Third-generation Mineralocorticoid Receptor Antagonists: Why Do We Need a Fourth?

ABSTRACT: The first mineralocorticoid receptor (MR) antagonist, spironolactone, was developed almost 60 years ago to treat primary aldosteronism and pathological edema. Its use waned in part because of its lack of selectivity. Subsequently, knowledge of the scope of MR function was expanded along with clinical evidence of the therapeutic importance of MR antagonists to prevent the ravages of inappropriate MR activation. Forty-two years elapsed between the first and MR-selective second generation of MR antagonists. Fifteen years later, despite serious shortcomings of the existing antagonists, a third-generation antagonist has yet to be marketed. Progress has been slowed by the lack of appreciation of the large variety of cell types that express the MR and its diverse cell-type-specific actions, and a

SUBMITTER: Gomez-Sanchez EP 

PROVIDER: S-EPMC4703541 | biostudies-literature | 2016 Jan

REPOSITORIES: biostudies-literature