Finerenone (For research purpose only) 1050477-31-0

Fenalidone is a novel mineralocorticoid receptor antagonist that has the effect of delaying the progression of chronic kidney disease. Some people may know about two other mineralocorticoid receptor antagonists: the diuretic antihypertensive drug spironolactone and eplerenone. And not Nalidone is their sibling, the third generation mineralocorticoid receptor antagonist that has just emerged after the two. The mechanism of action of mineralocorticoid receptors is one of the reasons for the elevation of urinary protein and deterioration of renal function. The mineralocorticoid receptor can be over activated by the increase of aldosterone, causing sodium retention, raising blood pressure, promoting renal inflammation, and accelerating renal fibrosis (renal failure). Antagonism of mineralocorticoid receptors to improve inflammation and fibrosis has been a key therapeutic target in the field of nephrology in recent years, and not the first true breakthrough has been achieved with nalide. Use Feneridone is the first non steroidal selective mineralocorticoid receptor antagonist, which can be used for the treatment of diabetes nephropathy, chronic nephropathy and end-stage renal disease, and can reduce proteinuria in patients and improve glomerular filtration rate. Finerenone (FIN, BAY94-8862) is a highly selective, orally active nonsteroidal antagonist of mineralocorticoid receptor (MR) with an IC50 value of 18 nM. Finerenone has the potential to study cardiorenal diseases such as type 2 diabetes and chronic kidney disease.

In July 2021, based on the positive results of the FIDELIO-DKD Phase III clinical study in adult patients with chronic kidney disease and type 2 diabetes, the US FDA approved the listing of fenelione. The application for listing of fenelione has been submitted in China and many other countries and regions around the world, and is under review.

In December 2021, the European Drug Administration (EMA) Human Medicinal Products Committee (CHMP) recommended the approval of the marketing application of non steroidal selective mineralocorticoid receptor antagonist fenelidone, and recommended the use of fenelidone (10mg or 20mg) for the treatment of chronic kidney disease (stages 3 and 4 with albuminuria) and type 2 diabetes in adults.