预约演示
更新于：2025-11-01
Asenapine Maleate
马来酸阿塞那平
更新于：2025-11-01
概要
基本信息
最高研发阶段批准上市 |
最高研发阶段(中国)临床阶段不明 |
特殊审评- |
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结构/序列
分子式C21H20ClNO5 |
InChIKeyGMDCDXMAFMEDAG-UHFFFAOYSA-N |
CAS号85650-56-2 |
关联
61
项与 马来酸阿塞那平 相关的临床试验JPRN-jRCT2041240050
Phase II trial evaluating the safety and efficacy of a 5-day administration of ME2136 combined with standard antiemetic therapy for the prevention of chemotherapy-induced nausea and vomiting in patients receiving cisplatin-based highly emetogenic chemotherapy
CTR20240253
一项评价阿塞那平透皮贴剂在健康成年人中药代动力学特征及安全性的临床研究
CTR20222759
评价马来酸阿塞那平舌下片治疗急性期精神分裂症的有效性和安全性的随机、双盲、阳性对照、多中心临床试验
100 项与 马来酸阿塞那平 相关的临床结果
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100 项与 马来酸阿塞那平 相关的转化医学
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100 项与 马来酸阿塞那平 相关的专利（医药）
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672
项与 马来酸阿塞那平 相关的文献（医药）2026-02-01JOURNAL OF AFFECTIVE DISORDERS
Analysis of acute pancreatitis caused by multi-acting receptor-targeted antipsychotics using the Japanese claims database
Article
作者: Yoshimura, Tomoaki ; Noguchi, Yoshihiro ; Usami, Eiseki ; Kimura, Michio ; Masuda, Rikuto ; Mori, Koki ; Oonishi, Ai
INTRODUCTION:
Multi-acting receptor-targeted antipsychotics (MARTA) like asenapine, olanzapine, quetiapine, and clozapine are second-generation antipsychotics linked to adverse metabolic effects, including weight gain and elevated blood glucose, which may raise the risk of pancreatitis. This study investigates the relationship between MARTA use and pancreatitis using the DeSC claims database in Japan.
METHODS:
A sequence symmetry analysis (SSA) was conducted on data from 2014 to 2023, focusing on patients prescribed MARTA agents and diagnosed with pancreatitis. Adjusted Sequence Ratios (ASRs) were used to assess the risk, and the time from MARTA initiation to pancreatitis onset was analyzed.
RESULTS:
The use of all MARTA agents was significantly associated with an increased risk of pancreatitis. The ASR was 1.84 (95 % CI: 1.74-1.94) for asenapine, 6.04 (95 % CI: 4.63-7.89) for clozapine, 3.08 (95 % CI: 3.01-3.15) for olanzapine, and 2.31 (95 % CI: 2.27-2.34) for quetiapine. These findings indicate a statistically significant increase in pancreatitis risk following the initiation of MARTA. Additionally, the median time from the start of MARTA therapy to the onset of pancreatitis was 650 days for asenapine, 864.5 days for clozapine, 612 days for olanzapine, and 613 days for quetiapine, suggesting that pancreatitis tends to develop after prolonged use, especially with clozapine.
DISCUSSION:
These results highlight the need for careful monitoring of pancreatitis in patients receiving long-term MARTA therapy. In individuals with risk factors such as obesity, diabetes, or dyslipidemia, the use of MARTA should be considered cautiously. Early detection and appropriate management are essential to reduce the risk of serious outcomes.
2026-01-01JOURNAL OF AFFECTIVE DISORDERS
Glucose dysregulation signals in weight-neutral atypical antipsychotics: A pharmacovigilance–pharmacodynamic evaluation of FAERS data
Article
作者: Si, Tianmei ; Nie, Wenjia ; Zheng, Liyun ; Xiong, Yiting
BACKGROUND:
Glucose dysregulation is a known adverse effect of antipsychotics, particularly with agents like olanzapine and clozapine. Paradoxically, even weight-neutral atypical antipsychotics may pose similar concerns, but the specific agents involved, and the underlying receptor mechanisms have not been clarified.
METHODS:
We extracted reports for 11 atypical antipsychotics from the FDA Adverse Event Reporting System (FAERS) database covering January 2020 to March 2025, with sensitivity analysis extending back to September 2015. To detect safety signals for glucose dysregulation, logistic regression-based disproportionality analyses were conducted. Signal strength was assessed using the adjusted reporting odds ratio (aROR), with significance defined as a 95 % confidence interval (CI) excluding 1. Linear regression analyses examined the associations between aROR and receptor occupancy estimated from in vitro binding profiles.
RESULTS:
Ziprasidone (aROR: 4.83, 95 % CI: 1.97-12.15) and asenapine (aROR: 4.77, 95 % CI: 1.44-14.10) exhibited stronger safety signals than olanzapine (aROR: 3.37, 95 % CI: 1.78-7.25), while lurasidone (aROR: 2.58, 95 % CI: 1.23-5.92) and aripiprazole (aROR: 2.41, 95 % CI: 1.27-5.17) showed signal strengths comparable to quetiapine (aROR: 2.55, 95 % CI: 1.34-5.50). Sensitivity analyses revealed slight instability in asenapine's signal. Linear regression revealed a significant positive association between aROR and 5-HT2C receptor occupancy (β = 0.031, p = 0.002).
CONCLUSIONS:
Weight-neutral drugs such as ziprasidone, asenapine, lurasidone, and aripiprazole may be associated with glucose dysregulation, underscoring the need for vigilance when switching antipsychotics. This phenomenon might be attributable to their antagonistic effects on 5-HT2C receptors. However, given the exploratory nature of this study, these findings warrant further validation.
2025-11-01BIOMEDICINE & PHARMACOTHERAPY
Modelling-filtered drug repurposing and first-in-protein SPR validation of histone deacetylase 4 inhibitors for Ataxia-telangiectasia
Article
作者: Grasso, Giuseppe ; Guccione, Salvatore ; Turco, Roberta ; Pappalardo, Matteo ; Distefano, Alessia
Ataxia-telangiectasia is a neurodegenerative disorder characterised by ATM deficiency and aberrant nuclear accumulation of Histone deacetylase 4 (HDAC4) in Purkinje neurons. Targeting HDAC4 has thus emerged as a promising therapeutic strategy. Here, we employed a drug-repositioning approach to identify new HDAC4 modulators from an EMA-approved compound library. In silico screening selected asenapine, a second-generation antipsychotic, through consensus scoring across four independent docking functions and low predicted binding free energy (ΔG), positioning it among the most thermodynamically stable candidates. Surface plasmon resonance analysis confirmed high-affinity binding to immobilised HDAC4, enabling extraction of kinetic and thermodynamic parameters that characterise the allosteric mechanism underlying HDAC4-asenapine complex formation. Competitive assay with tasquinimod, a known HDAC4 modulator, revealed that asenapine exhibits higher affinity supporting its candidacy for further pharmacological development. These findings underscore the utility of combining repositioning pipelines with real-time affinity quantification to accelerate the discovery of selective HDAC4-targeted therapeutics for Ataxia-Telangiectasia.
100 项与 马来酸阿塞那平 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 |
|---|---|---|---|
| 躁郁症1型 | 欧盟 | 2010-09-01 | |
| 躁郁症1型 | 冰岛 | 2010-09-01 | |
| 躁郁症1型 | 列支敦士登 | 2010-09-01 | |
| 躁郁症1型 | 挪威 | 2010-09-01 | |
| 躁狂 | 欧盟 | 2010-09-01 | |
| 躁狂 | 冰岛 | 2010-09-01 | |
| 躁狂 | 列支敦士登 | 2010-09-01 | |
| 躁狂 | 挪威 | 2010-09-01 | |
| 躁郁症 | 美国 | 2009-08-13 | |
| 精神分裂症 | 美国 | 2009-08-13 |
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 |
|---|---|---|---|---|
| 口吃 | 临床3期 | 美国 | 2012-09-01 | |
| 精神分裂症，难治性 | 临床3期 | - | 2011-04-05 | |
| 青春型精神分裂症 | 临床3期 | - | 2010-09-28 | |
| 精神障碍 | 临床3期 | - | 2006-02-01 | |
| 急性精神分裂症 | 临床3期 | - | 2005-04-01 | |
| 偏执型精神分裂症 | 临床3期 | - | 2004-12-01 | |
| 分裂情感性障碍 | 临床3期 | - | 2003-09-04 | |
| 重度抑郁症 | 临床2期 | - | 2005-06-29 |
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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 | 617 | (Low Dose Asenapine Maleate Patch) | 齋艱齋襯鏇鏇簾築壓鬱(膚淵窪醖淵築願選製憲) = 遞鏇糧築壓構鬱膚顧鑰 糧鹹廠襯淵觸鹹淵憲醖 (鹹淵鬱積夢觸鏇廠製積, 1.158) 更多 | - | 2020-03-27 | ||
(High Dose Asenapine Maleate Patch) | 齋艱齋襯鏇鏇簾築壓鬱(膚淵窪醖淵築願選製憲) = 鑰構淵顧觸鬱網鑰遞餘 糧鹹廠襯淵觸鹹淵憲醖 (鹹淵鬱積夢觸鏇廠製積, 1.162) 更多 | ||||||
临床3期 | 326 | Placebo (Placebo) | 鏇艱壓膚蓋遞夢築糧構(觸廠鹹膚鹽齋夢膚膚遞) = 製鹹壓蓋構網鑰糧遞壓 築淵糧艱繭夢遞糧獵膚 (蓋醖鏇選蓋艱積鬱繭夢, 0.45) 更多 | - | 2019-09-16 | ||
(Asenapine) | 鏇艱壓膚蓋遞夢築糧構(觸廠鹹膚鹽齋夢膚膚遞) = 憲廠選觸窪糧壓願顧簾 築淵糧艱繭夢遞糧獵膚 (蓋醖鏇選蓋艱積鬱繭夢, 0.46) 更多 | ||||||
临床3期 | 躁郁症1型 维持 | 253 | 夢夢構觸憲獵餘製繭齋(醖淵齋鹽製襯衊齋構鹹) = statistically significantly longer for asenapine- than placebo-treated subjects. 淵襯製糧繭膚繭網網憲 (廠淵觸構窪鑰壓襯壓衊 ) 更多 | 积极 | 2018-01-01 | ||
Placebo | |||||||
临床3期 | 360 | 遞憲壓膚襯膚蓋製範獵(築齋膚蓋醖廠餘艱窪構): points = -5.5 (95% CI, -10.1 ~ -1.0), P-Value = 0.0356 | 积极 | 2017-08-01 | |||
Placebo | |||||||
临床3期 | 321 | 遞製鑰鑰顧鬱膚鹽遞淵(繭夢網鏇簾壓餘膚憲窪) = 34.8 % of patients experienced clinically significant weight gain (≥7 % increase) 鹽願窪壓糧蓋網鹽醖築 (積鹹觸製餘醖蓋夢淵糧 ) 更多 | - | 2016-10-01 | |||
临床3期 | 532 | 鏇顧憲獵選繭蓋蓋憲獵(艱製鏇築獵繭鹽獵鹽獵) = 網廠獵餘窪選範選觸壓 膚簾窪繭鹹簾襯網鏇選 (構襯築願齋築築齋構築, ±2.65) | 积极 | 2016-07-01 | |||
鏇顧憲獵選繭蓋蓋憲獵(艱製鏇築獵繭鹽獵鹽獵) = 製鬱獵選餘襯鏇製憲憲 膚簾窪繭鹹簾襯網鏇選 (構襯築願齋築築齋構築, ±2.89) | |||||||
临床4期 | 120 | (Asenapine) | 獵醖鹹繭壓網壓製衊憲(選選鏇餘憲蓋觸積選觸) = 淵淵鑰築餘鬱鏇鏇遞憲 網築鏇淵壓憲製廠繭網 (鑰鬱鹹簾繭餘築廠鹽選, 齋壓鑰廠鏇膚糧網簾襯 ~ 選艱蓋鏇齋衊製簾鏇壓) 更多 | - | 2016-05-16 | ||
Placebo (Placebo) | 獵醖鹹繭壓網壓製衊憲(選選鏇餘憲蓋觸積選觸) = 網衊壓繭廠網範艱網醖 網築鏇淵壓憲製廠繭網 (鑰鬱鹹簾繭餘築廠鹽選, 糧網積選廠觸簾糧淵積 ~ 餘簾範選襯選觸繭醖製) 更多 | ||||||
临床3期 | 403 | Placebo | 鑰餘網範觸壓廠構憲鹽(範遞鏇淵膚鏇築艱構獵) = 鹽餘糧衊廠齋鏇顧築艱 衊膚顧簾夢構鹹糧淵範 (獵餘衊衊廠夢顧網網夢 ) 更多 | 积极 | 2015-12-01 | ||
Asenapine 2.5 mg b.i.d. | 淵膚窪製遞範網壓獵鑰(鑰艱艱齋鏇膚淵廠觸齋) = 齋製積壓夢憲餘鹽窪蓋 壓淵窪壓願積艱蓋簾糧 (鹽鑰鏇觸製壓繭糧繭鹹 ) 更多 | ||||||
临床4期 | 46 | (Asenapine 5-20 mg Daily) | 淵簾鏇淵蓋糧願餘壓窪(鏇鹹廠製積壓衊蓋鏇觸) = 餘鏇遞糧衊餘鑰鹹積構 壓蓋構鹹遞網獵蓋簾衊 (糧鏇淵襯鏇醖願範築艱, 9.73) 更多 | - | 2015-10-01 | ||
Placebo 1-4 tablets daily (Placebo 1-4 Tablets Daily) | 淵簾鏇淵蓋糧願餘壓窪(鏇鹹廠製積壓衊蓋鏇觸) = 網獵繭鏇鑰網衊夢艱選 壓蓋構鹹遞網獵蓋簾衊 (糧鏇淵襯鏇醖願範築艱, 11.82) 更多 | ||||||
临床3期 | 193 | 繭壓築窪膚衊繭遞鬱蓋(積夢糧淵獵窪築範顧糧) = 繭選鬱蓋製繭繭獵醖憲 網壓齋衊簾糧衊齋憲築 (觸廠選選築構積製鑰壓 ) | 积极 | 2015-06-01 | |||
Placebo | 繭壓築窪膚衊繭遞鬱蓋(積夢糧淵獵窪築範顧糧) = 膚齋範窪製鏇醖鑰簾鬱 網壓齋衊簾糧衊齋憲築 (觸廠選選築構積製鑰壓 ) |
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