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eplerenone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
mineralocorticoid receptor (MR, MCR, aldosterone receptor) antagonists	1032	107724-20-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: eplerenone (+)-Eplerenone epoxymexrenone	A spironolactone derivative and selective ALDOSTERONE RECEPTOR antagonist that is used in the management of HYPERTENSION and CONGESTIVE HEART FAILURE, post-MYOCARDIAL INFARCTION. Molecular weight: 414.50 Formula: C24H30O6 CLOGP: 0.47 LIPINSKI: 0 HAC: 6 HDO: 0 TPSA: 82.20 ALOGS: -4.66 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

eplerenone
(+)-Eplerenone
epoxymexrenone

A spironolactone derivative and selective ALDOSTERONE RECEPTOR antagonist that is used in the management of HYPERTENSION and CONGESTIVE HEART FAILURE, post-MYOCARDIAL INFARCTION.

Molecular weight: 414.50
Formula: C24H30O6
CLOGP: 0.47
LIPINSKI: 0
HAC: 6
HDO: 0
TPSA: 82.20
ALOGS: -4.66
ROTB: 2

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
50	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	69 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	3 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.72 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
Sept. 27, 2002	FDA	GD SEARLE LLC

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Cardiac failure	206.27	21.36	119	5843	89023	63394037
Hyperkalaemia	162.77	21.36	86	5876	54117	63428943
Acute kidney injury	157.49	21.36	156	5806	263259	63219801
Cardiac failure chronic	103.22	21.36	31	5931	4387	63478673
Subclavian vein thrombosis	79.46	21.36	21	5941	1869	63481191
Drug interaction	75.67	21.36	100	5862	229031	63254029
Atrial fibrillation	72.96	21.36	71	5891	116565	63366495
Hypotension	69.33	21.36	105	5857	272499	63210561
Cardiomyopathy	52.97	21.36	28	5934	17556	63465504
Hyponatraemia	51.78	21.36	58	5904	111842	63371218

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Cardiac failure	643.22	15.57	519	23594	90729	34842089
Cardiac failure chronic	380.34	15.57	158	23955	7721	34925097
Rales	257.43	15.57	129	23984	9754	34923064
Ventricular tachycardia	256.93	15.57	183	23930	26396	34906422
Acute kidney injury	232.87	15.57	591	23522	304397	34628421
Ejection fraction decreased	218.34	15.57	146	23967	19008	34913810
Oedema peripheral	213.62	15.57	332	23781	119480	34813338
N-terminal prohormone brain natriuretic peptide increased	203.74	15.57	75	24038	2640	34930178
Hypotension	182.94	15.57	443	23670	221206	34711612
Mitral valve incompetence	182.66	15.57	119	23994	14824	34917994

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Cardiac failure	889.80	16.54	593	27086	154249	79562460
Cardiac failure chronic	519.66	16.54	181	27498	10954	79705755
Acute kidney injury	466.83	16.54	723	26956	518681	79198028
Hyperkalaemia	349.65	16.54	301	27378	114097	79602612
Ventricular tachycardia	302.98	16.54	186	27493	41749	79674960
Hypotension	265.86	16.54	515	27164	439802	79276907
Rales	261.04	16.54	131	27548	19870	79696839
Oedema peripheral	252.22	16.54	370	27309	251918	79464791
Ejection fraction decreased	236.14	16.54	148	27531	34429	79682280
N-terminal prohormone brain natriuretic peptide increased	209.17	16.54	74	27605	4681	79712028

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C03DA04	CARDIOVASCULAR SYSTEM DIURETICS ALDOSTERONE ANTAGONISTS AND OTHER POTASSIUM-SPARING AGENTS Aldosterone antagonists
CHEBI has role	CHEBI:35674	antihypertensive drugs
FDA EPC	N0000175557	Aldosterone Antagonist
FDA MoA	N0000011310	Aldosterone Antagonists
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D004232	Diuretics
MeSH PA	D006727	Hormone Antagonists
MeSH PA	D000451	Mineralocorticoid Receptor Antagonists
MeSH PA	D045283	Natriuretic Agents

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Hypertensive disorder	indication	38341003	DOID:10763
Chronic Heart Failure Following Myocardial Infarction	indication
Hyperkalemia	contraindication	14140009
Diabetic renal disease	contraindication	127013003
Impaired renal function disorder	contraindication	197663003
Disease of liver	contraindication	235856003	DOID:409

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🐶 Veterinary Drug Use

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🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

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Orange Book patent data (new drug applications)

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Orange Book exclusivity data (new drug applications)

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Mineralocorticoid receptor	Nuclear hormone receptor	P08235	MCR_HUMAN	ANTAGONIST	IC50	7	WOMBAT-PK	CHEMBL
Glucocorticoid receptor	Nuclear hormone receptor	P04150	GCR_HUMAN		IC50	4.74	CHEMBL
Androgen receptor	Nuclear hormone receptor	P10275	ANDR_HUMAN		IC50	4.77	CHEMBL
Progesterone receptor	Nuclear hormone receptor	P06401	PRGR_HUMAN		Ki	4.70	CHEMBL
Mineralocorticoid receptor	Transcription factor		MCR_RAT		IC50	7.40	CHEMBL

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External reference:

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ID	Source
YNU	PDB_CHEM_ID
009774	NDDF
147386	MMSL
16969	MMSL
2876	IUPHAR_LIGAND_ID
298869	RXNORM
398699008	SNOMEDCT_US
4021363	VUID
4021363	VANDF
407010008	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Eplerenone	HUMAN PRESCRIPTION DRUG LABEL	1	0185-5368	TABLET	25 mg	ORAL	ANDA	25 sections
Eplerenone	HUMAN PRESCRIPTION DRUG LABEL	1	0185-5368	TABLET	25 mg	ORAL	ANDA	25 sections
Eplerenone	HUMAN PRESCRIPTION DRUG LABEL	1	0185-5369	TABLET	50 mg	ORAL	ANDA	25 sections
Eplerenone	HUMAN PRESCRIPTION DRUG LABEL	1	0185-5369	TABLET	50 mg	ORAL	ANDA	25 sections
Eplerenone	HUMAN PRESCRIPTION DRUG LABEL	1	0378-1030	TABLET, FILM COATED	25 mg	ORAL	ANDA	27 sections
Eplerenone	HUMAN PRESCRIPTION DRUG LABEL	1	0378-1030	TABLET, FILM COATED	25 mg	ORAL	ANDA	27 sections
Eplerenone	HUMAN PRESCRIPTION DRUG LABEL	1	0378-1031	TABLET, FILM COATED	50 mg	ORAL	ANDA	27 sections
Eplerenone	HUMAN PRESCRIPTION DRUG LABEL	1	0378-1031	TABLET, FILM COATED	50 mg	ORAL	ANDA	27 sections
Eplerenone	HUMAN PRESCRIPTION DRUG LABEL	1	16729-293	TABLET, FILM COATED	25 mg	ORAL	ANDA	26 sections
Eplerenone	HUMAN PRESCRIPTION DRUG LABEL	1	16729-294	TABLET, FILM COATED	50 mg	ORAL	ANDA	26 sections

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