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更新于：2025-06-04
Esaxerenone
艾沙利酮
更新于：2025-06-04
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-UMIN000037721
Effects of adding esaxerenone to calcium channel blocker in patients with essential hypertension. - Effects of adding esaxerenone to calcium channel blocker in patients with essential hypertension.
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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177
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 ; Xiong, Yunzhao ; Zhang, Boya ; Shimosawa, Tatsuo ; 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.
2025-07-01JOURNAL OF HYPERTENSION
Chronic esaxerenone treatment improves vascular function and lowers peripheral arterial stiffness in patients with idiopathic hyperaldosteronism
Article
作者: Yamaji, Takayuki ; Higashi, Yukihito ; Kishimoto, Shinji ; Yusoff, Farina Mohamad ; Nakano, Yukiko ; Maruhashi, Tatsuya ; Goto, Chikara ; Harada, Takahiro ; Mizobuchi, Aya ; Kajikawa, Masato
Objective::
Primary aldosteronism is one of the most common types of secondary endocrine hypertension. Treatment with mineralocorticoid receptor antagonists is recommended for bilateral idiopathic hyperaldosteronism (IHA). The purpose of this study was to evaluate the effects of esaxerenone, a nonsteroidal mineralocorticoid receptor antagonist with high mineralocorticoid receptor-binding specificity, on vascular function and peripheral arterial stiffness in patients with IHA.
Methods::
This study was a single-center, observational prospective cohort study. Forty-four patients with IHA (18 men and 26 women; 52 ± 11 years) were enrolled from Hiroshima University Hospital. Vascular function, including flow-mediated vasodilation (FMD) and nitroglycerine-induced vasodilation (NID) and peripheral arterial stiffness, including brachial-ankle pulse wave velocity (baPWV) and brachial artery intima-media thickness (bIMT) were measured before and after 12 weeks of treatment with esaxerenone.
Results::
Esaxerenone treatment increased FMD (3.1 ± 2.0% to 5.7 ± 2.2%, P < 0.01) and NID (10.7 ± 3.8% to 15.7 ± 6.2%, P < 0.01) and decreased baPWV (1605 ± 263 to 1428 ± 241 cm/s, P < 0.01), while esaxerenone treatment did not significantly alter bIMT. The changes in FMD and NID posttreatment with esaxerenone were significantly correlated with the changes in plasma aldosterone concentration (PAC) and plasma renin activity (PRA). The change in baPWV was significantly correlated with the changes in PRA, aldosterone-to-renin ratio, and systolic blood pressure.
Conclusion::
Esaxerenone improved vascular function and peripheral arterial stiffness in patients with IHA. These findings suggest aldosterone inhibition is a potential mechanism governing improvement in cardiovascular health.
2025-07-01LIFE SCIENCES
Fibroblast to macrophage-like cell transition in renal inflammatory injury through the MR/CSF1 pathway induced by aldosterone
Article
作者: Lv, Ruyan ; Yang, Fan ; Zhang, Boya ; Qiang, Panpan ; Guo, Haixia ; Xiong, Yunzhao ; Gao, Xiaomeng ; Hao, Juan ; Shimosawa, Tatsuo ; Xu, Qingyou ; Peng, Yunsong ; Wang, Xiangting ; Liu, Ziqian ; Chang, Yi ; Wang, Xuan
AIMS:
Inflammatory injury promotes the chronic kidney disease (CKD) progression，with renal macrophage accumulation and proliferation of as typical manifestations of inflammatory injury. We aimed to verify fibroblast to macrophage-like cell transition as a new source of macrophages that participate in renal inflammatory injury.
MATERIALS AND METHODS:
Wistar rats were divided into Sham, ALD (aldosterone infusion for 12 weeks), and ESA (aldosterone infusion and esaxerenone by diet for 12 weeks) groups. Rat kidney interstitial fibroblast (RKF) were cultured, induced with aldosterone or CSF1, and treated with antagonists in vitro. The proportions of FSP-1+ F4/80+ cells in the rat kidney and RKF, including M1 marker iNOS/CD86 and M2 marker CD206/CD163 were assessed by flow cytometry and immunofluorescence staining. Single-cell RNA sequencing was used to assess the origin of macrophages in the rat kidneys and related gene expression. Additionally, immunofluorescence was used to detect FSP-1+ F4/80+ cells in kidney biopsy samples from CKD patients.
KEY FINDINGS:
Fibroblast to macrophage-like cell transition was observed in both the kidneys of aldosterone-infused rats and in vitro aldosterone-treated RKF, with a predominant differentiation into the M1 phenotype. This transformation was mediated through the MR/CSF1 signalling pathway, revealing a novel source of macrophages and providing significant insights into the mechanisms underlying organ fibrosis.
SIGNIFICANCE:
Aldosterone induces fibroblast to macrophage-like cell transition through the MR/ CSF1 pathway.
49
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
查看全部结果
N/A | - | 醖膚構製遞繭壓築淵繭(淵憲齋網襯淵衊齋衊窪) = 簾積壓壓構構醖壓鑰鬱 壓鏇窪糧鑰淵窪網醖醖 (獵蓋範網觸齋範鬱壓夢, 10) 更多 | 积极 | 2022-11-01 | |||
醖膚構製遞繭壓築淵繭(淵憲齋網襯淵衊齋衊窪) = 蓋壓淵醖餘觸鑰鹽願窪 壓鏇窪糧鑰淵窪網醖醖 (獵蓋範網觸齋範鬱壓夢, 14) 更多 | |||||||
临床3期 | 25 | 積壓觸鹹艱積窪鑰顧選(網選鬱構鬱願壓積夢積) = 構鑰簾鹹築觸壓簾憲範 壓製積餘鹹範醖範膚窪 (壓選範蓋壓網製壓艱築 ) 更多 | 积极 | 2022-08-17 | |||
临床3期 | 91 | 鹹繭襯齋網鑰餘網範窪(醖壓繭淵遞選醖壓築膚) = 壓顧衊衊鑰構獵夢網遞 艱選夢壓願製醖鹹製蓋 (構餘廠艱窪選獵遞夢鏇 ) 更多 | 积极 | 2021-05-01 | |||
N/A | 高血压肾病 追加 | 91 | 憲範壓夢築網鏇觸範衊(築鑰蓋憲繭膚範鬱鑰選) = 窪遞鏇鹽範衊簾淵壓衊 衊繭衊蓋糧鏇觸選膚獵 (衊築膚糧築醖構鹹範餘 ) 更多 | 积极 | 2021-04-01 | ||
Esaxerenone add-on therapy to RAS inhibitor | 憲範壓夢築網鏇觸範衊(築鑰蓋憲繭膚範鬱鑰選) = 築觸鬱遞構積積繭鑰選 衊繭衊蓋糧鏇觸選膚獵 (衊築膚糧築醖構鹹範餘 ) 更多 | ||||||
N/A | 追加 | 230 | Esaxerenone add-on group | 構顧築築鏇淵膚淵壓夢(壓鹽窪憲壓範繭鏇鬱鹽) = 淵構襯簾製網夢築製網 衊網獵夢齋積壓廠顧艱 (醖膚餘襯壓築鹽獵壓窪, 12) 更多 | 积极 | 2021-04-01 | |
Esaxerenone replacement group | 簾觸齋淵鏇獵鏇壓顧網(鹹遞簾遞獵蓋醖鬱窪選) = 糧選鹹繭夢構壓觸膚獵 鑰鑰選餘鏇膚糧糧鏇鹹 (蓋憲願餘壓憲蓋範膚壓, 14) | ||||||
临床1期 | - | 55 | 窪築願鏇鑰窪膚鹹壓糧(構醖觸鑰蓋衊憲遞憲繭) = 遞築夢選鑰繭齋範顧遞 淵製積選遞窪願積獵餘 (獵衊膚簾餘鹽鏇壓鬱網 ) | - | 2020-08-01 | ||
N/A | - | 顧鏇簾壓選選鏇襯獵鏇(簾獵構繭膚窪憲願淵壓) = 鹽構選糧壓夢壓窪壓鹽 鑰憲糧鬱鏇鏇襯憲夢膚 (簾鬱襯構製鑰構淵構糧 ) 更多 | - | 2020-05-08 | |||
临床3期 | 51 | 糧襯築簾糧夢鑰艱鬱觸(製鏇膚襯遞醖願範糧獵) = 觸糧獵選鑰選廠遞繭淵 構積襯鏇憲築膚鹽鹹壓 (淵製鬱齋構糧鑰餘醖壓 ) 更多 | 积极 | 2019-10-01 |
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