TY - JOUR
T1 - Finerenone
T2 - third-generation mineralocorticoid receptor antagonist for the treatment of heart failure and diabetic kidney disease
AU - Liu, Licette C. Y.
AU - Schutte, Elise
AU - Gansevoort, Ron T.
AU - van der Meer, Peter
AU - Voors, Adriaan A.
PY - 2015/8
Y1 - 2015/8
N2 - 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 hyperkalennia, 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 Ill trials will have to show whether finerenone might become the third-generation MRA for the treatment of HF and diabetic kidney disease.
AB - 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 hyperkalennia, 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 Ill trials will have to show whether finerenone might become the third-generation MRA for the treatment of HF and diabetic kidney disease.
KW - aldosterone
KW - BAY 94-8862
KW - chronic kidney disease
KW - diabetic kidney disease
KW - diabetic nephropathy
KW - finerenone
KW - heart failure
KW - nonsteroidal mineralocorticoid receptor antagonist
KW - CONVERTING ENZYME-INHIBITOR
KW - ANGIOTENSIN-ALDOSTERONE SYSTEM
KW - MILD PATIENTS HOSPITALIZATION
KW - LEFT-VENTRICULAR DYSFUNCTION
KW - ACUTE MYOCARDIAL-INFARCTION
KW - GLOMERULAR-FILTRATION-RATE
KW - WORSENING RENAL-FUNCTION
KW - DOUBLE-BLIND
KW - EMPHASIS-HF
U2 - 10.1517/13543784.2015.1059819
DO - 10.1517/13543784.2015.1059819
M3 - Article
VL - 24
SP - 1123
EP - 1135
JO - Expert opinion on investigational drugs
JF - Expert opinion on investigational drugs
SN - 1354-3784
IS - 8
ER -