Eplerenone

Aldosterone Antagonist — CARDIOVASCULAR SYSTEM

Key facts

Eplerenone is an ofp drug in the Aldosterone Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 2002. Its mechanism of action is classified as Aldosterone Antagonists. DrugCentral lists 5 molecular targets, including Nr3c2, NR3C2 and AR. Recorded indications include Chronic Heart Failure Following Myocardial Infarction and Hypertensive disorder.

• Approval status: ofp (first approved 2002 by the FDA).
• Drug class: Aldosterone Antagonist.
• Mechanism of action: Aldosterone Antagonists.
• Molecular targets: Nr3c2, NR3C2, AR and NR3C1 (5 listed in DrugCentral).
• Indications: Chronic Heart Failure Following Myocardial Infarction and Hypertensive disorder.
• ATC code: C03DA04 (Aldosterone antagonists).
• Molecular formula: C24H30O6; molecular weight 414.50 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• Chronic Heart Failure Following Myocardial Infarction
• Hypertensive disorder

Contraindications (4)

• Diabetic renal disease
• Disease of liver
• Hyperkalemia
• Impaired renal function disorder

Mechanism & targets

• Mechanism of action (MoA): Aldosterone Antagonists
• Established pharmacologic class: Aldosterone Antagonist

Molecular targets (5)

Target	Gene	Action	Activity
Mineralocorticoid receptor	Nr3c2	unknown	IC50 7.40
Mineralocorticoid receptor	NR3C2	antagonist	IC50 7.00
Androgen receptor	AR	unknown	IC50 4.77
Glucocorticoid receptor	NR3C1	unknown	IC50 4.74
Progesterone receptor	PGR	unknown	Ki 4.70

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2002-09-27	FDA	—	GD SEARLE LLC

ATC classification

ATC code	Therapeutic hierarchy
C03DA04	CARDIOVASCULAR SYSTEM › DIURETICS › ALDOSTERONE ANTAGONISTS AND OTHER POTASSIUM-SPARING AGENTS › Aldosterone antagonists
C03DA54	CARDIOVASCULAR SYSTEM › DIURETICS › ALDOSTERONE ANTAGONISTS AND OTHER POTASSIUM-SPARING AGENTS › Aldosterone antagonists

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Cardiac failure	1282.5
Acute kidney injury	825.7
Cardiac failure chronic	718.5
Hyperkalaemia	539.1
Hypotension	514.4
Ventricular tachycardia	407.9
Ejection fraction decreased	314.2
Oedema peripheral	310.7
Atrial fibrillation	300.9
Rales	271.8
N-terminal prohormone brain natriuretic peptide increased	264.1
Mitral valve incompetence	259.9

Chemical structure

• Molecular formula: C₂₄H₃₀O₆
• Molecular weight: 414.50 g/mol
• CAS number: 107724-20-9
• InChIKey: JUKPWJGBANNWMW-VWBFHTRKSA-N
• PubChem CID: 443872

COC(=O)[C@@H]1CC2=CC(=O)CC[C@]2(C)[C@@]23O[C@@H]2C[C@@]2(C)[C@@H](CC[C@@]22CCC(=O)O2)[C@H]13

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Eplerenone used for?

DrugCentral lists the following indications for Eplerenone: Chronic Heart Failure Following Myocardial Infarction and Hypertensive disorder.

How does Eplerenone work?

Eplerenone is classified as Aldosterone Antagonists; its molecular targets in DrugCentral include Nr3c2, NR3C2 (antagonist), AR and NR3C1.

When was Eplerenone first approved?

Eplerenone was first approved by the FDA in 2002.

What drug class does Eplerenone belong to?

Eplerenone is in the Aldosterone Antagonist class.

What is the chemical formula of Eplerenone?

Eplerenone has the molecular formula C24H30O6 and a molecular weight of 414.50 g/mol.

Sources

• DrugCentral drug card 1032 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1095097 — compound record and bioactivity
• PubChem CID 443872 — chemical identifiers
• DrugBank DB00700 — drug record
• FDA UNII 6995V82D0B — substance identity
• DailyMed: FDA labels for Eplerenone — current prescribing information (label search)
• UniProt P08235 (NR3C2) — target protein
• UniProt P10275 (AR) — target protein
• UniProt P04150 (NR3C1) — target protein
• UniProt P06401 (PGR) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.