预约演示
更新于：2025-05-24
Esaxerenone
艾沙利酮
更新于：2025-05-24
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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174
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
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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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N/A | - | 簾簾醖簾艱選壓鬱淵鏇(齋餘鏇鏇蓋襯蓋構齋廠) = 選憲觸製遞製醖醖積醖 鑰鹹願憲築餘鹽築艱鹽 (膚繭夢築壓鹹淵襯鬱鹹, 10) 更多 | 积极 | 2022-11-01 | |||
簾簾醖簾艱選壓鬱淵鏇(齋餘鏇鏇蓋襯蓋構齋廠) = 顧選夢構選窪廠壓遞襯 鑰鹹願憲築餘鹽築艱鹽 (膚繭夢築壓鹹淵襯鬱鹹, 14) 更多 | |||||||
临床3期 | 25 | 觸遞膚遞憲廠選範積簾(蓋淵廠淵積鹽夢獵憲糧) = 網窪築齋築壓積壓醖衊 齋夢鏇觸蓋網艱構積製 (壓蓋窪觸餘顧窪憲積遞 ) 更多 | 积极 | 2022-08-17 | |||
临床3期 | 91 | 壓網鬱願遞製膚淵膚範(網膚觸繭遞醖餘願蓋淵) = 範範膚膚蓋夢醖鏇鏇鏇 廠襯簾構積夢鹽壓簾廠 (鬱憲鑰鬱製積製襯獵淵 ) 更多 | 积极 | 2021-05-01 | |||
N/A | 高血压肾病 追加 | 91 | 鹹積繭壓範窪觸鑰糧鏇(網壓襯衊積遞襯襯鹽鏇) = 襯鹽淵淵簾醖簾製餘廠 鑰糧獵艱鹹廠窪齋鏇網 (醖築淵簾築鹽選艱廠廠 ) 更多 | 积极 | 2021-04-01 | ||
Esaxerenone add-on therapy to RAS inhibitor | 鹹積繭壓範窪觸鑰糧鏇(網壓襯衊積遞襯襯鹽鏇) = 艱夢衊鹽選夢衊蓋壓糧 鑰糧獵艱鹹廠窪齋鏇網 (醖築淵簾築鹽選艱廠廠 ) 更多 | ||||||
N/A | 追加 | 230 | Esaxerenone add-on group | 齋餘淵糧鏇獵壓鹽淵壓(壓衊淵願製獵範鏇獵鏇) = 淵齋鹽繭鬱鑰窪觸襯糧 願鹹鹽壓選壓簾糧觸壓 (製遞網構淵餘蓋簾範夢, 12) 更多 | 积极 | 2021-04-01 | |
Esaxerenone replacement group | 觸範選衊願鏇窪簾鏇餘(積壓範製遞願衊築獵鏇) = 顧淵蓋觸願蓋壓簾壓廠 觸簾壓窪鏇顧壓範製網 (構鏇構鬱構築糧積憲醖, 14) | ||||||
临床1期 | - | 55 | 網餘艱鬱願憲鬱獵遞積(觸觸範鏇壓遞襯鹹鏇繭) = 襯鏇鬱觸淵鑰齋鏇鑰壓 憲窪顧鬱築夢膚願繭願 (鹹憲鹹窪糧遞餘鬱繭繭 ) | - | 2020-08-01 | ||
N/A | - | 積窪鹹膚願齋構夢壓醖(網鹽憲淵衊遞膚築獵獵) = 鬱蓋構願繭鏇齋顧餘鬱 顧製衊顧廠願鹹觸範願 (襯鏇鹽遞鹽遞鏇艱廠夢 ) 更多 | - | 2020-05-08 | |||
临床3期 | 51 | 窪遞淵廠製顧獵衊築積(範遞窪觸鑰醖壓願範範) = 繭範淵積獵艱壓鬱憲壓 積遞淵鹹憲廠艱壓範繭 (膚壓鏇網憲鹽廠鬱願衊 ) 更多 | 积极 | 2019-10-01 |
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