Is there a new dawn for selective mineralocorticoid receptor antagonism?

Luther JM
Curr Opin Nephrol Hypertens. 2014 23 (5): 456-61

PMID: 24992570 · PMCID: PMC4248353 · DOI:10.1097/MNH.0000000000000051

PURPOSE OF REVIEW - Aldosterone and the mineralocorticoid receptor contribute to resistant hypertension and cardiovascular mortality, and mineralocorticoid receptor antagonists effectively reduce these complications. Their use is limited in certain populations with a higher risk of hyperkalemia or renal dysfunction. This review will highlight recent developments in extra-renal mineralocorticoid receptor research and the development of novel mineralocorticoid receptor antagonists.

RECENT FINDINGS - Tissue-specific knockout-out models provide definitive evidence that the vascular mineralocorticoid receptor directly contributes to hypertension and vascular remodeling, independent of renal effects. Several nonsteroidal mineralocorticoid receptor antagonists are in preclinical development or early-stage clinical trials. Several nonsteroidal mineralocorticoid receptor antagonists have demonstrated preserved cardiovascular benefit with a reduced incidence of hyperkalemia in preclinical studies.

SUMMARY - Novel, potent nonsteroidal mineralocorticoid receptor antagonists are in development, although their effect on cardiovascular and adverse drug events requires further investigation.

MeSH Terms (13)

Animals Antihypertensive Agents Blood Pressure Blood Vessels Drug Design Humans Hyperkalemia Hypertension Mineralocorticoid Receptor Antagonists Receptors, Mineralocorticoid Risk Factors Signal Transduction Treatment Outcome

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