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Mineralocorticoid receptor antagonists have evolved to treat hypertension, heart failure, and kidney diseases, though steroidal MRAs are associated with hyperkalemia and endocrine abnormalities.
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This review summarizes the historical development, clinical applications, and future prospects of mineralocorticoid receptor antagonists in cardiovascular and kidney diseases.
Mineralocorticoid receptor antagonists (MRAs) have significantly evolved since the introduction of the first steroidal MRA, spironolactone, in the 1950s. Initially discovered for treating hypertension and heart failure (HF), the clinical applications of MRAs have been expanded to chronic kidney disease (CKD) and diabetic nephropathy. Steroidal MRAs, such as spironolactone and eplerenone, effectively suppress mineralocorticoid receptor activation but are associated with side effects like hyperkalemia and endocrine abnormalities. Current research aims to optimize MRAs further for broader therapeutic applications, including nondiabetic kidney and cardiovascular diseases, and to improve safety profiles. In this review, we reflect on the historical development, classification, evolution, major clinical trials, and future prospects of MRAs.
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Kalmath et al. (2026) conducted a review in Hypertension, heart failure, chronic kidney disease, and diabetic nephropathy. Mineralocorticoid receptor antagonists (MRAs) was evaluated. Mineralocorticoid receptor antagonists have evolved to treat hypertension, heart failure, and kidney diseases, though steroidal MRAs are associated with hyperkalemia and endocrine abnormalities.
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