预约演示
更新于：2025-11-25
Esaxerenone
艾沙利酮
更新于：2025-11-25
概要
基本信息
原研机构 |
非在研机构- |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 日本 (2019-01-08), |
最高研发阶段(中国)- |
特殊审评- |
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结构/序列
分子式C22H21F3N2O4S |
InChIKeyNOSNHVJANRODGR-UHFFFAOYSA-N |
CAS号1632006-28-0 |
关联
40
项与 艾沙利酮 相关的临床试验CTRI/2025/02/080030
A Multicentric, Randomized, Prospective, Double Blind, Parallel Group, Comparative, Active Controlled, Phase III Clinical Study to Evaluate the Efficacy, Safety And Tolerability Of Esaxerenone 5mg Versus Eplerenone 50mg In Patients With Uncontrolled Or Resistant Hypertension. - NIL
CTRI/2024/12/077633
A Randomized, open label, balanced, two treatments, two period, two sequence, single dose, crossover, bioequivalence study of Test product (T) Esaxerenone Tablet 5 mg of Eris Lifesciences Limited India with Reference product (R) MINNEBRO (Esaxerenone) Tablets 5 mg of Daiichi Sankyo Company, Limited in normal, healthy, adult, human subjects under fasting condition. - NIL
JPRN-UMIN000037722
Safety and antihypertensive effect of switching from eplerenone to esaxerenone in hypertensive patients. - Safety and antihypertensive effect of switching from eplerenone to esaxerenone in hypertensive patients.
100 项与 艾沙利酮 相关的临床结果
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100 项与 艾沙利酮 相关的转化医学
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100 项与 艾沙利酮 相关的专利（医药）
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165
项与 艾沙利酮 相关的文献（医药）2026-01-01JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY
Esaxerenone attenuates high salt-induced hypertension and renal damage via CD8+T cell- associated NCC activation in aldosterone treated rats
Article
作者: Zhong, Yan ; Xu, Chang ; An, Jingwen ; Wang, Xiangting ; Liu, Fengrui ; Wang, Zheng ; Wang, Hongshuang ; Fang, Fang ; Zhai, Nan
Salt-water retention plays key roles in chronic kidney disease (CKD) and hypertension. The mineralocorticoid receptor (MR) blocker esaxerenone could attenuate hypertension and renal injury; however, the mechanism is only partially understood. In this study, we used rats that were fed 8 % high-salt diet or/and infused with aldosterone to explore the possible mechanism of salt-water retention in CKD and hypertension, and the protective effect of esaxerenone. The blood pressure and renal injury were observed. Moreover, salt- water retention, CD8+T cells infiltration and MR activation were detected. After treatment with high-salt diet plus aldosterone, the blood pressure level was significantly increased, and renal injury was more obvious than with the high-salt diet or aldosterone alone. The expression levels of the sodium transporter, as well as the mineralocorticoid receptor (NR3C2), were significantly upregulated in the ALD+HS group. Furthermore, the infiltration of CD3+ and CD8+ T cells were increased in the ALD+HS group. Besides, our results proved that esaxerenone could alleviate high-salt diet plus aldosterone-induced salt-water retention and renal injury. In conclusion, aldosterone plus high salt diet enhances renal infiltration of CD8+T cells and upregulates NCC expression and phosphorylation, resulting in hypertension and kidney injury. Esaxerenone antagonizes the activation of mineralocorticoid receptors to decrease the infiltration of CD8+T cells and the phosphorylation level of NCC, thereby alleviating salt-water retention and kidney injury.
2025-12-01INFLAMMATION RESEARCH
Aldosterone induces renal lymphangiogenesis through macrophage-lymphatic endothelial cell transformation and Inhibition by esaxerenone
Article
作者: Qiang, Panpan ; Xu, Qingyou ; Lv, Ruyan ; Yang, Fan ; Liu, Ziqian ; Chang, Yi ; Shimosawa, Tatsuo ; Xiong, Yunzhao ; Zhang, Boya ; Wang, Xuan ; Guo, Haixia
OBJECTIVE AND DESIGN:
Inflammation plays a crucial role in the occurrence and development of renal fibrosis. Lymphatic vessels have emerged as new hotspots in the domain of inflammation. Recent studies have revealed that macrophages are involved in lymphangiogenesis through direct and indirect mechanisms. However, the underlying mechanisms of macrophage transdifferentiation into lymphatic endothelial cells (LECs) are still poorly understood.
METHODS:
In vivo, thirty male Wistar rats were randomly divided into a sham group, an aldosterone group and an aldosterone + esaxerenone group. In vitro, Raw 264.7 cells and bone marrow-derived macrophages (BMDMs) were used. H&E, Masson, western blotting, immunohistochemistry, immunofluorescence, flow cytometry, and BMDM tube formation assays were used to assess renal fibrosis and lymphangiogenesis in a rat model of aldosterone-induced renal injury.
RESULTS:
In this study, we observed pathological renal fibrosis and lymphangiogenesis in 12-week-old rats after aldosterone infusion. In addition, the treatment of rats with esaxerenone, a mineralocorticoid receptor blocker (MRB), significantly reduced renal lymphangiogenesis and fibrosis. Interestingly, we found that aldosterone can activate MR to stimulate macrophages to secrete vascular endothelial growth factor C (VEGF-C) and promote lymphatic angiogenesis.
CONCLUSIONS:
Our data suggest that renal fibrosis occurs in aldosterone-treated rats and that inflammation-induced macrophage transdifferentiation into LECs occurs during this process and that MRB attenuates renal fibrosis and lymphangiogenesis due to inflammatory injury.
2025-12-01LIFE SCIENCES
Esaxerenone inhibits renal macrophage proliferation through MR/TGF-β1 pathway in db/db mice
Article
作者: Qiang, Panpan ; Zhao, Yicong ; Lv, Ruyan ; Shimosawa, Tatsuo ; Xu, Qingyou ; Yang, Fengwen ; Liu, Ziqian ; Yang, Fan ; Tan, Jinchuan ; Li, Yuan
AIMS:
To investigate the effect of mineralocorticoid receptor (MR) blockade esaxerenone on renal macrophage proliferation in db/db mice and its potential role in the progression of diabetic kidney disease (DKD).
MATERIALS AND METHODS:
Eight-week-old db/db mice were administered esaxerenone at a dose of 1 mg/kg/day for six weeks. The origin of macrophages (resident versus recruited) and their phenotypic subtypes (M1 vs. M2) were evaluated using molecular markers, including F4/80, Ki-67, Ly6C, iNOS, and CD206. Immunohistochemistry, flow cytometry, and single-cell RNA sequencing were utilized to evaluate these parameters. The inhibitory effects of esaxerenone and the TGF-β1 inhibitor LY2109761 on the proliferation of bone marrow-derived macrophages (BMDMs) under high-glucose conditions were examined in vitro.
KEY FINDINGS:
Marked increases in macrophage infiltration and proliferation were observed in the kidneys of db/db mice. Both recruited and resident macrophages exhibited significant proliferative activity, with recruited macrophages predominantly adopting an M1 phenotype and resident macrophages primarily exhibiting an M2 phenotype. Proliferating macrophages displayed enhanced pro-inflammatory and pro-fibrotic responses compared to non-proliferating counterparts. In vivo, esaxerenone treatment significantly suppressed macrophage proliferation. In vitro studies demonstrated that high glucose activated MR, upregulated TGF-β1 expression, and subsequently promoted BMDMs proliferation, particularly within the M1 subtype. TGF-β1 alone also induced BMDMs proliferation, an effect attenuated by LY2109761.
SIGNIFICANCE:
Esaxerenone inhibits renal macrophage proliferation mediated by high glucose-induced activation of MR and downstream TGF-β1 signaling pathways, thereby mitigating inflammatory and fibrotic damage. These findings suggest that MR blockade may directly target macrophage proliferation and inflammation in DKD.
55
项与 艾沙利酮 相关的新闻（医药）2025-04-17
ASCO会议临床结果
2025-01-06
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2024-12-09
100 项与 艾沙利酮 相关的药物交易
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 高血压 | 日本 | 2019-01-08 |
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 |
|---|---|---|---|---|
| 白蛋白尿 | 临床3期 | 日本 | 2016-06-01 | |
| 2型糖尿病 | 临床3期 | 日本 | 2016-06-01 | |
| 肾性高血压 | 临床3期 | 日本 | 2016-06-01 | |
| 原发性高血压 | 临床3期 | 日本 | 2016-03-01 | |
| 糖尿病肾病 | 临床2期 | 日本 | 2015-01-01 | |
| 醛固酮增多症 | 临床阶段不明 | 日本 | 2016-09-01 |
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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3期 | 25 | 簾鬱鬱繭構範觸遞遞淵(醖顧範遞淵糧築鏇製構) = 繭齋淵襯遞憲膚憲遞醖 顧廠獵膚鹹積觸窪窪鹽 (鹹觸鬱糧構衊餘鬱築襯 ) 更多 | 积极 | 2022-08-17 | |||
临床3期 | 91 | 壓窪壓膚壓遞窪構膚鬱(蓋築鹹鏇鹹醖鬱繭鹹鹹) = 觸襯獵糧選鹹蓋網願鹹 範選繭選網製夢鑰醖廠 (顧範簾觸築網壓築壓鹽 ) 更多 | 积极 | 2021-05-01 | |||
临床1期 | - | 55 | 繭糧壓顧憲積淵遞鬱鏇(鹽壓襯窪範蓋淵願餘構) = 憲願糧齋願窪夢顧製製 構艱廠壓範構壓願鹽製 (膚觸壓網鏇積膚憲積鏇 ) | - | 2020-08-01 | ||
临床3期 | 51 | 鹹鹽鹽淵壓憲範繭構壓(鏇鹹簾醖憲顧窪積範遞) = 鹽築艱範觸鏇廠構築鑰 製繭淵網夢襯範夢窪鹽 (餘齋鹹範鹹齋選顧夢醖 ) 更多 | 积极 | 2019-10-01 |
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