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

被引:65
作者
Liu, Licette C. Y. [1 ]
Schutte, Elise [2 ]
Gansevoort, Ron T. [2 ]
van der Meer, Peter [1 ]
Voors, Adriaan A. [3 ]
机构
[1] Univ Groningen, Univ Med Ctr Groningen, Dept Cardiol, NL-9713 GZ Groningen, Netherlands
[2] Univ Groningen, Univ Med Ctr Groningen, Dept Nephrol, NL-9713 GZ Groningen, Netherlands
[3] Univ Groningen, Univ Med Ctr Groningen, Dept Cardiol, Cardiol, NL-9713 GZ Groningen, Netherlands
关键词
aldosterone; BAY; 94-8862; chronic kidney disease; diabetic kidney disease; diabetic nephropathy; finerenone; heart failure; nonsteroidal mineralocorticoid receptor antagonist; CONVERTING ENZYME-INHIBITOR; ANGIOTENSIN-ALDOSTERONE SYSTEM; MILD PATIENTS HOSPITALIZATION; LEFT-VENTRICULAR DYSFUNCTION; ACUTE MYOCARDIAL-INFARCTION; GLOMERULAR-FILTRATION-RATE; WORSENING RENAL-FUNCTION; DOUBLE-BLIND; EMPHASIS-HF; BAY; 94-8862;
D O I
10.1517/13543784.2015.1059819
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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.
引用
收藏
页码:1123 / 1135
页数:13
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