预约演示
更新于：2026-02-27
Abexinostat
甲苯磺酸艾贝司他
更新于：2026-02-27
概要
基本信息
原研机构 |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)临床3期 |
特殊审评快速通道 (美国)、优先审评 (中国) |
登录后查看时间轴
结构/序列
分子式C21H23N3O5 |
InChIKeyMAUCONCHVWBMHK-UHFFFAOYSA-N |
CAS号783355-60-2 |
关联
30
项与 甲苯磺酸艾贝司他 相关的临床试验CTR20233511
甲苯磺酸艾贝司他片变更前后的两制剂在中国健康受试者中的单中心、随机、开放、两制剂、空腹、单次给药、两周期、两序列、交叉设计的生物等效性研究
NCT05698524
A Phase I Study of Metronomic Temozolomide With Abexinostat (PCI-24781) for Patients With Recurrent High Grade Glioma
NCT04498520
Phase I Trial of Abexinostat Combined With Palbociclib and Fulvestrant in Patients With Antiestrogen Refractory ER+, HER2- Breast Cancer and Gynecological Metastatic Tumors
100 项与 甲苯磺酸艾贝司他 相关的临床结果
登录后查看更多信息
100 项与 甲苯磺酸艾贝司他 相关的转化医学
登录后查看更多信息
100 项与 甲苯磺酸艾贝司他 相关的专利（医药）
登录后查看更多信息
111
项与 甲苯磺酸艾贝司他 相关的文献（医药）2025-12-01Alzheimers & Dementia
Exploring the Potential of Abexinostat as a Therapeutic Agent for Amyloid‐Beta Pathology in Alzheimer’s Disease: A Multimodal Approach
Article
作者: Das, Anik Kumar ; Sharma, Lalit
Abstract:
Background:
Alzheimer’s disease (AD) is a progressive neurodegenerative disorder characterized by cognitive decline and neuronal damage, with amyloid‐beta (Aβ) aggregation being a hallmark of AD pathology. Histone deacetylase (HDAC) inhibitors, including Abexinostat, have shown potential in modulating neurodegenerative processes by influencing protein aggregation and oxidative stress. This study aimed to evaluate the therapeutic potential of Abexinostat in AD through computational, in vitro, and in vivo methodologies.
Method:
Computational docking studies assessed the binding interactions between Abexinostat and Aβ to explore its potential to inhibit Aβ aggregation. In vitro experiments evaluated the effects of Abexinostat on Aβ42 fibril formation, protease digestion, and oxidative stress modulation. Western blotting measured the expression of key proteins involved in Aβ metabolism, including Aβ precursor protein (APP) and beta‐secretase (BACE1). RT‐PCR analysis examined the expression of antioxidant genes, such as superoxide dismutase (SOD) and catalase. Cognitive function and memory were evaluated in an Aβ42 intracerebroventricular (ICV) mouse model using the Morris water maze and Y‐maze. Histopathological analysis assessed amyloid plaque burden and neuronal damage in brain sections.
Results:
Computational docking studies revealed strong binding between Abexinostat and Aβ, indicating its potential to inhibit Aβ aggregation. In vitro, Abexinostat reduced Aβ42 fibril formation by 45% at 10 µM and 72% at 20 µM (p < 0.05, p < 0.01) and promoted protease digestion by 33% at 10 µM and 58% at 20 µM (p < 0.01). Western blotting showed a 34% reduction in APP and a 42% reduction in BACE1 expression (p < 0.05, p < 0.01). RT‐PCR analysis demonstrated a 52% increase in SOD and a 39% increase in catalase expression (p < 0.01, p < 0.05). Behavioral tests showed a 40% reduction in escape latency and a 35% increase in platform crossings in the Morris water maze (p < 0.05, p < 0.01). Histopathological analysis revealed a 50% reduction in amyloid plaque burden and 41% less neuronal damage (p < 0.01, p < 0.05).
Conclusion:
Abexinostat demonstrates potential as a dual‐target therapeutic for AD, inhibiting Aβ aggregation and improving cognitive function by modulating oxidative stress and Aβ metabolism. Further investigation is needed to explore its clinical applications.
2024-12-05LEUKEMIA & LYMPHOMA
A phase 1 trial of abexinostat with ibrutinib in relapsed/refractory mantle cell lymphoma and non-germinal center diffuse large B cell lymphoma
Article
作者: Zhu, Menglei ; Zelenetz, Andrew D. ; Bantilan, Kurt S. ; Kumar, Anita ; Matasar, Matthew ; Joseph, Ashlee ; Salles, Gilles ; von Keudell, Gottfried ; Gurumurthi, Ashwath ; Biggar, Erin ; Castro, Ali ; Hamlin, Paul A.
In this phase 1 study, we hypothesized that the combination of the HDAC inhibitor, abexinostat, with ibrutinib would be safe and efficacious in relapsed and refractory MCL and non-germinal center (non-GCB) dLBCL.The main limitation of this study is the premature closure of the trial resulting in small patient numbers without the planned dose expansion cohort with targeted accrual of 34 patients.Furthermore, three MCL responders were unable to complete the full duration of therapy.The trial was terminated in late 2021 due to the evolving therapeutic landscape for relapsed MCL, such as a shift from ibrutinib to the use of 2nd generation BTK inhibitors and the approval of Brexucabtagene autoleucel CAR-T therapy in third-line therapy for MCL.
2024-12-01INTERNATIONAL IMMUNOPHARMACOLOGY
Identification of mitochondria-related genes as diagnostic biomarkers for diabetic nephropathy and their correlation with immune infiltration: New insights from bioinformatics analysis
Article
作者: Lin, Haibiao ; Zhang, Qiaoxuan ; Huang, Fei ; Han, Liqiao ; Zhan, Min ; Yan, Qiaofang ; Yan, Jun ; Du, Yuanyuan ; Wu, Junbiao ; Huang, Xianzhang ; Zhang, Pengwei
BACKGROUND:
Diabetic nephropathy (DN) is a common and severe microvascular complication of diabetes. Mitochondrial dysfunction and immune inflammation are important factors in the pathogenesis of DN. However, the specific mechanisms and their intricate interactions in DN remain unclear. Besides, there are no effective specific predictive or diagnostic biomarkers for DN so far. Therefore, this study aims to elucidate the role of mitochondrial-related genes and their possibility as predictive or diagnostic biomarkers, as well as their crosstalk with immune infiltration in the progression of DN.
METHODS:
Based on the GEO database and limma R package, the differentially expressed genes (DEGs) of DN were identified. Mitochondrial-related DEGs (MitoDEGs) were then obtained by intersecting these DEGs with mitochondria-related genes from the MitoCarta 3.0 database. Subsequently, the candidate hub genes were further screened by gene co-expression network analysis (WGCNA), and verified mRNA levels of these genes by real-time quantitative PCR (qRT-PCR) in high-glucose-treated human proximal tubular (HK-2) cells. The verified hub genes were utilized to construct a combined diagnostic model for DN, with its diagnostic efficacy assessed across the GSE30122 and GSE96804 datasets. Additionally, the immune infiltration pattern in DN was assessed with the CIBERSORT algorithm, and the Nephroseq v5 database was used to analyze the correlation between hub genes and clinical features of DN.
RESULTS:
Seven mitochondria-related candidate hub genes were screened from 56 MitoDEGs. Subsequently, the expression levels of six of them, namely EFHD1, CASP3, AASS, MPC1, NT5DC2, and BCL2A1, exhibited significant inter-group differences in the HK-2 cell model. The diagnostic model based on the six genes demonstrated good diagnostic efficacy in both training and validation sets. Furthermore, correlation analysis indicated that EFHD1 and AASS, downregulated in DN, are positively correlated with eGFR and negatively with serum creatinine. Conversely, CASP3, NT5DC2, and BCL2A1, upregulated in DN, show opposite correlations. In addition, spearman analysis revealed that the six hub genes were significantly associated with the infiltration of immune cells, including M1 and M2 macrophages, mast cells, resting NK cells, gamma delta T cells, and follicular helper T cells.
CONCLUSION:
This study elucidated the characteristics of mitochondria-related genes and their correlation with immune cell infiltration in DN, providing new insights for exploring the pathogenesis of DN and facilitating the identification of new potential biomarkers and therapeutic targets.
100 项与 甲苯磺酸艾贝司他 相关的药物交易
登录后查看更多信息
研发状态
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 局部晚期肾细胞癌 | 临床3期 | 美国 | - | 2018-10-12 |
| 局部晚期肾细胞癌 | 临床3期 | 中国 | - | 2018-10-12 |
| 局部晚期肾细胞癌 | 临床3期 | 捷克 | - | 2018-10-12 |
| 局部晚期肾细胞癌 | 临床3期 | 法国 | - | 2018-10-12 |
| 局部晚期肾细胞癌 | 临床3期 | 意大利 | - | 2018-10-12 |
| 局部晚期肾细胞癌 | 临床3期 | 波兰 | - | 2018-10-12 |
| 局部晚期肾细胞癌 | 临床3期 | 韩国 | - | 2018-10-12 |
| 局部晚期肾细胞癌 | 临床3期 | 西班牙 | - | 2018-10-12 |
| 局部晚期肾细胞癌 | 临床3期 | 英国 | - | 2018-10-12 |
| 转移性肾细胞癌 | 临床3期 | 美国 | - | 2018-10-12 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床1期 | 12 | 蓋顧繭憲鑰餘願餘餘夢(簾襯網築鹽齋觸觸廠鬱) = 鏇衊製繭遞構蓋蓋襯鹹 鑰淵範獵壓齋衊齋願願 (衊遞鏇廠獵築艱選鹽網, 7.33 ~ NE) 更多 | 积极 | 2025-05-30 | |||
蓋顧繭憲鑰餘願餘餘夢(簾襯網築鹽齋觸觸廠鬱) = 積選壓築憲艱壓顧艱憲 鑰淵範獵壓齋衊齋願願 (衊遞鏇廠獵築艱選鹽網, 7.33 ~ NE) 更多 | |||||||
临床1期 | - | 醖鬱鏇願憲齋願憲壓夢(憲衊獵鹽鑰夢願醖齋艱) = 艾贝司他联合伊布替尼有效率（CR和ORR）及无进展生存期（PFS）均优于单独使用伊布替尼 醖壓顧鏇鏇壓蓋構憲窪 (觸鹽網構蓋窪齋願積顧 ) | 积极 | 2024-06-28 | |||
临床2期 | 滤泡性淋巴瘤 三线 | 90 | 艱網鹹鏇顧願積網醖憲(鹹鹽鹹醖齋餘窪蓋壓鑰) = 襯積壓齋築鹹鬱選醖窪 遞積淵鏇鹹積夢網網膚 (淵積衊壓憲觸顧繭繭蓋, 55.8 ~ 77.1) 更多 | 积极 | 2024-05-24 | ||
(pts with > 3 lines of prior therapy) | 艱網鹹鏇顧願積網醖憲(鹹鹽鹹醖齋餘窪蓋壓鑰) = 願鏇繭廠簾襯繭鏇淵窪 遞積淵鏇鹹積夢網網膚 (淵積衊壓憲觸顧繭繭蓋, 49.2 ~ 84.7) | ||||||
临床1期 | 43 | (HDAC2高表达) | 鑰壓範襯鏇願簾鹽選鑰(簾製膚齋鬱蓋簾獵構廠) = 蓋顧鑰鹹簾窪醖膚窪積 壓醖衊淵觸艱鹽鬱繭製 (襯顧壓艱齋鏇衊齋繭淵 ) 更多 | 积极 | 2022-06-09 | ||
(HDAC2低表达) | 鑰壓範襯鏇願簾鹽選鑰(簾製膚齋鬱蓋簾獵構廠) = 選淵餘艱壓鏇蓋繭糧觸 壓醖衊淵觸艱鹽鬱繭製 (襯顧壓艱齋鏇衊齋繭淵 ) 更多 | ||||||
临床2期 | 41 | 鹹夢憲廠製餘繭積繭膚(窪鹹壓夢簾淵鹽鏇艱蓋) = 醖範構選醖鹹顧製願襯 餘獵憲獵膚選顧憲鏇齋 (糧鏇鏇選築獵膚鹽獵醖 ) 更多 | 积极 | 2022-06-02 | |||
临床1期 | 51 | (dose escalation) | 築糧範夢獵簾憲艱淵繭(憲顧願積築糧齋夢繭鹹) = 蓋製窪衊夢鑰範製構觸 築齋窪構艱獵範觸艱襯 (憲遞繭鹽餘淵餘構齋窪 ) | 积极 | 2022-06-02 | ||
(RCC + dose expansion) | 築糧範夢獵簾憲艱淵繭(憲顧願積築糧齋夢繭鹹) = 蓋願鑰膚齋築蓋蓋鏇襯 築齋窪構艱獵範觸艱襯 (憲遞繭鹽餘淵餘構齋窪 ) | ||||||
临床1期 | 51 | 襯艱顧範艱製鬱淵齋觸(糧夢淵繭鹹壓鹽築獵獵) = 壓醖網顧鑰範蓋鏇醖鹽 齋選淵齋鑰醖觸製鬱襯 (鏇繭醖積艱願獵積獵壓 ) 更多 | 积极 | 2019-05-26 | |||
(RCC) | - | ||||||
临床1期 | 52 | 繭鏇衊膚憲鏇蓋鹽餘窪(選膚積夢憲憲鹹獵淵窪) = 10% 淵築範獵窪築鏇鬱顧鑰 (鹹膚鏇範鬱製觸築範範 ) 更多 | 积极 | 2016-07-15 | |||
临床1期 | 52 | 願繭憲齋積鑰衊衊衊膚(蓋醖齋艱簾膚願膚窪築) = The most common grade ≥ 3 related adverse events observed were diarrhea (10%) 顧齋範艱選憲糧顧艱積 (衊鏇簾齋衊淵鬱鑰選廠 ) 更多 | 积极 | 2016-05-20 | |||
临床1期 | 20 | (participants received abexinostat 15 mg/m(2) or 30 mg/m(2) twice daily.) | 鏇窪鑰衊選窪簾顧網簾(膚願糧構艱齋鑰構夢鹹) = DLTs of grade 3 and 4 neutropenia were observed in 2 of 3 participants who received abexinostat 30 mg/m(2) twice daily.Two DLTs were observed at the 60 mg/m(2) twice-daily dose (grade 3 infection, grade 4 thrombocytopenia). 獵顧窪憲餘獵餘壓憲鹽 (衊積構範糧淵鏇製艱蓋 ) | 积极 | 2015-04-15 | ||
(participants received abexinostat at doses of 30 mg/m(2), 45 mg/m(2), or 60 mg/m(2) twice daily, all with mandated G-CSF support.) |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
生物医药百科问答
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用