Finerenone, sold under the brand name Kerendia, is a

medication A medication (also called medicament, medicine, pharmaceutical drug, medicinal drug or simply drug) is a drug used to diagnose, cure, treat, or prevent disease. Drug therapy (pharmacotherapy) is an important part of the medical field and re ...

used to reduce the risk of kidney function decline, kidney failure, cardiovascular death, non-fatal heart attacks, and hospitalization for heart failure in adults with chronic kidney disease associated with type2 diabetes. Finerenone is a

non-steroidal A nonsteroidal compound is a drug that is not a steroid nor a steroid derivative. Nonsteroidal anti-inflammatory drugs (NSAIDs) are distinguished from corticosteroids as a class of anti-inflammatory agents. List of nonsteroidal steroid receptor ...

mineralocorticoid receptor antagonist Mineralocorticoids are a class of corticosteroids, which in turn are a class of steroid hormones. Mineralocorticoids are produced in the adrenal cortex and influence salt and water balances (Electrolyte#Physiological importance, electrolyte balan ...

(MRA). Common side effects include hyperkalemia (high levels of potassium), hypotension (low blood pressure), and hyponatremia (low levels of sodium). Finerenone was approved for medical use in the United States in July 2021, and in the European Union in February 2022.

Medical uses

In the United States, finerenone is

indicated In medicine, an indication is a valid reason to use a certain test, medication, procedure, or surgery. There can be multiple indications to use a procedure or medication. An indication can commonly be confused with the term diagnosis. A diagnosis ...

to reduce the risk of kidney function decline, kidney failure, cardiovascular death, non-fatal heart attacks, and hospitalization for heart failure in adults with

chronic kidney disease Chronic kidney disease (CKD) is a type of kidney disease in which a gradual loss of kidney function occurs over a period of months to years. Initially generally no symptoms are seen, but later symptoms may include leg swelling, feeling tired, vo ...

associated with type2 diabetes. In the European Union, finerenone is indicated for the treatment of chronic kidney disease (stage 3 and 4 with albuminuria) associated with type2 diabetes in adults.

Pharmacology

Finerenone has less relative

affinity Affinity may refer to: Commerce, finance and law * Affinity (law), kinship by marriage * Affinity analysis, a market research and business management technique * Affinity Credit Union, a Saskatchewan-based credit union * Affinity Equity Par ...

to other

steroid hormone receptor Steroid hormone receptors are found in the nucleus, cytosol, and also on the plasma membrane of target cells. They are generally intracellular receptors (typically cytoplasmic or nuclear) and initiate signal transduction for steroid hormones which ...

s than currently available aldosterone antagonists such as

eplerenone Eplerenone, sold under the brand name Inspra, is an aldosterone antagonist type of potassium-sparing diuretic that is used to treat chronic heart failure and high blood pressure, particularly for patients with resistant hypertension due to ele ...

and

spironolactone Spironolactone, sold under the brand name Aldactone among others, is a medication that is primarily used to treat fluid build-up due to heart failure, liver scarring, or kidney disease. It is also used in the treatment of high blood pressure ...

, which should result in fewer adverse effects like

gynaecomastia Gynecomastia (also spelled gynaecomastia) is the abnormal non-cancerous enlargement of one or both breasts in males due to the growth of breast tissue as a result of a hormone imbalance between estrogens and androgens. Updated by Brent Wisse (1 ...

impotence Erectile dysfunction (ED), also called impotence, is the type of sexual dysfunction in which the penis fails to become or stay erect during sexual activity. It is the most common sexual problem in men.Cunningham GR, Rosen RC. Overview of male ...

, and low libido. Finerenone blocks

mineralocorticoid receptor The mineralocorticoid receptor (or MR, MLR, MCR), also known as the aldosterone receptor or nuclear receptor subfamily 3, group C, member 2, (NR3C2) is a protein that in humans is encoded by the ''NR3C2'' gene that is located on chromosome 4q31 ...

s, which makes it a

potassium-sparing diuretic Potassium-sparing diuretics refers to drugs that cause diuresis without causing potassium loss in the urine. They are typically used as an adjunct in management of hypertension, cirrhosis, and congestive heart failure. The steroidal aldostero ...

. This table compares inhibitory (blocking) concentrations ( IC₅₀, unit: nM) of three antimineralocorticoids. Mineralocorticoid receptor inhibition is responsible for the desired action of the drugs, whereas inhibition of the other receptors potentially leads to side effects. Lower values mean stronger inhibition. The above-listed drugs have insignificant affinity for the

estrogen receptor Estrogen receptors (ERs) are a group of proteins found inside cells. They are receptors that are activated by the hormone estrogen ( 17β-estradiol). Two classes of ER exist: nuclear estrogen receptors (ERα and ERβ), which are members of the ...

. Finerenone acts as an antagonist to mineralocorticoid receptors harboring the S810L mutation, unlike other traditional MR inhibitors such as spironolactone and eplerenone that incidentally act as agonists.

Adverse Effects

Finerenone may cause electrolyte imbalances that must be resolved by a healthcare professional. In the case of potassium, patients taking Finerenone may experience a higher level of potassium in the blood. Symptoms that correlate to this clinical finding include nausea, weakness, chest pain and loss of movement. Another common electrolyte imbalance which may occur for patients on Finerenone is that patients may have low sodium, which can manifest as headaches, confusion, weakness and feeling off balance for patients.

History

The efficacy of finerenone to improve kidney and heart outcomes was evaluated in a randomized, multicenter, double-blind, placebo-controlled study in adults with chronic kidney disease associated with type2 diabetes. In this study, 5,674 participants were randomly assigned to receive either finerenone or a placebo. The study compared the two groups for the number of participants whose disease progressed to a composite (or combined) endpoint that included at least a 40% reduction in kidney function, progression to kidney failure, or kidney death. Results showed that 504 of the 2,833 participants who received finerenone had at least one of the events in the composite endpoint compared to 600 of the 2,841 participants who received a placebo. The U.S.

Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is respon ...

(FDA) granted the application for finerenone

priority review Priority review is a program of the United States Food and Drug Administration (FDA) to expedite the review process for drugs that are expected to have a particularly great impact on the treatment of a disease. The priority review voucher program ...

and

fast track The fast track is an informal English term meaning "the quickest and most direct route to achievement of a goal, as in competing for professional advancement". By definition, it implies that a less direct, slower route also exists. Fast track or F ...

designations. The FDA granted the approval of Kerendia to Bayer Healthcare.

Society and culture

Legal status

On 16 December 2021, the

Committee for Medicinal Products for Human Use The Committee for Medicinal Products for Human Use (CHMP), formerly known as Committee for Proprietary Medicinal Products (CPMP), is the European Medicines Agency's committee responsible for elaborating the agency's opinions on all issues regarding ...

(CHMP) of the

European Medicines Agency The European Medicines Agency (EMA) is an agency of the European Union (EU) in charge of the evaluation and supervision of medicinal products. Prior to 2004, it was known as the European Agency for the Evaluation of Medicinal Products or Euro ...

(EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Kerendia, intended for the treatment of chronic kidney disease associated with type2 diabetes in adults. The applicant for this medicinal product is Bayer AG. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged. Finerenone was approved for medical use in the European Union in February 2022.

Research

In the Phase II ARTS-DN study, finerenone dose-dependently reduced urine albumin to creatinine ratio in patients with

diabetic kidney disease Diabetic nephropathy, also known as diabetic kidney disease, is the chronic loss of kidney function occurring in those with diabetes mellitus. Diabetic nephropathy is the leading causes of chronic kidney disease (CKD) and end-stage renal disease ...

. Based on these findings, finerenone is being studied in the large Phase III FIDELIO and FIGARO outcome studies designed to assess whether finerenone reduces risk of CKD progression and adverse cardiovascular events in patients with Chronic Kidney Disease and Type 2 Diabetes. These trials have enrolled more than 13,000 patients with primary completion of FIDELIO anticipated in 2020 and FIGARO IN 2021.

References

External links

* {{Portal bar , Medicine Antimineralocorticoids Carboxamides Phenol ethers Nitriles Naphthyridines