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
Inspra (generic drugs available since 2008-07-30)
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
Clinical Trials
136 clinical trials
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Indications Phases 4
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Hypertension | D006973 | EFO_0000537 | I10 | 4 | 6 | 4 | 14 | 8 | 36 |
| Heart failure | D006333 | HP_0001635 | I50 | 2 | 4 | 6 | 10 | 9 | 30 |
| Kidney diseases | D007674 | EFO_0003086 | N08 | 2 | 4 | 1 | 2 | — | 9 |
| Chronic renal insufficiency | D051436 | — | N18 | 1 | 4 | 1 | 2 | — | 8 |
| Essential hypertension | D000075222 | — | I10 | — | 3 | 2 | 1 | 2 | 8 |
| Hyperaldosteronism | D006929 | HP_0011736 | E26 | — | — | — | 3 | 5 | 8 |
| Central serous chorioretinopathy | D056833 | — | H35.71 | — | 3 | 1 | 2 | 3 | 8 |
| Myocardial infarction | D009203 | EFO_0000612 | I21 | — | 2 | 1 | 2 | 2 | 7 |
| Infarction | D007238 | EFO_0009463 | — | — | 2 | 1 | 2 | 2 | 7 |
| Diabetes mellitus | D003920 | HP_0000819 | E08-E13 | — | 2 | 1 | 2 | 2 | 7 |
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Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Kidney transplantation | D016030 | — | — | — | 1 | 1 | — | — | 2 |
| Hyperkalemia | D006947 | HP_0002153 | E87.5 | — | 1 | 1 | — | — | 2 |
| Duchenne muscular dystrophy | D020388 | EFO_0000429 | — | — | — | 1 | — | 1 | 2 |
| Muscular dystrophies | D009136 | HP_0003560 | G71.0 | — | — | 1 | — | 1 | 2 |
| Reperfusion injury | D015427 | — | — | — | — | 1 | — | 1 | 2 |
| Hyperparathyroidism | D006961 | EFO_0008506 | E21.3 | — | 1 | 1 | — | — | 1 |
| Primary hyperparathyroidism | D049950 | EFO_0008519 | E21.0 | — | 1 | 1 | — | — | 1 |
| Breast neoplasms | D001943 | EFO_0003869 | C50 | — | 1 | 1 | — | — | 1 |
| Glucose intolerance | D018149 | HP_0000833 | R73.03 | — | — | 1 | — | — | 1 |
| St elevation myocardial infarction | D000072657 | — | — | — | — | 1 | — | — | 1 |
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Diabetic nephropathies | D003928 | EFO_0000401 | — | 1 | 2 | — | — | 1 | 4 |
| Inferior wall myocardial infarction | D056989 | EFO_1000983 | — | — | 1 | — | — | 1 | 2 |
| Albuminuria | D000419 | EFO_0004285 | R80.9 | — | 1 | — | — | 1 | 2 |
| Wounds and injuries | D014947 | — | T14.8 | — | 1 | — | — | 1 | 2 |
| Gitelman syndrome | D053579 | Orphanet_358 | N15.8 | 1 | 1 | — | — | — | 1 |
| Liver cirrhosis | D008103 | EFO_0001422 | K74.0 | — | 1 | — | — | — | 1 |
| Ascites | D001201 | HP_0001541 | R18 | — | 1 | — | — | — | 1 |
| Papilledema | D010211 | EFO_1001074 | H35.81 | — | 1 | — | — | — | 1 |
| Hiv infections | D015658 | EFO_0000764 | B20 | — | 1 | — | — | — | 1 |
| Fatty liver | D005234 | EFO_0003934 | — | — | 1 | — | — | — | 1 |
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Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Healthy volunteers/patients | — | — | — | 6 | — | — | — | — | 6 |
| Pure autonomic failure | D054970 | — | — | 1 | — | — | — | — | 1 |
| Fasting | D005215 | EFO_0002756 | — | 1 | — | — | — | — | 1 |
| Pharmacokinetics | D010599 | — | — | 1 | — | — | — | — | 1 |
| Aortic valve stenosis | D001024 | HP_0001650 | — | 1 | — | — | — | — | 1 |
| Malnutrition | D044342 | EFO_0008572 | E40-E46 | 1 | — | — | — | — | 1 |
| Therapeutic equivalency | D013810 | — | — | 1 | — | — | — | — | 1 |
Indications Without Phase
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Adenoma | D000236 | — | — | — | — | — | — | 3 | 3 |
| Hiv | D006678 | — | — | — | — | — | — | 2 | 2 |
| Covid-19 | D000086382 | — | — | — | — | — | — | 1 | 1 |
| Vascular diseases | D014652 | EFO_0004264 | I77 | — | — | — | — | 1 | 1 |
| Hyperplasia | D006965 | EFO_0000536 | — | — | — | — | — | 1 | 1 |
| Congenital adrenal hyperplasia | D000312 | — | E25.0 | — | — | — | — | 1 | 1 |
| Adrenogenital syndrome | D047808 | — | E25.9 | — | — | — | — | 1 | 1 |
| Renal dialysis | D006435 | EFO_0010690 | Z99.2 | — | — | — | — | 1 | 1 |
| Hypoglycemia | D007003 | HP_0001943 | E16.2 | — | — | — | — | 1 | 1 |
| Adrenocortical adenoma | D018246 | — | — | — | — | — | — | 1 | 1 |
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Epidemiology
Epidemiological information for investigational and approved indications
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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
Variants
No data
Financial
Revenue by drug
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Inspra – Pfizer
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Estimated US medical usage
Eplerenone
Total medical expenditures per year (USD, in millions)
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Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 6,218 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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4,681 adverse events reported
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