FINERENONE Mineralocorticoid receptor (MR) antagonist Treatment of chronic kidney disease/diabetic nephropathy Treatment of heart failure

摘要

Targeting aldosterone via the mineralocorticoid receptor (MR) is a proven strategy for treating hypertension, heart failure and kidney disease, among other indications. Efforts to overcome the disadvantages of the established MR antagonists spironolactone and eplerenone, primarily hyperkalemia, led to the discovery of the nonsteroidal agent finerenone. Finerenone has greater MR potency than spironolactone and eplerenone and greater selectivity for the MR than spironolactone. Models of myocardial infarction, hypertension and renal injury encouraged further development of the compound, which went on to be studied in the ARTS series of clinical trials. Finerenone has demonstrated efficacy in these phase II studies in patients with heart failure and reduced left ventricular ejection fraction (HFrEF) associated with chronic kidney disease (CKD), patients with HFrEF with type 2 diabetes and/or CKD and in patients with diabetes and albuminuria. Phase III development has begun in patients with HFrEF and type 2 diabetes and/or CKD and in patients with diabetic kidney disease.