Description
Finerenone is a novel mineralocorticoid receptor antagonist that has the effect of delaying the progression of chronic kidney disease. Some people may be aware of two other mineralocorticoid receptor antagonists: the diuretic antihypertensive drug spironolactone, and eplerenone.Finerenone is their cognate derivative and is a third-generation mineralocorticoid receptor antagonist. So far, finerenone is the only nonsteroidal mineralocorticoid receptor antagonist to be FDA approved. Finerenone was granted FDA approval on 9 July 2021, followed by the EMA approval on 11 March 2022.
Uses
Finerenone is the first non-steroidal selective mineralocorticoid receptor antagonist, which can be used for the treatment of diabetic nephropathy, chronic kidney disease and end-stage renal disease. It can reduce the proteinuria of patients and improve the glomerular filtration rate.
brand name
Finerenone is sold under the brand name Kerendia and Firialta.
Biological Activity
Finerenone (FIN, BAY 94-8862) is a highly selective, orally active, nonsteroidal antagonist of mineralocorticoid receptor (MR) with IC50 of 18 nM. Finerenone has the potential to study cardio-renal diseases such as type 2 diabetes and chronic kidney disease.
in vivo
Finerenone (BAY 94-8862) lowers albuminuria by >40% and significantly reduces systolic blood pressure (SBP) in Munich Wistar Fr?mter (MWF) rat.
Mode of action
Finerenone is a Nonsteroidal Mineralocorticoid-Receptor Antagonist. The mechanism of action of finerenone is as a Mineralocorticoid Receptor Antagonist. Finerenone inhibits the effects of mineralocorticoids like aldosterone and cortisol when the MR is overactivated, possibly reducing inflammation and fibrosis in the heart and kidney.
References
Kolkhof, P., Hartmann, E., Freyberger, A., et al.Effects of finerenone combined with empagliflozin in a model of hypertension-induced end-organ damage. Am. J. Nephrol. 52(8), 642-652 (2021).
DOI:
10.1159/000516213Cardiovascular Events with Finerenone in Kidney Disease and Type 2 Diabetes.
