Finerenone : third-generation mineralocorticoid receptor antagonist for the treatment of heart failure and diabetic kidney disease

Expert Opin Investig Drugs. 2015;24(8):1123-35. doi: 10.1517/13543784.2015.1059819. Epub 2015 Jun 20.

Abstract

Introduction: The mineralocorticoid receptor antagonists (MRAs) spironolactone and eplerenone reduce the risk of hospitalizations and mortality in patients with heart failure (HF) with reduced ejection fraction (HFrEF), and attenuate progression of diabetic kidney disease. However, their use is limited by the fear of inducing hyperkalemia, especially in patients with renal dysfunction. Finerenone is a novel nonsteroidal MRA, with higher selectivity toward the mineralocorticoid receptor (MR) compared to spironolactone and stronger MR-binding affinity than eplerenone.

Areas covered: This paper discusses the chemistry, pharmacokinetics, clinical efficacy and safety of finerenone.

Expert opinion: The selectivity and greater binding affinity of finerenone to the MR may reduce the risk of hyperkalemia and renal dysfunction and thereby overcome the reluctance to start and uptitrate MRAs in patients with HF and diabetic kidney disease. Studies conducted in patients with HFrEF and moderate chronic kidney disease and diabetic kidney disease, showed promising results. Phase III trials will have to show whether finerenone might become the third-generation MRA for the treatment of HF and diabetic kidney disease.

Keywords: BAY 94-8862; aldosterone; chronic kidney disease; diabetic kidney disease; diabetic nephropathy; finerenone; heart failure; nonsteroidal mineralocorticoid receptor antagonist.

Publication types

  • Review

MeSH terms

  • Animals
  • Diabetic Nephropathies / drug therapy*
  • Diabetic Nephropathies / physiopathology
  • Heart Failure / drug therapy*
  • Heart Failure / physiopathology
  • Hospitalization
  • Humans
  • Mineralocorticoid Receptor Antagonists / pharmacology
  • Mineralocorticoid Receptor Antagonists / therapeutic use
  • Naphthyridines / pharmacology
  • Naphthyridines / therapeutic use*

Substances

  • Mineralocorticoid Receptor Antagonists
  • Naphthyridines
  • finerenone