Eplerenone
Eplerenone, Inspra (eplerenone) is a small molecule pharmaceutical. Eplerenone was first approved as Inspra on 2002-09-27. It is used to treat hypertension and systolic heart failure in the USA. The pharmaceutical is active against mineralocorticoid receptor.
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Commercial
Therapeutic Areas
Therapeutic Area | MeSH |
|---|---|
| cardiovascular diseases | D002318 |
Trade Name
FDA
EMA
Eplerenone, Inspra (discontinued: Eplerenone, Inspra)
Labels
FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| eplerenone | ANDA | 2024-08-23 |
| inspra | New Drug Application | 2023-07-18 |
Indications
FDA
EMA
Indication | Ontology | MeSH | ICD-10 |
|---|---|---|---|
| systolic heart failure | EFO_1001207 | D054143 | I50.20 |
| hypertension | EFO_0000537 | D006973 | I10 |
Agency Specific
FDA
EMA
No data
Patent Expiration
No data
HCPCS
No data
Clinical
No data
Drug
General
| Drug common name | Eplerenone |
| INN | eplerenone |
| Description | Eplerenone, sold under the brand name Inspra, is an aldosterone antagonist type of potassium-sparing diuretic that is used to treat chronic heart failure and high blood pressure, particularly for patients with resistant hypertension due to elevated aldosterone. It is a steroidal antimineralocorticoid of the spirolactone group and a selective aldosterone receptor antagonist (SARA). Eplerenone is more selective than spironolactone at the mineralocorticoid receptor relative to binding at androgen, progestogen, glucocorticoid, or estrogen receptors.
|
| Classification | Small molecule |
| Drug class | aldosterone antagonists (spironolactone type) |
| Image (chem structure or protein) |  |
| Structure (InChI/SMILES or Protein Sequence) | COC(=O)[C@@H]1CC2=CC(=O)CC[C@]2(C)[C@@]23O[C@@H]2C[C@@]2(C)[C@@H](CC[C@@]24CCC(=O)O4)[C@H]13 |
Identifiers
| PDB | — |
| CAS-ID | 107724-20-9 |
| RxCUI | — |
| ChEMBL ID | CHEMBL1095097 |
| ChEBI ID | 31547 |
| PubChem CID | 5282131 |
| DrugBank | DB00700 |
| UNII ID | 6995V82D0B (ChemIDplus, GSRS) |
Target
Agency Approved
NR3C2
NR3C2
Organism
Homo sapiens
Gene name
NR3C2
Gene synonyms
MCR, MLR
NCBI Gene ID
Protein name
mineralocorticoid receptor
Protein synonyms
aldosterone receptor, mineralocorticoid receptor 1, mineralocorticoid receptor 2, mineralocorticoid receptor delta, Nuclear receptor subfamily 3 group C member 2
Uniprot ID
Mouse ortholog
Nr3c2 (110784)
mineralocorticoid receptor (Q8VII9)
Alternate
No data
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Financial
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Inspra – Pfizer
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Eplerenone
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Safety
Black-box Warning
No Black-box warning
Adverse Events
0 adverse events reported
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