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eplerenone
- Development stage
- Approved
- Lead developer
- Pfizer
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Eplerenone is a selective mineralocorticoid (aldosterone) receptor antagonist and potassium-sparing diuretic used to treat high blood pressure (hypertension) and heart failure, particularly after a heart attack. It works by blocking the action of aldosterone at the mineralocorticoid receptor in epithelial tissues such as the kidney, thereby reducing sodium reabsorption, decreasing blood volume, and lowering blood pressure. Eplerenone is more selective for the mineralocorticoid receptor than spironolactone and has fewer side effects related to sex hormone receptors. It was developed as an improvement over spironolactone to reduce adverse effects like gynecomastia while maintaining efficacy in cardiovascular conditions[1][2][3][5][6][8].
- Brand names
- Inspra
- Other names
- EpoxymexrenoneAldosterone antagonist
02
Targets
MR (Mineralocorticoid receptor)
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