Investigational Drug Details
| Drug ID: | D200 |
| Drug Name: | Eplerenone |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB00700 |
| DrugBank Description: | 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. |
| PubChem ID: | 443872 |
| CasNo: | 107724-20-9 |
| Repositioning for NAFLD: | Yes |
| SMILES: | [H][C@@]12CC[C@@]3(CCC(=O)O3)[C@@]1(C)C[C@H]1O[C@@]11[C@@]2([H])[C@@H](CC2=CC(=O)CC[C@]12C)C(=O)OC |
| Structure: |
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| InChiKey: | JUKPWJGBANNWMW-VWBFHTRKSA-N |
| Molecular Weight: | 414.4914 |
| DrugBank Targets: | Mineralocorticoid receptor |
| DrugBank MoA: | 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. |
| DrugBank Pharmacology: | 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. |
| DrugBank Indication: | 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. |
| Targets: | |
| Therapeutic Category: | |
| Clinical Trial Progress: | |
| Latest Progress: |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0619 | NCT02841280 | PHASE2 | COMPLETED | YES | 2016-07 | 2023-05-15 | Details |
| L0663 | NCT00680043 | PHASE2 | COMPLETED | YES | 2008-06 | 2012-06-29 | Details |
| L0819 | NCT04397653 | PHASE4 | UNKNOWN | NO | 2020-05-04 | 2020-05-26 | Details |
| L0849 | NCT00503698 | PHASE3 | TERMINATED | YES | 2007-07 | 2017-03-07 | Details |
| L1159 | NCT00977080 | PHASE4 | COMPLETED | YES | 2009-11 | 2012-06-20 | Details |
| L2301 | NCT01492465 | PHASE1 | TERMINATED | NO | 2011-11 | 2013-02-15 | Details |
| L2933 | NCT03414892 | PHASE1 | COMPLETED | NO | 2018-01-03 | 2020-01-03 | Details |
| L3984 | NCT01368081 | PHASE3 | COMPLETED | YES | 2011-05 | 2014-06-17 | Details |
| L4043 | NCT04242758 | PHASE4 | UNKNOWN | NO | 2019-06-04 | 2020-01-27 | Details |
| L4280 | NCT01223196 | PHASE4 | COMPLETED | YES | 2009-08 | 2016-01-11 | Details |
| L5007 | NCT00743002 | PHASE2 | COMPLETED | NO | 2008-08 | 2013-06-21 | Details |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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| Article ID | PMID | Source | Title |
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