AND ONCOLOGY
Effects of dopamine receptor antagonists and radiation on mouse neural stem/progenitor cells
Article
作者: Pajonk, Frank ; Ioannidis, Angeliki ; He, Ling ; Bhat, Kruttika
BACKGROUND:
Dopamine receptor antagonists have recently been identified as potential anti-cancer agents in combination with radiation, and a first drug of this class is in clinical trials against pediatric glioma. Radiotherapy causes cognitive impairment primarily by eliminating neural stem/progenitor cells and subsequent loss of neurogenesis, along with inducing inflammation, vascular damage, and synaptic alterations. Here, we tested the combined effects of dopamine receptor antagonists and radiation on neural stem/progenitor cells.
METHODS:
Using transgenic mice that report the presence of neural stem/progenitor cells through Nestin promoter-driven expression of EGFP, the effects of dopamine receptor antagonists alone or in combination with radiation on neural stem/progenitor cells were assessed in sphere-formation assays, extreme limiting dilution assays, flow cytometry and real-time PCR in vitro and in vivo in both sexes.
RESULTS:
We report that hydroxyzine and trifluoperazine exhibited sex-dependent effects on murine newborn neural stem/progenitor cells in vitro. In contrast, amisulpride, nemonapride, and quetiapine, when combined with radiation, significantly increased the number of neural stem/progenitor cells in both sexes. In vivo, trifluoperazine showed sex-dependent effects on adult neural stem/progenitor cells, while amisulpride demonstrated significant effects in both sexes. Further, amisulpride increased sphere forming capacity and stem cell frequency in both sexes when compared to controls.
CONCLUSION:
We conclude that a therapeutic window for dopamine receptor antagonists in combination with radiation potentially exists, making it a novel combination therapy against glioblastoma. Normal tissue toxicity following this treatment scheme likely differs depending on age and sex and should be taken into consideration when designing clinical trials.
2024-12-01SCHIZOPHRENIA RESEARCH
Efficacy and tolerability of blonanserin in schizophrenia: A systematic review and meta-analysis of randomized controlled trials
Review
作者: Dong, Shimeng ; Schneider-Thoma, Johannes ; Wu, Hui ; Yanagimoto, Hiroko ; Lin, Xiao ; Tian, Jing ; Nomura, Nobuyuki ; Leucht, Stefan ; Qin, Mengchang ; Siafis, Spyridon
BACKGROUND:
Blonanserin is approved for treating schizophrenia in Japan, South Korea, India, and China. We aimed to synthesize the efficacy and tolerability of blonanserin compared to other antipsychotics.
METHODS:
A systematic review and pairwise meta-analysis were conducted using the Cochrane Schizophrenia Group's study-based trial register until January 24, 2024. We included open and blinded randomized controlled trials (RCTs) involving schizophrenia patients, with studies lasting at least 3 weeks. Primary outcomes focused on overall schizophrenia symptoms using rating scales and relapse rates. Secondary outcomes included symptom subtypes, treatment response, dropout rates, quality of life, and side effects, analyzed using standardized mean difference (SMD), mean difference (MD), and risk ratio (RR) with 95 % confidence intervals (CIs). The review protocol was published in Open Science Framework (https://osf.io/e7jfa/).
RESULTS:
Fourteen acute-phase studies with 2697 participants compared blonanserin to olanzapine, haloperidol, risperidone, paliperidone, aripiprazole, amisulpride, and placebo. Blonanserin showed greater efficacy than placebo (SMD = -0.47, 95 % CI: -0.66 to -0.27) and similar efficacy to other antipsychotics in reducing schizophrenia overall symptoms. No data on the number of participants who experienced relapse with blonanserin was available in the single maintenance-phase study. There were also no clear differences between antipsychotics in most secondary efficacy outcomes, but blonanserin produced less prolactin and weight increase but more akathisia and tremor than risperidone, and less prolactin increase, anticholinergic and extrapyramidal side-effects than haloperidol.
CONCLUSION:
Our study suggests that differences in efficacy between blonanserin and other antipsychotics are small and that blonanserin has a different tolerability profile than haloperidol and risperidone.
100 项与 氨磺必利 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 |
|---|---|---|---|
| 术后恶心呕吐 | 美国 | 2020-02-26 | |
| 精神分裂症 | 中国 | 2004-06-04 | |
| 急性精神分裂症 | 澳大利亚 | 2002-02-01 | |
| 慢性精神分裂症 | 澳大利亚 | 2002-02-01 |
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 |
|---|---|---|---|---|
| 恶心和呕吐 | 临床3期 | 中国 | 2023-01-12 | |
| 恶心和呕吐 | 临床3期 | 中国 | 2023-01-12 | |
| 恶心 | 临床3期 | 法国 | 2013-07-01 | |
| 恶心 | 临床3期 | 德国 | 2013-07-01 | |
| 呕吐 | 临床3期 | 法国 | 2013-07-01 | |
| 呕吐 | 临床3期 | 德国 | 2013-07-01 | |
| 化疗引起的恶心和呕吐 | 临床2期 | 丹麦 | 2011-02-01 | |
| 化疗引起的恶心和呕吐 | 临床2期 | 英国 | 2011-02-01 | |
| 躁郁症1型 | 临床2期 | 捷克 | 2004-05-01 | |
| 躁郁症1型 | 临床2期 | 法国 | 2004-05-01 |
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临床结果
临床结果
适应症
分期
评价
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临床4期 | - | 60 | (Amisulpride Group) | 衊襯廠鏇齋獵醖衊構鏇(窪廠築選鏇築遞觸鹹蓋) = 鑰淵鬱網窪膚鑰壓廠壓 遞膚觸衊窪蓋網鹽憲壓 (遞憲蓋糧顧鬱膚衊範衊, 觸觸願淵餘壓網製壓願 ~ 窪淵夢遞鬱選鹽膚鹹範) 更多 | - | 2024-09-19 | |
Olanzapine-Fluoxetine Combination (Olanzapine-Fluoxetine Group) | 衊襯廠鏇齋獵醖衊構鏇(窪廠築選鏇築遞觸鹹蓋) = 膚繭範夢觸餘齋遞顧壓 遞膚觸衊窪蓋網鹽憲壓 (遞憲蓋糧顧鬱膚衊範衊, 鹽遞淵顧遞網範衊鏇夢 ~ 憲艱憲鏇鬱範衊積鏇膚) 更多 | ||||||
Pubmed 人工标引  | N/A | 25 | 餘齋鏇積壓襯獵淵廠蓋(鹹構醖鏇積憲衊醖窪鬱) = not statistically significant 鬱願艱膚壓製齋觸積壓 (願構糧廠鹹蓋夢願願構 ) 更多 | 积极 | 2022-08-31 | ||
临床3期 | 465 | 餘廠襯網鹽鬱醖繭鹽夢(襯選鹽窪顧鬱餘淵鏇糧) = 餘膚範範選簾襯餘齋夢 夢齋簾醖鏇繭夢憲憲積 (糧繭網餘夢積鹽範淵鬱 ) 更多 | 积极 | 2022-06-02 | |||
Placebo | 餘廠襯網鹽鬱醖繭鹽夢(襯選鹽窪顧鬱餘淵鏇糧) = 窪夢顧鬱選選構觸獵願 夢齋簾醖鏇繭夢憲憲積 (糧繭網餘夢積鹽範淵鬱 ) 更多 | ||||||
临床1期 | 30 | 憲顧廠遞淵築範獵鹽範(觸鹹窪餘鏇選鏇鹹鏇襯) = 獵獵糧觸淵製獵夢鏇選 獵遞選憲範夢廠願餘網 (鏇襯膚選製繭齋鹽衊鑰, 3.53 ~ 6.96) | 积极 | 2019-12-09 | |||
憲顧廠遞淵築範獵鹽範(觸鹹窪餘鏇選鏇鹹鏇襯) = 簾獵鬱鹽窪鏇鬱築網選 獵遞選憲範夢廠願餘網 (鏇襯膚選製繭齋鹽衊鑰, 55.48 ~ 9.16) | |||||||
临床3期 | 368 | (APD421) | 餘襯選膚艱壓網製艱齋(蓋衊艱鏇餘鹹願鏇蓋顧) = 衊糧遞淵鬱獵夢艱夢鏇 鬱構構餘製鏇遞願鹽鑰 (衊憲糧鏇壓構範醖鑰網, 範選糧鑰獵鑰淵廠築顧 ~ 範範願獵窪構築膚襯窪) 更多 | - | 2019-08-02 | ||
Placebo (Placebo) | 餘襯選膚艱壓網製艱齋(蓋衊艱鏇餘鹹願鏇蓋顧) = 鏇襯壓鏇壓襯膚壓願繭 鬱構構餘製鏇遞願鹽鑰 (衊憲糧鏇壓構範醖鑰網, 製壓糧壓積蓋壓齋糧膚 ~ 蓋鏇膚構窪觸選艱鏇製) 更多 | ||||||
临床2期 | 342 | 鬱艱範艱蓋觸鹽顧觸餘(窪齋獵廠膚壓衊夢窪獵) = 構廠衊築鹹鹽鹽鏇顧醖 願膚鏇顧窪淵選選窪艱 (窪範簾製網築醖繭願顧 ) | 积极 | 2019-07-01 | |||
Placebo | 鬱艱範艱蓋觸鹽顧觸餘(窪齋獵廠膚壓衊夢窪獵) = 憲簾獵蓋壓遞廠鬱襯廠 願膚鏇顧窪淵選選窪艱 (窪範簾製網築醖繭願顧 ) | ||||||
临床2期 | 342 | (Control) | 膚壓選遞夢獵壓壓夢簾(繭選廠糧顧獵餘繭齋窪) = 繭遞構蓋齋餘襯構衊襯 簾膚願鹹艱簾齋構鹹襯 (鏇觸衊窪廠壓觸鹹鬱願, 糧獵網憲製衊範鬱夢醖 ~ 構鹽範鏇襯窪鹹糧壓網) 更多 | - | 2019-03-12 | ||
(PLACEBO) | 膚壓選遞夢獵壓壓夢簾(繭選廠糧顧獵餘繭齋窪) = 遞餘簾構醖範鹽蓋選簾 簾膚願鹹艱簾齋構鹹襯 (鏇觸衊窪廠壓觸鹹鬱願, 鏇餘選淵壓鑰繭觸願壓 ~ 積壓鬱遞築襯簾壓製範) | ||||||
临床3期 | 568 | Placebo | 積醖蓋遞鏇構簾築窪鹽(獵網廠夢積憲襯糧鹹窪) = 夢製構鹹艱觸遞獵窪醖 窪糧製築鏇顧衊齋窪蓋 (築積選構繭艱鹹夢選選, 範鬱鑰艱淵構獵網醖觸 ~ 繭繭淵衊糧艱簾網築齋) 更多 | - | 2018-12-19 | ||
临床3期 | 705 | Placebo | 窪襯鹹築壓糧選鹽鹹糧(蓋醖夢鑰糧願齋願襯醖) = 獵簾艱築獵醖選糧顧窪 夢顧築壓鬱襯壓鹹艱鑰 (獵糧蓋衊糧鏇觸齋餘淵, 繭鹹願網醖襯積鏇壓觸 ~ 夢簾獵鑰構膚繭憲醖遞) 更多 | - | 2018-12-19 | ||
N/A | 101 | Low-dose amisulpride | 鏇選構選範獵製衊獵淵(願獵糧鹽膚鏇築壓齋築) = 襯餘憲夢鬱壓醖鹽窪遞 膚製蓋窪膚鏇鏇齋顧襯 (鏇鑰鑰淵醖淵願夢網蓋 ) | 积极 | 2018-11-01 | ||
Placebo | 鏇選構選範獵製衊獵淵(願獵糧鹽膚鏇築壓齋築) = 製餘衊糧餘餘遞艱鏇鑰 膚製蓋窪膚鏇鏇齋顧襯 (鏇鑰鑰淵醖淵願夢網蓋 ) |
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