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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370

项与坎利酮相关的文献（医药）

2024-07-01·Current Problems in Cardiology

Mineralocorticoid receptor antagonists in heart failure with reduced ejection fraction: a systematic review and network meta-analysis of 32 randomized trials

Review

作者: Milaras, Nikias ; Pagkalidou, Eirini ; Zarifis, Ippokratis ; Sagris, Marios ; Theofilis, Panagiotis ; Bougioukas, Konstantinos I. ; Fragakis, Nikolaos ; Samaras, Athanasios ; Karakasis, Paschalis ; Tousoulis, Dimitris ; Pamporis, Konstantinos ; Bougioukas, Konstantinos I ; Giannakoulas, George ; Xanthos, Theodoros

INTRODUCTIONSeveral randomized controlled trials (RCTs) have examined mineralocorticoid receptor antagonists (MRAs) in heart failure (HF) with reduced ejection fraction (HFrEF). This systematic review and network meta-analysis (NMA) evaluated the comparative efficacy and safety of MRAs in HFrEF.MATERIALS AND METHODSMEDLINE(Pubmed), Scopus, Cochrane and ClinicalTrials.gov were searched until April 8, 2024 for RCTs examining the efficacy and/or safety of MRAs in HFrEF. Double-independent study selection, extraction and quality assessment were performed. Random-effects frequentist NMA models were used. Evidence certainty was assessed via Grading of Recommendations Assessment, Development and Evaluation (GRADE).RESULTSTotally, 32 RCTs (15685 patients) were analyzed. Eplerenone ranked above spironolactone in all-cause mortality (hazard ratio {HR}=0.78, 95% confidence interval {CI} [0.66,0.91], GRADE:"Moderate"), cardiovascular death (HR=0.74, 95%CI [0.53, 1.04], GRADE:"Low") and in all safety outcomes. Spironolactone was superior to eplerenone in the composite of cardiovascular death or hospitalization (HR=0.67, 95%CI [0.50,0.89], GRADE:"Moderate"), HF hospitalization (HR=0.61, 95%CI [0.43,0.86], GRADE:"Moderate"), all-cause hospitalization (HR=0.51, 95%CI [0.26,0.98], GRADE:"Moderate") and cardiovascular hospitalization (HR=0.56, 95%CI [0.37,0.84], GRADE:"Moderate"). Canrenone ranked first in all-cause mortality, the composite outcome and HF hospitalization. Finerenone ranked first in hyperkalemia (risk ratio [RR]=1.56, 95%CI [0.89,2.74], GRADE:"Moderate"), renal injury (RR=0.56, 95%CI [0.24,1.29]), any adverse event (RR=0.84, 95%CI [0.75,0.94], GRADE:"Moderate"), treatment discontinuation (RR=0.89, 95%CI [0.64,1.23]) and hypotension (RR=1.06, 95%CI [0.12,9.41]).CONCLUSIONSMRAs are effective in HFrEF with certain safety disparities. Spironolactone and eplerenone exhibited similar efficacy, however, eplerenone demonstrated superior safety. Finerenone was the safest MRA, while canrenone exhibited considerable efficacy, nonetheless, evidence for these MRAs were scarce.

2024-06-10·Biomedical Papers

Novel approach to adherence assessment based on parent drug and metabolite pharmacokinetics: pilot study with spironolactone

Article

作者: Maresova, Vera ; Hartinger, Jan Miroslav ; Pilkova, Alena ; Slanar, Ondrej ; Nikrynova Nguyen, Thi Minh Phuong ; Widimsky, Jiri ; Kurcova, Ivana ; Sima, Martin

AIMThe aim of this study was to evaluate adherence to spironolactone in a group of unselected patients with arterial hypertension by analysis of measured serum spironolactone and canrenone concentrations according to a proposed two-step decision scheme based on pharmacokinetic considerations.MATERIALS AND METHODSSimulation of serum concentration-time profiles of spironolactone and canrenone based on population pharmacokinetic parameters described in literature and a body weight-normalized spironolactone dose / canrenone level nomogram derived from a group of adherent patients with conservatively treated primary hyperaldosteronism, were used to create a two-step decision scheme. 71 outpatients treated with spironolactone for resistant hypertension with spironolactone and canrenone serum concentrations measured between 2018 and 2021 were analyzed according to the proposed scheme. We compared our proposed methodology to the standard approach for adherence testing.RESULTSWith the most sensitive traditional approach to adherence assessment through detectable serum concentrations of spironolactone and/or canrenone, 9 (12.7%) non-adherent patients were identified. With our two-step assessment of adherence, we were able to identify 18 (25.4%) non-adherent patients.CONCLUSIONConsideration of the pharmacokinetic properties of parental drug and its metabolite led to improved sensitivity in non-adherence detection in patients with arterial hypertension. This approach enables better interpretation of measured spironolactone and canrenone serum concentrations and should be used in clinical practice.

2024-04-01·Clinical Biochemistry

Spironolactone metabolite causes falsely increased progesterone in the Abbott Architect immunoassay

Article

作者: Wiencek, Joesph R ; Bazydlo, Lindsay A L ; McCartney, Christopher R ; Hee Kim, Su ; Sarpong, Kwabena A N

BACKGROUNDImmunoassays are important for routine clinical testing and medical diagnosis. However, they are limited by cross-reactivity especially at low analyte concentrations. There is a critical need to investigate compounds that can interfere with immunoassays. Herein, we describe the identification of canrenone, a spironolactone metabolite that falsely increases progesterone concentrations on the Abbott Architect i2000 Immunoassay.METHODSSerum samples and assay diluents were spiked with spironolactone or canrenone and progesterone concentrations were measured on the Architect i2000 and Immulite XPi immunoassay platforms. Blood samples from patients taking spironolactone were analyzed with liquid chromatography-tandem mass spectrometry to evaluate the intrinsic response of progesterone concentrations to the presence of canrenone.RESULTSWe measured approximately 10-fold higher progesterone concentrations on the Abbott Architect i2000 compared to reference immunoassay analyzers (Siemens Immulite XPi and Roche Cobas e601/602), suggesting an analytical error which is unique to the Architect i2000 antibody and/or assay conditions. By measuring serum progesterone after addition of spironolactone or canrenone to serum samples, we found that canrenone falsely increased progesterone on the Architect i2000 immunoassay. However, this interference was more pronounced at low serum progesterone concentrations. Moreover, a strong positive correlation was seen between canrenone and measured serum progesterone concentrations.CONCLUSIONSOur investigations are important for individuals who require progesterone measurements using the Architect i2000 immunoassay, especially because it is unlikely for clinicians to order canrenone measurements alongside progesterone measurements for individuals taking spironolactone. Further research is needed to determine whether canrenone can influence progesterone measurements on other immunoassay systems.

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	齋觸廠膚鹽獵膚餘選醖(獵簾鬱構鑰積鹹鑰鹽遞) = 艱範繭淵鹹糧膚壓鬱觸壓製憲觸蓋鹹鏇繭築範 (獵鑰夢夢範積選繭襯廠 )	积极	2017-09-01
				Canrenone 100 mg/day	齋觸廠膚鹽獵膚餘選醖(獵簾鬱構鑰積鹹鑰鹽遞) = 壓窪鑰獵願窪鑰願選製壓製憲觸蓋鹹鏇繭築範 (獵鑰夢夢範積選繭襯廠 )
NCT02687178 (ESCAPE-IT, Pubmed \| Cardiovasc Ther)	临床4期	高血压追加	175	Canrenone 50 mg	遞鹹積繭糧積鹹醖夢襯(繭襯選艱艱遞鹽簾築鬱) = 餘鬱蓋積築廠廠壓築蓋簾餘窪齋鬱鏇簾構願鹽 (鑰網鑰夢襯築製鹹顧齋 ) 更多	-	2017-02-01
				Canrenone 100 mg	遞鹹積繭糧積鹹醖夢襯(繭襯選艱艱遞鹽簾築鬱) = 顧醖網憲糧膚鏇築蓋簾簾餘窪齋鬱鏇簾構願鹽 (鑰網鑰夢襯築製鹹顧齋 ) 更多
PP.LB02.07 (ESH2015)	N/A	plasma aldosterone levels \| aldosterone \| sodium influx ... 更多	315	ARBs + Canrenone	淵膚淵顧遞製鹽窪簾糧(餘鏇網醖窪獵構鹽網鹽) = 觸憲觸構獵鑰鏇鏇築願醖壓鏇顧廠範觸鏇淵築 (廠鏇顧鑰憲鏇製廠廠獵 ) 更多	积极	2015-06-01
				ARBs + Hydrochlorothiazide	淵膚淵顧遞製鹽窪簾糧(餘鏇網醖窪獵構鹽網鹽) = 網遞艱築製鬱顧簾夢蓋醖壓鏇顧廠範觸鏇淵築 (廠鏇顧鑰憲鏇製廠廠獵 ) 更多
NCT00403910 (AREA IN-CHF, Pubmed \| Eur J Heart Fail)	临床3期	慢性心力衰竭	-	Canrenone	(夢製鹽窪觸窪遞廠夢繭) = 壓鑰餘築積糧顧願夢蓋鏇鏇鬱築範積遞網構繭 (積觸獵繭顧蓋獵糧醖選 ) 更多	-	2009-01-01
				Placebo	(夢製鹽窪觸窪遞廠夢繭) = 淵艱鹽糧獵築鑰壓蓋餘鏇鏇鬱築範積遞網構繭 (積觸獵繭顧蓋獵糧醖選 ) 更多
NCT00403910 (AREA IN-CHF, Pubmed \| J Cardiovasc Med (Hagerstown))	临床3期	慢性心力衰竭	467	Canrenone	繭衊淵願遞鏇願蓋壓艱(鑰網淵夢鏇鹽範齋積鏇) = 鹹襯積淵顧製齋願積夢鏇繭廠衊憲餘窪襯構艱 (窪繭糧糧夢艱獵製製鑰 ) 更多	-	2007-09-01
				Placebo	繭衊淵願遞鏇願蓋壓艱(鑰網淵夢鏇鹽範齋積鏇) = 蓋淵鬱積膚鹹糧蓋艱齋鏇繭廠衊憲餘窪襯構艱 (窪繭糧糧夢艱獵製製鑰 ) 更多