A non-steroidal mineralocorticoid receptor antagonist
Finerenone is a non-steroidal mineralocorticoid receptor antagonist (IC50 = 18 nM).1 It is selective for the mineralocorticoid receptor over glucocorticoid, progesterone, and androgen receptors (IC50s = >10,000 nM for all), as well as L-type calcium channels (IC50 = >10,000 nM). Finerenone (3 mg/kg) reduces renal vasculopathy, fibrosis, and tubular degeneration, as well as cardiac fibrosis, in a rat model of hypertension-induced end-organ damage.2 It also increases exercise capacity and prevents diastolic dysfunction in ovariectomized mice.3
1.Kolkhof, P., Jaisser, F., Kim, S.-Y., et al.Steroidal and novel non-steroidal mineralocorticoid receptor antagonists in heart failure and cardiorenal diseases: Comparison at bench and bedsideHandb. Exp. Pharmacol.243271-305(2017) 2.Kolkhof, P., Hartmann, E., Freyberger, A., et al.Effects of finerenone combined with empagliflozin in a model of hypertension-induced end-organ damageAm. J. Nephrol.52(8)642-652(2021) 3.Pieronne-Deperrois, M., Guéret, A., Djerada, Z., et al.Mineralocorticoid receptor blockade with finerenone improves heart function and exercise capacity in ovariectomized miceESC Heart Fail.8(3)1933-1943(2021)
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