4.3 Review

The Time to Reconsider Mineralocorticoid Receptor Blocking Strategy: Arrival of Nonsteroidal Mineralocorticoid Receptor Blockers

Journal

CURRENT HYPERTENSION REPORTS
Volume 24, Issue 7, Pages 215-224

Publisher

SPRINGER
DOI: 10.1007/s11906-022-01177-6

Keywords

Esaxerenone; Finerenone; Nonsteroidal mineralocorticoid receptor blocker; Mineralocorticoid receptor; Hypertension

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This review explores the advantages of nonsteroidal mineralocorticoid receptor blockers (MRBs) in the management of hypertension and cardiovascular and renal diseases compared to conventional MRBs. The unique structures of nonsteroidal MRBs result in higher selectivity for mineralocorticoid receptors (MRs) and no agonist activity for major steroid hormone receptors. Clinical trials have shown that nonsteroidal MRBs achieve similar MR blockade with smaller doses and have fewer off-target side effects.
Purpose of Review The study aims to verify the advantages of nonsteroidal mineralocorticoid receptor blockers (MRBs) in the management of hypertension and cardiovascular and renal diseases, comparing with conventional MRBs. Recent Findings Based on the unique structures, the nonsteroidal MRBs have higher selectivity for mineralocorticoid receptors (MRs) and show no agonist activity for major steroid hormone receptors in contrast to steroidal MRBs. Today, there are two nonsteroidal MRBs, esaxerenone and finerenone, which completed phase 3 clinical trials. Series of clinical trials have shown that both agents achieve similar MR blockade with smaller doses as compared with steroidal MRBs, but have no off-target side effect such as gynecomastia. Esaxerenone has persistent blood pressure-lowering effects in various hypertensive populations, including essential hypertension and those with diabetes and/or chronic kidney disease, while finerenone has demonstrated reduction of the cardiovascular risk rather than blood pressure in patients with diabetes and chronic kidney disease. Nonsteroidal MRBs are a more refined agent which contributes to appropriate MR blocking with minimized unpleasant adverse effects.

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