Finerenone

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Finerenone
Clinical data
Trade namesKerendia
Other namesBAY 94-8862
AHFS/Drugs.comMonograph
MedlinePlusa621038
License data
Pregnancy
category
Routes of
administration		Oral
Drug classPotassium-sparing diuretic
ATC code
Legal status
Legal status
Identifiers
  • (4S)-4-(4-Cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
E number{{#property:P628}}
CompTox Dashboard (EPA)
  • {{#property:P3117}}Lua error in Module:EditAtWikidata at line 29: attempt to index field 'wikibase' (a nil value).
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Chemical and physical data
FormulaC21H22N4O3
Molar mass378.432 g·mol−1
3D model (JSmol)
  • NC(=O)C1=C(C)Nc2c(C)cnc(OCC)c2[C@@H]1c3ccc(C#N)cc3OC
  • InChI=1S/C21H22N4O3/c1-5-28-21-18-17(14-7-6-13(9-22)8-15(14)27-4)16(20(23)26)12(3)25-19(18)11(2)10-24-21/h6-8,10,17,25H,5H2,1-4H3,(H2,23,26)/t17-/m1/s1
  • Key:BTBHLEZXCOBLCY-QGZVFWFLSA-N

Finerenone, marketed under the brand name Kerendia among others, is a medication 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 type 2 diabetes.[8] Finerenone is a non-steroidal mineralocorticoid receptor antagonist.[7] It is taken orally (swallowed by mouth).

Common side effects include abnormally high levels of potassium in the bloodstream, abnormally low levels of sodium in the bloodstream, and abnormally low blood pressure.[8]

Finerenone was approved for medical use in the United States in July 2021,[8][10] and in the European Union in February 2022.[9] The US Food and Drug Administration considers it to be a first-in-class medication.[11]

Medical uses

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In the United States, finerenone is indicated 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 type 2 diabetes.[8]

In the European Union, finerenone is indicated for the treatment of chronic kidney disease (stage 3 and 4 with albuminuria) associated with type 2 diabetes in adults.[9]

Pharmacology

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Finerenone has less relative affinity to other steroid hormone receptors than currently available aldosterone antagonists such as eplerenone and spironolactone, which should result in fewer adverse effects like gynaecomastia, impotence, and low libido.[12][13]

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.[14]

Spironolactone Eplerenone Finerenone
Mineralocorticoid receptor 24 990 18
Glucocorticoid receptor 2400 22,000 >10,000
Androgen receptor 77 21,200 >10,000
Progesterone receptor 740 31,200 >10,000

Finerenone acts as an antagonist to mineralocorticoid receptors harboring the S810L mutation, unlike other traditional inhibitors of mineralocorticoids such as spironolactone and eplerenone that incidentally act as agonists.[15]

A meta-analysis of data from seven randomized controlled trials (13,783 participants) found a benefit to using finerenone in people with diabetic kidney disease and overt proteinuria.[16]

Adverse effects

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Finerenone may cause electrolyte imbalances.[17] Symptoms that correlate with higher levels of potassium include nausea, weakness, chest pain, and loss of movement.[17] People with lower levels of sodium may experience headaches, confusion, weakness, and feeling off balance.[17]

History

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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 type 2 diabetes.[8] In this study, 5,674 participants were randomly assigned to receive either finerenone or a placebo.[8]

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.[8] 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.[8]

The US Food and Drug Administration (FDA) granted the application for finerenone priority review and fast track designations.[8] The FDA granted the approval of Kerendia to Bayer Healthcare.[8]

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In December 2021, the Committee for Medicinal Products for Human Use of the European Medicines Agency 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 type 2 diabetes in adults.[18] Finerenone was approved for medical use in the European Union in February 2022.[9][19]

Brand names

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Finerenone is sold under the brand names Kerendia and Firialta.[20]

Research

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In a phase II study, finerenone reduced urine albumin to creatinine ratio in patients with diabetic kidney disease.[21] Based on that finding, it is being studied in phase studies designed to assess whether it reduces risk of progression of chronic kidney disease and adverse cardiovascular events in patients with type 2 diabetes. These studies have enrolled more than 13,000 patients with primary completion anticipated in 2020 and 2021.[22][full citation needed][23][full citation needed]

References

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  8. ^ a b c d e f g h i j k Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value). Public Domain This article incorporates text from this source, which is in the public domain.
  9. ^ a b c d Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value). Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
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  22. ^ Clinical trial number NCT02540993 for "Efficacy and Safety of Finerenone in Subjects With Type 2 Diabetes Mellitus and Diabetic Kidney Disease (FIDELIO-DKD)" at ClinicalTrials.gov
  23. ^ Clinical trial number NCT02545049 for "Efficacy and Safety of Finerenone in Subjects With Type 2 Diabetes Mellitus and the Clinical Diagnosis of Diabetic Kidney Disease (FIGARO-DKD)" at ClinicalTrials.gov

Further reading

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