Mineralocorticoid receptor

Class

Non-steroidal mineralocorticoid receptor antagonist

The mineralocorticoid receptor (MR) is a hormone-activated protein that, when bound by the hormone aldosterone, moves into the cell nucleus and switches on genes controlling sodium retention and potassium excretion, chiefly in the kidney. This regulation is central to blood pressure and fluid balance, but sustained overactivation of the MR pathway also drives fibrosis and inflammation in the heart, blood vessels, and kidney. Blocking the receptor with an antagonist reduces sodium and fluid retention and limits this tissue damage, which is why MR antagonism is relevant across hypertension, heart failure, and chronic kidney disease, particularly when these conditions occur together, as in diabetic kidney disease. Older MR antagonists are steroid-based molecules that also interact with related hormone receptors, causing hormonal side effects. Non-steroidal MR antagonists, a newer chemical class, are designed to bind the receptor with a different molecular shape, aiming to preserve the beneficial blockade of sodium retention and tissue injury while reducing interaction with unrelated steroid receptors and altering the balance of effects on the heart and kidney compared with older agents.