坎利酮(Canrenone) - 药物靶点：MR_在研适应症：高血压_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Canrenone (USAN)、canrenone

+ [2]

靶点

MR

作用方式

调节剂

作用机制

MR调节剂(盐皮质激素受体调节剂)

治疗领域

心血管疾病

在研适应症

高血压

非在研适应症-

原研机构-

在研机构-

非在研机构-

最高研发阶段批准上市

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C22H28O3

InChIKeyUJVLDDZCTMKXJK-WNHSNXHDSA-N

CAS号976-71-6

关联

5

项与坎利酮相关的临床试验

EUCTR2021-001360-20-IT

/ Unknown status临床2期IIT

MINECRAFT Study: MINEralcorticoid receptor antagonism with CanRenone As eFfective Treatment in moderate to severe ARDS in COVID-19, a phase 2 clinical trial. - Canrenone for COVID-19 patients

开始日期2021-07-29

申办/合作机构-

NCT03536806

/ Unknown status临床4期IIT

Clinical Efficacy of Potassium Canrenoate - Canrenone in Sinus Rhythm Restoration Among Patients With Atrial Fibrillation and Elevated Blood Pressure - a Pilot Randomized Controlled Trial.

The purpose of this randomized, double blind, placebo-controlled, superiority clinical trial was to assess clinical efficacy of potassium canrenoate - canrenone in rapid conversion of atrial fibrillation to sinus rhythm.

开始日期2018-06-01

申办/合作机构-

NCT03263962

/ CompletedN/AIIT

Canrenone Effects on Cardiovascular Mortality in Patients With Congestive Heart Failure: the Coffee-it Study

To evaluate canrenone effects compared to other therapies on cardiovascular mortality in patients with congestive heart failure and preserved systolic function after 12 years of evaluation.

开始日期2017-07-13

申办/合作机构

Universitiamo By Unipv

100 项与坎利酮相关的临床结果

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100 项与坎利酮相关的转化医学

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100 项与坎利酮相关的专利（医药）

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791

项与坎利酮相关的文献（医药）

2025-03-01·Industrial Crops and Products

Beneficial microbial consortia effectively alleviated plant stress caused by the synergistic toxicity of microplastics and cadmium

作者: Gao, Shan-Shan ; Li, Yu-Ying ; Zhang, Yu ; Li, B. Larry ; Han, Hui ; Chen, Zhao-Jin ; Chen, Yan ; Jiao, Rui-Qi

Combined pollution from microplastics and heavy metals has garnered research interest because of the potential for complex interactions between these contaminants.Composite functional bacteria present significant benefits in the bioremediation of contaminated soils and have attracted widespread attention.Researchers have yet to elucidate how effectively plant growth-promoting bacterial (PGPB) consortia mitigate the stress induced by combined pollution from microplastics and heavy metals.Pot experiments indicate that combined polyvinyl chloride (PVC) + cadmium (Cd) pollution results in "synergistic toxicity" relative to Cd or PVC pollution alone.The application of PGPB consortia inoculants is more effective than the use of single strains in alleviating stress caused by PVC + Cd pollution.The combined inoculant increased bioenergy plant sorghum growth and biomass and increased the contents of total nitrogen, total phosphorus, total potassium, available potassium, and available phosphorus in the soil.Under combined PVC + Cd pollution conditions, PGPB inoculation affected the composition of the sorghum rhizosphere bacterial community.Cooccurrence network anal. revealed that the PGPB consortia can alter soil bacterial community diversity and increase the stability of soil bacterial communities.PGPB consortia can alter the composition of soil metabolites and impact various metabolic pathways.These changes increase the ability of sorghum plants to respond to PVC + Cd stress.This study revealed that the use of combined PGPB affects the soil inorganic nutrient content and the functional composition of bacterial communities, effectively alleviating stress caused by combined microplastic and heavy metal pollution.These findings provide tech. support for the development of bioremediation strategies tailored to address combined microplastic and heavy metal pollution.

2025-02-01·Environmental Pollution

Occurrence and potential risk of steroid hormones in selected surface water and wastewater treatment plants in western Kenya

Article

作者: Shahid, Naeem ; Krauss, Martin ; Kiprop, Ambrose ; Kandie, Faith ; Tanui, Isaac Cheruiyot ; Piotrowska, Aleksandra ; Brack, Werner ; Liess, Matthias ; Hollert, Henner ; Finckh, Saskia

Steroid hormones are significant contributors to endocrine disruption, affecting the hormonal functions of both humans and aquatic organisms. However, data on their occurrence and risks in fresh water systems particularly in low- and middle-income countries, is scarce. In this regard, a comprehensive investigation of 58 steroid hormones in rivers and wastewater treatment plants (WWTPs) was conducted in western Kenya. Grab water samples were extracted by solid phase extraction, and analysed using liquid chromatography tandem mass spectrometry (LC-MS/MS) and liquid chromatography high-resolution mass spectrometry (LC-HRMS). Forty-three steroids were identified with 24 of them being found in both rivers and WWTPs. The median concentrations of detected steroids ranged from 0.06 ng/L to 9 ng/L in rivers, 1.9 ng/L to 670 ng/L in the influents and 0.61 ng/L to 270 ng/L at the effluents. The most frequently detected compound in the rivers was 17β-estradiol occurring in 64% of the samples. Although 23 compounds were reduced to undetectable levels in WWTPs, 90% of the effluents exceeded tentative risk thresholds for estrogenicity. In rivers, concentrations of estrogenic and glucocorticoid effects were in the range of risk thresholds, while androgenic and progestagenic concentrations were below risk thresholds. This study contributes to the occurrence of steroid hormones and an understanding of their potential impacts on freshwater ecosystem and human health. The data generated from the study provides crucial information for the formulation of environmental policies in Kenya.

2025-01-01·Journal of Ethnopharmacology

Novel detoxifier of spironolactone against triptolide-induced hepatotoxicity through inhibition of RPB1 degradation

Article

ETHNOPHARMACOLOGICAL RELEVANCETriptolide is a major bioactive and toxic ingredient isolated from the traditional Chinese herb Tripterygium wilfordii (T. wilfordii) Hook F. It exhibits potent antitumor, immunosuppressive, and anti-inflammatory biological activities; however, its clinical application is hindered by severe systemic toxicity. Two preparations of T. wilfordii, including T. wilfordii glycoside tablets and T. wilfordii tablets, containing triptolide, are commonly used in clinical practice. However, their adverse side effects, particularly hepatotoxicity, limit their safe use. Therefore, it is crucial to discover potent and specific detoxification medicines for triptolide.AIM OF THE STUDYThis study aimed to investigate the detoxification effects and potential mechanism of action of spironolactone on triptolide-induced hepatotoxicity to provide a potential detoxifying strategy for triptolide, thereby promoting the safe applications of T. wilfordii preparations in clinical settings.MATERIALS AND METHODSCell viability was assessed using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and crystal violet staining. Nuclear fragmentation was visualized using 4',6-diamidino-2-phenylindole (DAPI) staining, and protein expression was analyzed by Western blotting. The inhibitory effect of spironolactone on triptolide-induced hepatotoxicity was evaluated by examining the effects of spironolactone on serum alanine aminotransferase and aspartate aminotransferase levels, as well as liver pathology in a mouse model of triptolide-induced acute hepatotoxicity. Furthermore, a survival assay was performed to investigate the effects of spironolactone on the survival rate of mice exposed to a lethal dose of triptolide. The effect of spironolactone on triptolide-induced global transcriptional repression was assessed through 5-ethynyl uridine staining.RESULTSTriptolide treatment decreased the cell viability, increased the nuclear fragmentation and the cleaved caspase-3 levels in both hepatoma cells and hepatocytes. It also increased the alanine aminotransferase and aspartate aminotransferase levels, induced the hepatocyte swelling and necrosis, and led to seven deaths out of 11 mice. The above effects could be mitigated by pretreatment with spironolactone. Additionally, molecular mechanism exploration unveiled that spironolactone inhibited triptolide-induced DNA-directed RNA polymerase II subunit RPB1 degradation, consequently increased the fluorescence intensity of 5-ethynyl uridine staining for nascent RNA.CONCLUSIONSThis study shows that spironolactone exhibits a potent detoxification role against triptolide hepatotoxicity, through inhibition of RPB1 degradation induced by triptolide and, in turn, retardation of global transcriptional inhibition in affected cells. These findings suggest a potential detoxification strategy for triptolide that may contribute to the safe use of T. wilfordii preparations.

100 项与坎利酮相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D03363	坎利酮	C03DA03	DB12221

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
高血压	-	-	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


[PP.09.18] (ESH2017)	N/A	原发性高血压	-	Canrenone 50 mg/day	觸選齋襯製鬱糧製遞襯(衊廠構網齋蓋蓋餘遞積) = 艱鏇糧衊衊膚選願壓範窪範簾繭選襯範膚顧鹹 (繭窪鑰鏇襯鹽範鏇鬱衊 )	积极	2017-09-01
				Canrenone 100 mg/day	觸選齋襯製鬱糧製遞襯(衊廠構網齋蓋蓋餘遞積) = 顧廠願壓夢簾衊鏇願衊窪範簾繭選襯範膚顧鹹 (繭窪鑰鏇襯鹽範鏇鬱衊 )
NCT02687178 (ESCAPE-IT, Pubmed \| Cardiovasc Ther)	临床4期	高血压追加	175	Canrenone 50 mg	鏇憲醖遞構憲壓獵膚顧(鹽顧糧觸衊壓範網觸遞) = 壓廠觸鹽衊窪網窪糧顧餘獵積廠憲鹽繭構醖觸 (構窪鑰顧顧鏇遞網餘築 ) 更多	-	2017-02-01
				Canrenone 100 mg	鏇憲醖遞構憲壓獵膚顧(鹽顧糧觸衊壓範網觸遞) = 廠壓淵鬱齋鏇顧壓鬱構餘獵積廠憲鹽繭構醖觸 (構窪鑰顧顧鏇遞網餘築 ) 更多
NCT00403910 (AREA IN-CHF, Pubmed \| Eur J Heart Fail)	临床3期	慢性心力衰竭	-	Canrenone	(醖憲夢鹽鏇構簾構簾糧) = 鏇製餘製範製鹽醖顧窪鑰觸顧製範築艱膚繭壓 (遞憲網壓鹽蓋製網構襯 ) 更多	-	2009-01-01
				Placebo	(醖憲夢鹽鏇構簾構簾糧) = 築範窪範鏇觸艱廠範廠鑰觸顧製範築艱膚繭壓 (遞憲網壓鹽蓋製網構襯 ) 更多
NCT00403910 (AREA IN-CHF, Pubmed \| J Cardiovasc Med (Hagerstown))	临床3期	慢性心力衰竭	467	Canrenone	淵夢製蓋醖壓願網繭網(簾獵襯網淵醖鑰選繭積) = 齋夢簾選艱繭網齋網壓觸積壓構糧醖積鹹製鏇 (獵觸夢鹹築網鹽選蓋餘 ) 更多	-	2007-09-01
				Placebo	淵夢製蓋醖壓願網繭網(簾獵襯網淵醖鑰選繭積) = 襯餘壓製構願網廠鹹遞觸積壓構糧醖積鹹製鏇 (獵觸夢鹹築網鹽選蓋餘 ) 更多