Finerenone

Finerenone (INN, USAN) (developmental code name BAY-94-8862) is a nonsteroidal antimineralocorticoid that is in phase III clinical trials for the treatment of chronic heart failure as of October 2015. It has less relative affinity to other steroid hormone receptors than currently available antimineralocorticoids such as eplerenone and spironolactone, which should result in fewer adverse effects like gynaecomastia, impotence, and low libido Finerenone (INN, USAN) (developmental code name BAY-94-8862) is a nonsteroidal antimineralocorticoid that is in phase III clinical trials for the treatment of chronic heart failure as of October 2015. It has less relative affinity to other steroid hormone receptors than currently available antimineralocorticoids such as eplerenone and spironolactone, which should result in fewer adverse effects like gynaecomastia, impotence, and low libido Finerenone blocks mineralocorticoid receptors, which makes it a potassium-sparing diuretic. This table compares inhibitory (blocking) concentrations (IC50, unit: nM) of three antimineralocorticoids. Mineralocorticoid receptor inhibition is responsible for the desired action of the drugs, whereas inhibition of the other receptors potentially leads to side effects. Lower values mean stronger inhibition. The above-listed drugs have insignificant affinity for the estrogen receptor. Finerenone acts as an antagonist to mineralocorticoid receptors harboring the S810L mutation, unlike other traditional MR inhibitors such as spironolactone and eplerenone that incidentally act as agonists. Unlike currently marketed antimineralocorticoids, finerenone is not a steroid but a dihydropyridine derivative. The drug is also being investigated in early trials for the treatment of diabetic nephropathy.