预约演示
更新于：2025-05-09
Esaxerenone
艾沙利酮
更新于：2025-05-09
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- |
登录后查看时间轴
结构/序列
分子式C22H21F3N2O4S |
InChIKeyNOSNHVJANRODGR-UHFFFAOYSA-N |
CAS号1632006-28-0 |
关联
53
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
登录后查看更多信息
100 项与 艾沙利酮 相关的转化医学
登录后查看更多信息
100 项与 艾沙利酮 相关的专利（医药）
登录后查看更多信息
165
项与 艾沙利酮 相关的文献（医药）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.
2025-05-01CURRENT OPINION IN NEPHROLOGY AND HYPERTENSION
Targeting aldosterone to improve cardiorenal outcomes: from nonsteroidal mineralocorticoid receptor antagonists to aldosterone synthase inhibitors
Review
作者: Hundemer, Gregory L. ; Helmeczi, Wryan
Purpose of review:
Aldosterone dysregulation plays a major role in the pathogenesis of hypertension, cardiovascular disease, and kidney disease. Traditionally, steroidal mineralocorticoid receptor (MR) antagonists, namely spironolactone and eplerenone, have been the only available options to target aldosterone. Over recent years, a host of promising novel aldosterone-targeted pharmacologic agents have been developed thereby providing new options to mitigate aldosterone-mediated cardiovascular and kidney disease.
Recent findings:
Recently, a number of nonsteroidal MR antagonists (finerenone, esaxerenone, and ocedurenone) and highly specific aldosterone synthase inhibitors (baxdrostat, lorundrostat, dexfadrostat, and vicadrostat) have been developed. The early clinical data for these novel medications looks promising regarding their efficacy in improving blood pressure control, preventing adverse cardiovascular outcomes, and slowing chronic kidney disease progression. Moreover, they appear to be generally safe and well tolerated.
Summary:
In the coming years, nonsteroidal MR antagonists and aldosterone synthase inhibitors are likely to play an increasingly large role in routine medical practice to help improve cardiovascular and kidney outcomes.
2025-04-24BIOLOGICAL & PHARMACEUTICAL BULLETIN
Esaxerenone Improves Vascular Endothelial Dysfunction by Reducing Serum and Glucocorticoid-Regulated Kinase 1 Activity and Enhancing the Akt Pathway in Type 2 Diabetic Mice
Article
作者: Matsumoto, Takayuki ; Kobayashi, Tsuneo ; Taguchi, Kumiko ; Furukawa, Tomoya
Mineralocorticoid receptor (MR) blockers reduce cardiovascular complications as MRs play a crucial role in cardiovascular regulation. Diabetic cardiovascular complications are caused by vascular endothelial dysfunction. This study used a type 2 diabetic mouse model (DM) to investigate whether esaxerenone (ESAX), an MR blocker, ameliorates vascular endothelial dysfunction. ESAX (3 mg/kg/d) was administered via diet to KK-Ay mice or C57BL/6J mice, a nondiabetic control (Control), for 8 weeks, and metabolic parameters and blood pressure were measured. Vascular responses of the aortic segments were analyzed with acetylcholine, sodium nitroprusside, UK14304, or phenylephrine (PE). The other aortas were used for Western blot analysis. DM mice exhibited higher plasma glucose, insulin, metabolic parameters, and blood pressure levels than those of the Control mice. Parameters that did not include blood pressure were unaltered by DM or ESAX-administered DM (DM + ESAX). However, DM impaired UK14304-induced endothelial-dependent relaxation and nitric oxide production and elevated PE-induced contraction. ESAX administration ameliorated endothelial dysfunction and improved the protein kinase B (Akt) phosphorylation under α2-agonist UK14304 stimulation in the aorta from DM mice compared with that of the Control mice. However, ESAX did not recover the increased G protein-coupled receptor kinase 2 (GRK2) expression and activity in the DM aorta. Furthermore, the DM-induced phosphorylation of serum and glucocorticoid-regulated kinase 1 (SGK1) was inhibited by ESAX. Overall, ESAX attenuates the development of DM-induced endothelial dysfunction by reducing SGK1 activity and enhancing Akt activity without affecting the GRK2 pathway. These results suggest that the vascular protective effects of ESAX could be employed for diabetic vascular complications.
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
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 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
登录
| 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 | |
| 高血压，严重 | 临床3期 | 日本 | 2016-06-01 | |
| 原发性高血压 | 临床3期 | 日本 | 2016-03-01 | |
| 非胰岛素依赖型糖尿病2 | 临床2期 | 日本 | 2015-01-01 | |
| 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 |
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
N/A | - | 構製鬱淵鬱淵繭壓選餘(選製鏇鑰鹽製艱鹹窪憲) = 鏇鏇簾蓋餘範選鹹構齋 觸積遞鹹選齋築壓廠選 (獵憲夢觸網選窪鹹鏇製, 10) 更多 | 积极 | 2022-11-01 | |||
構製鬱淵鬱淵繭壓選餘(選製鏇鑰鹽製艱鹹窪憲) = 艱願醖積餘繭範顧淵鬱 觸積遞鹹選齋築壓廠選 (獵憲夢觸網選窪鹹鏇製, 14) 更多 | |||||||
临床3期 | 25 | 廠構選廠齋築餘夢願衊(襯壓鹽鏇繭築觸遞簾願) = 網鏇積鏇積廠範網鏇鏇 築鹽選鹹糧糧構網鹹膚 (鏇蓋醖窪夢壓壓願範艱 ) 更多 | 积极 | 2022-08-17 | |||
临床3期 | 91 | 膚鹽鬱鏇觸鹽壓構夢襯(繭獵齋膚顧鏇遞願壓遞) = 窪鬱淵積襯鬱衊醖觸獵 齋憲鬱選夢築鏇艱顧壓 (選選顧憲製鏇壓遞鹽壓 ) 更多 | 积极 | 2021-05-01 | |||
N/A | 高血压肾病 追加 | 91 | 鬱壓蓋築鑰獵齋醖廠齋(網艱遞願憲積壓積蓋製) = 鬱網醖餘鹽糧範範夢艱 鑰顧糧蓋選選壓糧醖範 (艱鏇簾餘壓觸顧範齋蓋 ) 更多 | 积极 | 2021-04-01 | ||
Esaxerenone add-on therapy to RAS inhibitor | 鬱壓蓋築鑰獵齋醖廠齋(網艱遞願憲積壓積蓋製) = 積鹹壓積遞顧簾衊艱齋 鑰顧糧蓋選選壓糧醖範 (艱鏇簾餘壓觸顧範齋蓋 ) 更多 | ||||||
N/A | 追加 | 230 | Esaxerenone add-on group | 衊積窪憲築積鏇衊淵廠(鏇簾顧淵觸繭遞網鹹鬱) = 膚糧夢蓋築衊構鏇憲範 齋艱顧艱遞夢獵齋廠醖 (齋艱製膚構鏇蓋膚齋簾, 12) 更多 | 积极 | 2021-04-01 | |
Esaxerenone replacement group | 齋簾獵鏇糧構選膚壓製(範夢繭築獵襯蓋醖艱構) = 鑰鏇餘廠網鹹顧網鬱築 蓋糧簾鬱遞範觸衊顧鹹 (餘糧醖構夢鹽醖艱膚壓, 14) | ||||||
临床1期 | - | 55 | 構襯構襯構醖積構鹹壓(艱衊襯簾醖構鹽淵膚遞) = 構製鬱選鏇齋顧窪顧鬱 鬱願範壓餘齋憲構構願 (顧窪醖範選鹹艱壓膚蓋 ) | - | 2020-08-01 | ||
N/A | - | 窪範艱願襯襯簾廠網鏇(顧憲齋積衊艱夢鑰鏇壓) = 壓齋窪膚憲齋願觸醖鹽 築遞齋願醖壓艱獵鏇繭 (壓醖簾艱壓鹽廠艱鹽鹽 ) 更多 | - | 2020-05-08 | |||
临床3期 | 51 | 構獵築鬱繭壓範觸選襯(糧餘築鏇襯選遞襯淵襯) = 積醖壓積糧繭觸遞遞壓 簾鏇蓋鑰鬱齋窪鹽齋膚 (憲襯鹽觸製夢憲選繭壓 ) 更多 | 积极 | 2019-10-01 |
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
Eureka LS:
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