Abstract
Finerenone is a novel non-steroidal mineralocorticoid receptor antagonist (MRA) with high selectivity and affinity to mineralocorticoid receptor (MR). Steroidal MRAs, like spironolactone and eplerenone, have been in use for decades. They have an established position in the management of hypertension and heart failure with reduced ejection fraction (HFrEF). There are studies showing that MR antagonism has anti-inflammatory and anti-fibrotic effects resulting in cardiovascular and renal protection. However, broader use of steroidal MRAs is seriously limited by antiandrogenic side effects and the risk of hyperkalemia. The differences in structure as well as pharmacokinetic and pharmacodynamic properties between steroidal and non-steroidal MRAs result in reduced risk of side effects while offering the benefit of cardiorenal protection. Finerenone is currently the only non-steroidal MRA approved by European Medicines Agency (EMA). It is indicated for patients with chronic kidney disease (CKD) with albuminuria and type 2 diabetes mellitus (DM2). Several studies showed a reduction of the risk of cardiovascular and renal events in this group of patients compared to placebo. The risk of hyperkalemia was increased resulting in discontinuation of treatment in more patients than placebo, but the risk of serious adverse events did not differ significantly. The other indications for finerenone, including heart failure (HF) management, are currently being researched.
Publisher
Warszawski Uniwersytet Medyczny
Reference47 articles.
1. Kolkhof, P.; Barfacker, L. 30 YEARS OF THE MINERALOCORTICOID RECEPTOR: Mineralocorticoid receptor antagonists: 60 years of research and development. J. Endocrinol. 2017, 234 (1), T125-T140. DOI: 10.1530/JOE-16-0600
2. Funder, J. W. Mineralocorticoid receptor antagonists: emerging roles in cardiovascular medicine. Integr. Blood Press. Control 2013, 6, 129-138. DOI: 10.2147/IBPC.S13783
3. Williams, B.; Mancia, G.; et al. 2018 ESC/ESH Guidelines for the management of arterial hypertension. Eur. Heart J. 2018, 39 (33), 3021-3104. DOI: 10.1093/eurheartj/ehy339
4. PubChem Compound Summary for CID 5833, Spironolactone. National Center for Biotechnology Information. https://pubchem.ncbi.nlm.nih.gov/compound/Spironolactone (accessed 2023 December 5th).
5. Delyani, J. A. Mineralocorticoid receptor antagonists: the evolution of utility and pharmacology. Kidney Int. 2000, 57 (4), 1408-1411. DOI: 10.1046/j.1523-1755.2000.00983.x