Finerenone
Finerenone is a nonsteroidal antimineralocorticoid that is in phase III clinical trials for the treatment of chronic kidney disease in people with type II diabetes. 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.
Pharmacology
Finerenone blocks mineralocorticoid receptors, which makes it a potassium-sparing diuretic.This table compares inhibitory concentrations 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.
Spironolactone | Eplerenone | Finerenone | |
Mineralocorticoid receptor | 24 | 990 | 18 |
Glucocorticoid receptor | 2400 | 22,000 | >10,000 |
Androgen receptor | 77 | 21,200 | >10,000 |
Progesterone receptor | 740 | 31,200 | >10,000 |
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.