U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C24H30O6
Molecular Weight 414.4923
Optical Activity UNSPECIFIED
Defined Stereocenters 8 / 8
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of EPLERENONE

SMILES

C[C@@]12CCC(=O)C=C2C[C@]([H])([C@@]3([H])[C@]4([H])CC[C@@]5(CCC(=O)O5)[C@@]4(C)C[C@]6([H])[C@@]31O6)C(=O)OC

InChI

InChIKey=JUKPWJGBANNWMW-VWBFHTRKSA-N
InChI=1S/C24H30O6/c1-21-7-4-14(25)10-13(21)11-15(20(27)28-3)19-16-5-8-23(9-6-18(26)30-23)22(16,2)12-17-24(19,21)29-17/h10,15-17,19H,4-9,11-12H2,1-3H3/t15-,16+,17-,19+,21+,22+,23-,24-/m1/s1

HIDE SMILES / InChI

Molecular Formula C24H30O6
Molecular Weight 414.4923
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 8 / 8
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: Description was created based on several sources, including https://www.drugs.com/cdi/eplerenone.html

Eplerenone, an aldosterone receptor antagonist similar to spironolactone, has been shown to produce sustained increases in plasma renin and serum aldosterone, consistent with inhibition of the negative regulatory feedback of aldosterone on renin secretion. The resulting increased plasma renin activity and aldosterone circulating levels do not overcome the effects of eplerenone. Eplerenone selectively binds to recombinant human mineralocorticoid receptors relative to its binding to recombinant human glucocorticoid, progesterone and androgen receptors. Eplerenone binds to the mineralocorticoid receptor and thereby blocks the binding of aldosterone (component of the renin-angiotensin-aldosterone-system, or RAAS). Aldosterone synthesis, which occurs primarily in the adrenal gland, is modulated by multiple factors, including angiotensin II and non-RAAS mediators such as adrenocorticotropic hormone (ACTH) and potassium. Aldosterone binds to mineralocorticoid receptors in both epithelial (e.g., kidney) and nonepithelial (e.g., heart, blood vessels, and brain) tissues and increases blood pressure through induction of sodium reabsorption and possibly other mechanisms. Used for improvement of survival of stable patients with left ventricular systolic dysfunction (ejection fraction <40%) and clinical evidence of congestive heart failure after an acute myocardial infarction.

Originator

Curator's Comment:: # Novartis

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
122.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
INSPRA

Approved Use

INSPRA is an aldosterone antagonist indicated for: Improving survival of stable patients with LV systolic dysfunction (LVEF ≤40%) and CHF after an acute myocardial infarction. Hypertension, alone or combined with other agents.

Launch Date

1.03299842E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2.49 μg/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EPLERENONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
18.4 μg × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EPLERENONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
3.01 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EPLERENONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
38.2%
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EPLERENONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
200 mg 2 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources:
unhealthy, 21-80 years
n = 48
Health Status: unhealthy
Condition: hypertension
Age Group: 21-80 years
Sex: M+F
Population Size: 48
Sources:
Other AEs: Arthralgia, Dizziness...
Other AEs:
Arthralgia (6%)
Dizziness (6%)
Leg cramps (6%)
Infection respiratory (13%)
Sinusitis (2%)
Nausea (4%)
Sources:
400 mg 1 times / day multiple, oral
Highest studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 21-80 years
n = 56
Health Status: unhealthy
Condition: hypertension
Age Group: 21-80 years
Sex: M+F
Population Size: 56
Sources:
Other AEs: Dizziness, Nausea...
Other AEs:
Dizziness (2%)
Nausea (5%)
Sources:
50 mg 1 times / day multiple, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
Other AEs: Palpitations, Diarrhoea...
Other AEs:
Palpitations (below serious, 1 patient)
Diarrhoea (below serious, 1 patient)
Fatigue (below serious, 2 patients)
Vessel puncture site reaction (below serious, 1 patient)
Fungal skin infection (below serious, 1 patient)
Nasopharyngitis (below serious, 3 patients)
Dizziness (below serious, 2 patients)
Headache (below serious, 5 patients)
Pollakiuria (below serious, 1 patient)
Sources:
AEs

AEs

AESignificanceDosePopulation
Infection respiratory 13%
200 mg 2 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources:
unhealthy, 21-80 years
n = 48
Health Status: unhealthy
Condition: hypertension
Age Group: 21-80 years
Sex: M+F
Population Size: 48
Sources:
Sinusitis 2%
200 mg 2 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources:
unhealthy, 21-80 years
n = 48
Health Status: unhealthy
Condition: hypertension
Age Group: 21-80 years
Sex: M+F
Population Size: 48
Sources:
Nausea 4%
200 mg 2 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources:
unhealthy, 21-80 years
n = 48
Health Status: unhealthy
Condition: hypertension
Age Group: 21-80 years
Sex: M+F
Population Size: 48
Sources:
Arthralgia 6%
200 mg 2 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources:
unhealthy, 21-80 years
n = 48
Health Status: unhealthy
Condition: hypertension
Age Group: 21-80 years
Sex: M+F
Population Size: 48
Sources:
Dizziness 6%
200 mg 2 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources:
unhealthy, 21-80 years
n = 48
Health Status: unhealthy
Condition: hypertension
Age Group: 21-80 years
Sex: M+F
Population Size: 48
Sources:
Leg cramps 6%
200 mg 2 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources:
unhealthy, 21-80 years
n = 48
Health Status: unhealthy
Condition: hypertension
Age Group: 21-80 years
Sex: M+F
Population Size: 48
Sources:
Dizziness 2%
400 mg 1 times / day multiple, oral
Highest studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 21-80 years
n = 56
Health Status: unhealthy
Condition: hypertension
Age Group: 21-80 years
Sex: M+F
Population Size: 56
Sources:
Nausea 5%
400 mg 1 times / day multiple, oral
Highest studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 21-80 years
n = 56
Health Status: unhealthy
Condition: hypertension
Age Group: 21-80 years
Sex: M+F
Population Size: 56
Sources:
Diarrhoea below serious, 1 patient
50 mg 1 times / day multiple, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
Fungal skin infection below serious, 1 patient
50 mg 1 times / day multiple, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
Palpitations below serious, 1 patient
50 mg 1 times / day multiple, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
Pollakiuria below serious, 1 patient
50 mg 1 times / day multiple, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
Vessel puncture site reaction below serious, 1 patient
50 mg 1 times / day multiple, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
Dizziness below serious, 2 patients
50 mg 1 times / day multiple, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
Fatigue below serious, 2 patients
50 mg 1 times / day multiple, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
Nasopharyngitis below serious, 3 patients
50 mg 1 times / day multiple, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
Headache below serious, 5 patients
50 mg 1 times / day multiple, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
Overview

OverviewOther

Other InhibitorOther SubstrateOther Inducer






Drug as perpetrator​Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
yes (co-administration study)
Comment: coadministered with ketoconazole increased elperenone AUC by 5.5-fold and Cmax by 1.7-fold and with erythromycin increased AUC by 1.8-fold and Cmax 61%
Page: 9, 10, 15
no
yes
yes (co-administration study)
Comment: coadminstration with fluconazole increased eplerenone AUC by 2.2-fold and Cmax by 1.4-fold
Page: 10.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Increased carotid wall elastic modulus and fibronectin in aldosterone-salt-treated rats: effects of eplerenone.
2002 Nov 26
Eplerenone: a new aldosterone receptor antagonist--are the FDAs restrictions appropriate?
2002 Nov-Dec
The role of aldosterone receptor blockade in the management of cardiovascular disease.
2002 Oct
Gateways to Clinical Trials.
2002 Sep
[Selective aldosterone blocker for hypertension and heart failure. Better tolerance than previous drugs].
2002 Sep 26
[Efficacy of an aldosterone receptor blocker eplerenone in high risk survivors of acute myocardial infarction with signs of heart failure: results of EPHESUS].
2003
Eplerenone, a new selective aldosterone blocker.
2003
Amiloride reduces stroke and renalinjury in stroke-prone hypertensive rats.
2003 Apr
Development and validation of a liquid chromatography-tandem mass spectrometric assay for Eplerenone and its hydrolyzed metabolite in human plasma.
2003 Apr 25
Eplerenone, a selective aldosterone blocker, in patients with left ventricular dysfunction after myocardial infarction.
2003 Apr 3
Aldosterone blockade and heart failure.
2003 Apr 3
Aldosterone receptor antagonists in the treatment of heart failure.
2003 Aug
Primary aldosteronism - treatment options.
2003 Aug
Selective aldosterone blockade with eplerenone in patients with congestive heart failure.
2003 Aug
Aldosterone blockade and vascular calcification in hemodialysis patients.
2003 Aug 15
Eplerenone: a selective aldosterone blocker.
2003 Fall
A validated SPE-LC-MS/MS assay for Eplerenone and its hydrolyzed metabolite in human urine.
2003 Feb 5
Assessment of the novel selective aldosterone blocker eplerenone using ambulatory and clinical blood pressure in patients with systemic hypertension.
2003 Jul 1
Transgenic model of aldosterone-driven cardiac hypertrophy and heart failure.
2003 Jul 11
Symptoms and the distress they cause: comparison of an aldosterone antagonist and a calcium channel blocking agent in patients with systolic hypertension.
2003 Jul 14
Eplerenone in patients with left ventricular dysfunction.
2003 Jul 3
Eplerenone in patients with left ventricular dysfunction.
2003 Jul 3
Eplerenone in patients with left ventricular dysfunction.
2003 Jul 3
[Anti-angiogenic effects of aldosterone antagonists in the fibrin chamber in rats].
2003 Jul-Aug
Hyperkalemia, congestive heart failure, and aldosterone receptor antagonism.
2003 Jul-Aug
Gateways to clinical trials.
2003 Jun
Late breaking heart failure trials from the 2003 ACC meeting: EPHESUS and COMPANION.
2003 Jun
Update of clinical trials from the American College of Cardiology 2003. EPHESUS, SPORTIF-III, ASCOT, COMPANION, UK-PACE and T-wave alternans.
2003 Jun
Aldosterone resurgens--letter from EPHESUS.
2003 Jun
Eplerenone. Pharmacia.
2003 Mar
Aldosterone as a target in congestive heart failure.
2003 Mar
Early inflammatory responses in experimental cardiac hypertrophy and fibrosis: effects of 11 beta-hydroxysteroid dehydrogenase inactivation.
2003 Mar
Aldosterone receptor blockade: a therapy resurrected.
2003 Mar-Apr
Aldosterone antagonism and hypertension.
2003 May
More hope for heart failure. Findings suggest expanded use of aldosterone-blockers.
2003 May
Eplerenone: cardiovascular protection.
2003 May 20
Aldosterone blockade in patients with acute myocardial infarction.
2003 May 27
Pharmacokinetics and metabolism of [14C]eplerenone after oral administration to humans.
2003 Nov
Can renin status predict the antihypertensive efficacy of eplerenone add-on therapy?
2003 Nov
Ask the doctor. I am a 50-year-old man with congestive heart failure. My doctor has me on all the usual drugs, and a couple of years ago added spironolactone. I did okay with it for a while, but then began to notice that my breasts were getting bigger and began to hurt. My doctor agreed that I should stop taking spironolactone, but I wonder if I am missing out on something.
2003 Oct
Aldosterone receptor blockade and the role of eplerenone: evolving perspectives.
2003 Oct
Two better than one.
2003 Oct 14
Aldosterone blockade in patients with systolic left ventricular dysfunction.
2003 Oct 14
Effects of eplerenone, enalapril, and eplerenone/enalapril in patients with essential hypertension and left ventricular hypertrophy: the 4E-left ventricular hypertrophy study.
2003 Oct 14
Long-term safety and efficacy of the selective aldosterone blocker eplerenone in patients with essential hypertension.
2003 Sep
Gateways to clinical trials.
2003 Sep
Should the aldosterone-receptor antagonist - eplerenone - be used after acute myocardial infarction with left ventricular dysfunction?
2003 Sep
New developments in the management of hypertension.
2003 Sep 1
Eplerenone: a selective aldosterone receptor antagonist for hypertension and heart failure.
2003 Sep-Oct
Adjunctive treatment with eplerenone reduced morbidity and mortality in acute myocardial infarction.
2003 Sep-Oct
Patents

Sample Use Guides

In Vivo Use Guide
Congestive heart failure post-myocardial infarction: Initial dosage: 25 mg orally once daily. Dosage should titrated to the target dose of 50 mg once daily preferably within 4 weeks. Usual Adult Dose for Hypertension 50 mg orally once daily. Patients with an inadequate blood pressure response should be increased to 50 mg twice a day.
Route of Administration: Oral
Eplerenone (10uM) significantly decreased corticosterone- (0.81 fold compared to treatment with corticosterone alone) and 11-DHC-driven (0.64 fold compared to treatment with 11-DHC alone) mouse VSMC calcification
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:06:14 UTC 2021
Edited
by admin
on Fri Jun 25 21:06:14 UTC 2021
Record UNII
6995V82D0B
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
EPLERENONE
HSDB   INN   JAN   MART.   MI   ORANGE BOOK   USAN   USP-RS   VANDF   WHO-DD  
INN   USAN  
Official Name English
EPLERENONE [WHO-DD]
Common Name English
EPLERENONE [JAN]
Common Name English
EPLERENONE [ORANGE BOOK]
Common Name English
INSPRA
Brand Name English
EPLERENONE [MI]
Common Name English
EPLERENONE [INN]
Common Name English
EPLERENONE [EP MONOGRAPH]
Common Name English
EPLERENONE [VANDF]
Common Name English
SC-66110
Code English
PREGN-4-ENE-7,21-DICARBOXYLIC ACID, 9,11-EPOXY-17-HYDROXY-3-OXO-, G-LACTONE, METHYL ESTER, (7.ALPHA.,11.ALPHA.,17.ALPHA)-
Common Name English
9,11.ALPHA.-EPOXY-17-HYDROXY-3-OXO-17.ALPHA.-PREGN-4-ENE-7.ALPHA.,21-DICARBOXYLIC ACID, .GAMMA.-LACTONE, METHYL ESTER
Common Name English
SC-6611O
Code English
EPLERENONE [MART.]
Common Name English
EPLERENONE [USP-RS]
Common Name English
EPLERENONE [HSDB]
Common Name English
EPLERENONE [USAN]
Common Name English
Classification Tree Code System Code
WHO-VATC QC03DA04
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
LIVERTOX 357
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
NCI_THESAURUS C270
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
WHO-ATC C03DA04
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
NDF-RT N0000175557
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
NDF-RT N0000011310
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
NCI_THESAURUS C843
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
Code System Code Type Description
EVMPD
SUB06574MIG
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
PRIMARY
PUBCHEM
443872
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
PRIMARY
INN
7596
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
PRIMARY
WIKIPEDIA
EPLERENONE
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
PRIMARY
DRUG CENTRAL
1032
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
PRIMARY
ChEMBL
CHEMBL1095097
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
PRIMARY
EPA CompTox
107724-20-9
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
PRIMARY
IUPHAR
2876
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
PRIMARY
RXCUI
298869
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
PRIMARY RxNorm
MERCK INDEX
M4951
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
PRIMARY Merck Index
HSDB
7522
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
PRIMARY
USP_CATALOG
1237553
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
PRIMARY USP-RS
MESH
C414690
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
PRIMARY
DRUG BANK
DB00700
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
PRIMARY
FDA UNII
6995V82D0B
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
PRIMARY
CAS
107724-20-9
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
PRIMARY
NCI_THESAURUS
C47513
Created by admin on Fri Jun 25 21:06:14 UTC 2021 , Edited by admin on Fri Jun 25 21:06:14 UTC 2021
PRIMARY
Related Record Type Details
EXCRETED UNCHANGED
FECAL; URINE
BINDER->LIGAND
BINDING
METABOLIC ENZYME -> SUBSTRATE
MAJOR
Related Record Type Details
METABOLITE -> PARENT
4% AUC; Primarily mediated via CYP3A4. No active metabolites of eplerenone have been identified in human plasma
MINOR
PLASMA
METABOLITE -> PARENT
Primarily mediated via CYP3A4. No active metabolites of eplerenone have been identified in human plasma
MINOR
FECAL; PLASMA; URINE
METABOLITE -> PARENT
Primarily mediated via CYP3A4. No active metabolites of eplerenone have been identified in human plasma
MAJOR
PLASMA; URINE
METABOLITE -> PARENT
Major in fecal and urine; Primarily mediated via CYP3A4. No active metabolites of eplerenone have been identified in human plasma
MAJOR
FECAL; PLASMA; URINE
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC ORAL ADMINISTRATION

Volume of Distribution PHARMACOKINETIC AT STEADY-STATE

Biological Half-life PHARMACOKINETIC