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

Details

Stereochemistry ABSOLUTE
Molecular Formula C24H30O6
Molecular Weight 414.4914
Optical Activity UNSPECIFIED
Defined Stereocenters 8 / 8
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of EPLERENONE

SMILES

[H][C@@]12C[C@@]3(C)[C@@]([H])(CC[C@@]34CCC(=O)O4)[C@]5([H])[C@@H](CC6=CC(=O)CC[C@]6(C)[C@@]15O2)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 414.4914
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 7 / 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

Novartis
173
Curator's Comment: # Novartis

Approval Year

2002
144
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2778
 122.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
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

2002
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2.49 μg/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/14570778
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
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/14570778
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
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/14570778
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%
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/14570778
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:
https://pubmed.ncbi.nlm.nih.gov/12160194
unhealthy, 21-80 years
n = 48
Health Status: unhealthy
Condition: hypertension
Age Group: 21-80 years
Sex: M+F
Population Size: 48
Sources:
https://pubmed.ncbi.nlm.nih.gov/12160194
Other AEs: Arthralgia, Dizziness...
Other AEs:
Arthralgia (6%)
Dizziness (6%)
Leg cramps (6%)
Infection respiratory (13%)
Sinusitis (2%)
Nausea (4%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/12160194
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:
https://pubmed.ncbi.nlm.nih.gov/12160194
unhealthy, 21-80 years
n = 56
Health Status: unhealthy
Condition: hypertension
Age Group: 21-80 years
Sex: M+F
Population Size: 56
Sources:
https://pubmed.ncbi.nlm.nih.gov/12160194
Other AEs: Dizziness, Nausea...
Other AEs:
Dizziness (2%)
Nausea (5%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/12160194
50 mg 1 times / day multiple, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01237899
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
https://clinicaltrials.gov/ct2/show/NCT01237899
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:
https://clinicaltrials.gov/ct2/show/NCT01237899
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:
https://pubmed.ncbi.nlm.nih.gov/12160194
unhealthy, 21-80 years
n = 48
Health Status: unhealthy
Condition: hypertension
Age Group: 21-80 years
Sex: M+F
Population Size: 48
Sources:
https://pubmed.ncbi.nlm.nih.gov/12160194
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:
https://pubmed.ncbi.nlm.nih.gov/12160194
unhealthy, 21-80 years
n = 48
Health Status: unhealthy
Condition: hypertension
Age Group: 21-80 years
Sex: M+F
Population Size: 48
Sources:
https://pubmed.ncbi.nlm.nih.gov/12160194
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:
https://pubmed.ncbi.nlm.nih.gov/12160194
unhealthy, 21-80 years
n = 48
Health Status: unhealthy
Condition: hypertension
Age Group: 21-80 years
Sex: M+F
Population Size: 48
Sources:
https://pubmed.ncbi.nlm.nih.gov/12160194
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:
https://pubmed.ncbi.nlm.nih.gov/12160194
unhealthy, 21-80 years
n = 48
Health Status: unhealthy
Condition: hypertension
Age Group: 21-80 years
Sex: M+F
Population Size: 48
Sources:
https://pubmed.ncbi.nlm.nih.gov/12160194
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:
https://pubmed.ncbi.nlm.nih.gov/12160194
unhealthy, 21-80 years
n = 48
Health Status: unhealthy
Condition: hypertension
Age Group: 21-80 years
Sex: M+F
Population Size: 48
Sources:
https://pubmed.ncbi.nlm.nih.gov/12160194
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:
https://pubmed.ncbi.nlm.nih.gov/12160194
unhealthy, 21-80 years
n = 48
Health Status: unhealthy
Condition: hypertension
Age Group: 21-80 years
Sex: M+F
Population Size: 48
Sources:
https://pubmed.ncbi.nlm.nih.gov/12160194
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:
https://pubmed.ncbi.nlm.nih.gov/12160194
unhealthy, 21-80 years
n = 56
Health Status: unhealthy
Condition: hypertension
Age Group: 21-80 years
Sex: M+F
Population Size: 56
Sources:
https://pubmed.ncbi.nlm.nih.gov/12160194
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:
https://pubmed.ncbi.nlm.nih.gov/12160194
unhealthy, 21-80 years
n = 56
Health Status: unhealthy
Condition: hypertension
Age Group: 21-80 years
Sex: M+F
Population Size: 56
Sources:
https://pubmed.ncbi.nlm.nih.gov/12160194
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:
https://clinicaltrials.gov/ct2/show/NCT01237899
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
https://clinicaltrials.gov/ct2/show/NCT01237899
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:
https://clinicaltrials.gov/ct2/show/NCT01237899
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
https://clinicaltrials.gov/ct2/show/NCT01237899
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:
https://clinicaltrials.gov/ct2/show/NCT01237899
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
https://clinicaltrials.gov/ct2/show/NCT01237899
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:
https://clinicaltrials.gov/ct2/show/NCT01237899
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
https://clinicaltrials.gov/ct2/show/NCT01237899
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:
https://clinicaltrials.gov/ct2/show/NCT01237899
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
https://clinicaltrials.gov/ct2/show/NCT01237899
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:
https://clinicaltrials.gov/ct2/show/NCT01237899
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
https://clinicaltrials.gov/ct2/show/NCT01237899
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:
https://clinicaltrials.gov/ct2/show/NCT01237899
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
https://clinicaltrials.gov/ct2/show/NCT01237899
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:
https://clinicaltrials.gov/ct2/show/NCT01237899
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
https://clinicaltrials.gov/ct2/show/NCT01237899
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:
https://clinicaltrials.gov/ct2/show/NCT01237899
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
https://clinicaltrials.gov/ct2/show/NCT01237899
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1737

inhibitor
1587

inducer
781
inhibitor
1767

substrate
1037
inhibitor
1852

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1524

CYP2C19
1478

P-gp
1461

CYP2E1
882
P-gp
1537
Cav1.2
4
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1692
 no [IC50 >300 uM]
CYP2C19
1553
 no [IC50 >300 uM]
CYP2C9
1819
 no [IC50 >300 uM]
CYP2D6
1891
 no [IC50 >300 uM]
CYP2E1
970
 no
CYP3A4
1925
 no
CYP3A4
1925
 no
P-gp
1650
 weak
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP3A4
1737
 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
P-gp
1537
 no
CYP2C9
1037
 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
Cav1.2
49
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:31547
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:31547
MolPort
MolPort-003-986-216
https://www.molport.com/shop/molecule-link/MolPort-003-986-216
Selleck Chemicals
Eplerenone(Inspra)
http://www.selleckchem.com/products/Eplerenone(Inspra).html
ZINC
ZINC000003985982
http://zinc15.docking.org/substances/ZINC000003985982
eMolecules
29539569
https://www.emolecules.com/cgi-bin/more?vid=29539569
eMolecules
32234158
https://www.emolecules.com/cgi-bin/more?vid=32234158
PubMed

PubMed

TitleDatePubMed
Mineralocorticoid and angiotensin receptor antagonism during hyperaldosteronemia.
2002 Aug
Efficacy of eplerenone added to renin-angiotensin blockade in hypertensive patients.
2002 Aug
Selective aldosterone blockade prevents angiotensin II/salt-induced vascular inflammation in the rat heart.
2002 Dec
Involvement of CYP3A in the metabolism of eplerenone in humans and dogs: differential metabolism by CYP3A4 and CYP3A5.
2002 Dec
Effects of long-term monotherapy with eplerenone, a novel aldosterone blocker, on progression of left ventricular dysfunction and remodeling in dogs with heart failure.
2002 Dec 3
Results from late-breaking clinical trial sessions at the American College of Cardiology 51st Annual Scientific Session.
2002 Jul 3
Interconversion pharmacokinetics of eplerenone, a selective aldosterone blocker, and its lactone-ring open form.
2002 Jun
Increased carotid wall elastic modulus and fibronectin in aldosterone-salt-treated rats: effects of eplerenone.
2002 Nov 26
The role of aldosterone receptor blockade in the management of cardiovascular disease.
2002 Oct
Aldosterone receptor antagonists for hypertension: what do they offer?
2003
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
[Aldosterone and its antagonists in heart failure].
2003 Jan 18
[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
Aldosterone resurgens--letter from EPHESUS.
2003 Jun
Eplerenone.
2003 Mar
Aldo is back: recent advances and unresolved controversies in hyperaldosteronism.
2003 Mar
Aldosterone antagonism and hypertension.
2003 May
New developments in the pharmacological treatment of chronic heart failure.
2003 May
Eplerenone: cardiovascular protection.
2003 May 20
RAAS escape: a real clinical entity that may be important in the progression of cardiovascular and renal disease.
2003 Oct
Long-term safety and efficacy of the selective aldosterone blocker eplerenone in patients with essential hypertension.
2003 Sep
New developments in the management of hypertension.
2003 Sep 1
Adjunctive treatment with eplerenone reduced morbidity and mortality in acute myocardial infarction.
2003 Sep-Oct
Aldosterone receptor antagonists: focus on eplerenone.
2003 Winter
Patents

Patents

07175854
29
07951398
20
JP2002538172A
25
JP2004507495A
2
JP2005527523A
6
JP2007016043A
1
JP2007210987A
1
JP2008100996A
1
JP2012500806A
10

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
In Vitro Use Guide
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 Dec 15 15:54:25 GMT 2023
Edited
by admin
on Fri Dec 15 15:54:25 GMT 2023
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 [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
9,11α-Epoxy-17-hydroxy-3-oxo-17α-pregn-4-ene-7α,21-dicarboxylic acid, γ-lactone, methyl ester
Common Name English
Eplerenone [WHO-DD]
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 Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
LIVERTOX NBK547930
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
NCI_THESAURUS C270
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
WHO-ATC C03DA04
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
NDF-RT N0000175557
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
NDF-RT N0000011310
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
NCI_THESAURUS C843
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
Code System Code Type Description
EVMPD
SUB06574MIG
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY
PUBCHEM
443872
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY
INN
7596
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY
WIKIPEDIA
EPLERENONE
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY
USAN
II-52
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY
DRUG CENTRAL
1032
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY
RS_ITEM_NUM
1237553
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY
ChEMBL
CHEMBL1095097
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY
EPA CompTox
DTXSID2046094
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY
IUPHAR
2876
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY
RXCUI
298869
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY RxNorm
MERCK INDEX
m4951
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY Merck Index
HSDB
7522
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY
CHEBI
31547
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY
MESH
C414690
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY
DAILYMED
6995V82D0B
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY
DRUG BANK
DB00700
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY
FDA UNII
6995V82D0B
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY
CAS
107724-20-9
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY
NCI_THESAURUS
C47513
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY
SMS_ID
100000092297
Created by admin on Fri Dec 15 15:54:25 GMT 2023 , Edited by admin on Fri Dec 15 15:54:25 GMT 2023
PRIMARY
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BINDER->LIGAND
BINDING
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Related Record Type Details
Structure of 6,15-DIHYDROXYEPLERENONE, (6.BETA.,15.ALPHA.)-
METABOLITE -> PARENT
MINOR
FECAL; URINE
Structure of SC-70303 FREE ACID
METABOLITE -> PARENT
MINOR
PLASMA
Structure of 3,6-DIHYDROXYEPLERENONE, (3.BETA.,6.BETA.)-
METABOLITE -> PARENT
MINOR
FECAL
Structure of 21-HYDROXYEPLERENONE
METABOLITE -> PARENT
Primarily mediated via CYP3A4. No active metabolites of eplerenone have been identified in human plasma
MINOR
FECAL; PLASMA; URINE
Structure of HYDROXYEPLERENONE, 6.BETA.-
METABOLITE -> PARENT
Primarily mediated via CYP3A4. No active metabolites of eplerenone have been identified in human plasma
MAJOR
PLASMA; URINE
Structure of 2,3,6-TRIHYDROXYEPLERENONE, (2.ALPHA.,3.BETA.,6.BETA.)-
METABOLITE -> PARENT
MINOR
FECAL
Structure of 3,6,21-TRIHYDROXYEPLERENONE, (3.ALPHA.,6.BETA.)-
METABOLITE -> PARENT
Primarily mediated via CYP3A4. No active metabolites of eplerenone have been identified in human plasma
MINOR
FECAL; URINE
Structure of 6,21-DIHYDROXYEPLERENONE, 6.BETA.-
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
Structure of 3,6,21-TRIHYDROXYEPLERENONE, (3.BETA.,6.BETA.)-
METABOLITE -> PARENT
Primarily mediated via CYP3A4. No active metabolites of eplerenone have been identified in human plasma
MINOR
FECAL
Structure of 3,6-DIHYDROXYEPLERENONE, (3.ALPHA.,6.BETA.)-
METABOLITE -> PARENT
Primarily mediated via CYP3A4. No active metabolites of eplerenone have been identified in human plasma
MINOR
FECAL; PLASMA; URINE
Related Record Type Details
Structure of 7.BETA.-EPLERENONE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
Structure of EPLERENONE 7-CARBOXYLIC ACID
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
Structure of SC-70303 FREE ACID
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
Structure of 11.ALPHA.,12.ALPHA.-EPOXY-7.ALPHA.-(METHOXYCARBONYL)-3-OXO-17.ALPHA.-PREGN-4-ENE-21,17-CARBOLACTONE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
Structure of MEXRENONE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
Structure of 7.ALPHA.-(METHOXYCARBONYL)-3-OXO-17.ALPHA.-PREGNA-4,9(11)-DIENE-21,17-CARBOLACTONE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
Structure of 3-OXO-17.ALPHA.-PREGN-4-ENE-7.ALPHA.,9:21,17-DICARBOLACTONE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
Related Record Type Details
Structure of EPLERENONE
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
NIH
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