Finerenone
[CAS# 1050477-31-0]

Identification

• Name: Finerenone
• Synonyms: (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide
• Molecular Formula: C₂₁H₂₂N₄O₃
• Molecular Weight: 378.42
• CAS Registry Number: 1050477-31-0
• EC Number: 814-499-5
• SMILES: CCOC1=NC=C(C2=C1[C@@H](C(=C(N2)C)C(=O)N)C3=C(C=C(C=C3)C#N)OC)C

Properties

• Density: 1.3±0.1 g/cm³, Calc.^*
• Index of Refraction: 1.627, Calc.^*
• Boiling Point: 554.7±50.0 °C (760 mmHg), Calc.^*
• Flash Point: 289.3±30.1 °C, Calc.^*

^* Calculated using Advanced Chemistry Development (ACD/Labs) Software.

Safety Data

• Risk Statements: H315-H319
• Safety Statements: P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313

Hazard Classification

Hazard	Class	Category Code	Hazard Statement
Acute toxicity	Acute Tox.	3	H301
Reproductive toxicity	Repr.	1B	H360
Chronic hazardous to the aquatic environment	Aquatic Chronic	1	H410

Discovery and Applications

Finerenone, a novel non-steroidal mineralocorticoid receptor antagonist (MRA), was discovered through research efforts aimed at developing new therapies for cardiovascular and kidney diseases. It was synthesized by Bayer AG as part of a program focused on identifying selective MRAs with improved safety and efficacy profiles compared to existing therapies.

Finerenone, a non-steroidal mineralocorticoid receptor antagonist (MRA), holds promise in the management of chronic kidney disease (CKD) and diabetic kidney disease (DKD). By selectively blocking the mineralocorticoid receptor, finerenone attenuates the deleterious effects of aldosterone, such as sodium retention, inflammation, fibrosis, and oxidative stress, which contribute to kidney damage and cardiovascular complications. Clinical trials have demonstrated that finerenone reduces proteinuria, slows the decline in estimated glomerular filtration rate (eGFR), and lowers the risk of adverse renal and cardiovascular events in patients with CKD and DKD, including those with type 2 diabetes mellitus. Finerenone has shown benefits in preserving renal function and reducing the progression of albuminuria, making it a promising therapeutic option for patients at risk of kidney disease progression and cardiovascular morbidity and mortality. Additionally, finerenone has been investigated in heart failure with preserved ejection fraction (HFpEF) and may offer renoprotective and cardioprotective effects in this patient population.

References

2012. Discovery of BAY 94‐8862: A Nonsteroidal Antagonist of the Mineralocorticoid Receptor for the Treatment of Cardiorenal Diseases. ChemMedChem, 7(8).
DOI: 10.1002/cmdc.201200081

2015. Finerenone Impedes Aldosterone-dependent Nuclear Import of the Mineralocorticoid Receptor and Prevents Genomic Recruitment of Steroid Receptor Coactivator-1. The Journal of biological chemistry, 290(36).
DOI: 10.1074/jbc.m115.657957

2024. Integrating the new pharmacological standard of care with traditional nutritional interventions in non-dialysis CKD. Journal of Nephrology, 37(8).
DOI: 10.1007/s40620-024-02135-y