Eplerenone is an aldosterone receptor antagonist used to improve survival of patients with symptomatic heart failure and to reduce blood pressure. 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.
- Mechanism
- Curator reviewed
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.
- Primary 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.Curator reviewed · 3 structured indications
- Formula / weight
- C24H30O6 · 414.4914 g/mol (avg)
- First approval
- Canada, 2017 · United States, 2002
- Also known as
- Epoxymexrenone
- Code names
- SC-66110 · SC-6611O
- Brand names
Resolves to
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Which drugs share a target with Eplerenone, and which of those have an active Phase 3 trial?
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