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更新于：2025-10-19
Esaxerenone
艾沙利酮
更新于：2025-10-19
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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166
项与 艾沙利酮 相关的文献（医药）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.
2025-09-30International Heart Journal
Esaxerenone Attenuates Atherogenesis and Vascular Dysfunction in Apolipoprotein E-Deficient Mice
Article
作者: Fukuda, Daiju ; Sata, Masataka ; Munkhjargal, Uugantsetseg ; Bavuu, Oyunbileg ; Hara, Tomoya ; Maeda, Juri
The pharmacological blockade of mineralocorticoid receptors (MR) is a potential therapeutic approach to reduce cardiovascular complications. Recent studies suggest that MR blockers affect several extrarenal tissues, including vascular function. We investigated the effects of a novel non-steroidal selective MR blocker, esaxerenone, on vascular function and atherogenesis.Esaxerenone (3 mg/kg/day) was orally administered for 20 weeks or vehicle for 8 weeks to apolipoprotein E-deficient (ApoE-/-) mice fed a Western-type diet to investigate the effects on atherogenesis or vascular dysfunction. Human umbilical vein endothelial cells (HUVEC) were used to perform in vitro experiments.Administration of esaxerenone for 20 weeks suppressed the development of atherosclerotic plaques in the aortic arch compared with the vehicle group (P < 0.001) without alteration of blood pressure. In addition, esaxerenone significantly reduced the expression of intercellular cell adhesion molecule-1, macrophage infiltration, and lipid deposition as determined by immunohistochemical analysis. Moreover, phosphorylation of eNOSSer1177 and Akt were increased in the aorta of esaxerenone-treated mice. Administration of esaxerenone for 8 weeks attenuated Western-type diet-induced endothelial dysfunction, accompanied by a decrease in expression of ICAM-1 and phosphorylation of JNK in the descending aorta. In an ex vivo vascular reactivity assay using ApoE-/- aortic rings, esaxerenone diminished aldosterone-induced endothelial dysfunction. In an in vitro experiment, aldosterone decreased the phosphorylation of eNOSSer1177 and increased the phosphorylation of eNOSThr495 in a dose-dependent manner, which were attenuated by esaxerenone in HUVECs.Esaxerenone ameliorated hyperlipidemia-induced atherosclerotic plaque progression and vascular dysfunction in ApoE-/- mice, suggesting that esaxerenone is a promising therapeutic approach for cardiovascular complications.
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
siRNA临床结果信使RNA
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
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 |
|---|---|---|---|
| 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 | 鬱製鏇餘糧艱憲構艱壓(鹽鏇範鏇顧願顧壓觸壓) = 鏇選顧顧衊艱壓蓋蓋鑰 齋廠鹹壓選廠齋憲蓋壓 (衊膚鹽獵齋醖襯鏇夢齋 ) 更多 | 积极 | 2022-08-17 | |||
临床3期 | 91 | 憲願鬱糧艱鏇壓鏇積製(淵鏇窪構膚艱獵憲糧製) = 遞製壓衊淵蓋糧鏇壓齋 艱衊築鏇觸簾鏇選繭鏇 (願簾醖淵醖遞獵製積齋 ) 更多 | 积极 | 2021-05-01 | |||
临床1期 | - | 55 | 壓獵鹹憲蓋顧衊襯製簾(壓築襯簾蓋鑰網醖膚鬱) = 襯網構遞積顧獵餘選遞 窪獵齋範鑰鏇網鹽製憲 (鑰鏇衊築壓襯鹹壓積鹽 ) | - | 2020-08-01 | ||
临床3期 | 51 | 繭顧夢夢淵選艱壓範醖(糧夢壓糧鏇選鏇遞糧膚) = 膚製顧艱衊製築餘積構 網顧膚鑰構網觸夢蓋夢 (築餘遞鏇選夢範觸蓋鑰 ) 更多 | 积极 | 2019-10-01 |
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