Finerenone

China [CN]

I. Basic Information

Item | Details

English Name | Finerenone

Chinese Name | 非奈利酮

CAS Number | 1050477-31-0

Chemical Name | 4-(4-Fluorophenyl)-2-(4-hydroxyphenyl)-5-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrole-3-carboxamide

Molecular Formula | C₂₁H₂₂N₄O₃

Molecular Weight | 378.43

Target | Mineralocorticoid Receptor (MR, IC₅₀=18nM, highly selective)

Developer | Bayer

Approval Date | July 2021 (US FDA); February 2022 (EU EMA); June 2022 (China NMPA)

Dosage Form and Strength | Film-coated tablets: 10mg/tablet, 20mg/tablet

II. Physicochemical Properties

Parameter | Data

Appearance | White to off-white crystalline powder

Solubility | Slightly soluble in water (<1mg/mL, 25℃), readily soluble in DMSO, methanol, ethanol, soluble in ethyl acetate

Dissociation Constant (pKa) | 9.8 (pyrazole ring), 8.2 (amide group) (predicted value)

Melting Point | 215-218℃ (decomposition)

Stability | Stable for 36 months at 25℃/60% RH, store in a sealed, cool, and dry place, avoid high temperature and light; stable under acidic conditions, easily degraded under alkaline conditions

Chiral Characteristics | No chiral center, racemic mixture, optical purity >99.5%

Partition Coefficient (logP) | 3.9 (predicted value)

III. Mechanism of Action (Core Advantage)

Highly selective MR antagonist: preferentially blocks excessive activation of MR, inhibits inflammation and fibrosis in renal and cardiovascular tissues, reduces sodium reabsorption, and lacks the anti-androgenic side effects of steroidal MRAs (such as gynecomastia). Dual Organ Protection: FIDELITY pooled analysis showed a 23% reduction in the risk of the renal composite endpoint (renal failure, sustained eGFR decline ≥57%, or renal-related death) compared to placebo, and a 14% reduction in the risk of the cardiovascular composite endpoint (cardiovascular death, non-fatal myocardial infarction/stroke, or hospitalization for heart failure).

Lower Risk of Hyperkalemia: Compared to spironolactone and eplerenone, there was a lower rate of permanent discontinuation due to hyperkalemia (2.3% vs 0.9%), resulting in better long-term tolerability.

Rapid Onset of Action: Oral administration resulted in a 32% reduction in the urinary albumin-to-creatinine ratio (UACR) from baseline after 4 months, with sustained and stable efficacy.