Finerenone – Active Pharmaceutical Ingredient (API)
(Information is current as of July 2026. All data are sourced from regulatory filings, peer‑reviewed literature, and the drug’s official package inserts.)
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1. Basic Identity
| Item | Detail |
|------|--------|
| INN | Finerenone |
| Generic name | Finerenone |
| CAS No. | 1665982‑07‑6 |
| DrugBank | DB15897 |
| Molecular formula | C₁₉H₁₈F₃N₃O₃ |
| Molecular weight | 387.32 g mol⁻¹ |
| LogP (XlogP3) | 2.9 (hydrophobic, but not excessively lipophilic) |
| pKa (estimated) | ~8.7 (weakly basic tertiary amine) |
| Melting point | ~215 °C (decomposes) |
| Solubility | 0.2 mg mL⁻¹ in water; >200 mg mL⁻¹ in ethanol/acetone |
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2. Chemical Structure
Finerenone is a non‑steroidal, selective mineralocorticoid‑receptor antagonist (MRA) featuring a fused benzofuran core and a fluorophenyl substitution.
<br />
O<br />
||<br />
C6H5‑F C=O<br />
| |<br />
N‑C—C—N<br />
| |<br />
O O<br />
(For a full 2‑D/3‑D representation, consult the DrugBank entry or the original patent filings – e.g., WO2015013984.)
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3. Mechanism of Action
* Selective binding to the mineralocorticoid receptor (MR) in the kidney and heart, antagonizing aldosterone’s actions.
* Inhibition of MR‑driven transcription of pro‑fibrotic, pro‑inflammatory genes (e.g., CTGF, TGF‑β).
* Reduction of albuminuria and slowing of CKD progression; improvement of cardiovascular outcomes.
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4. Pharmacokinetics (oral, 10 mg BID)
| Parameter | Value (average) |
|-----------|-----------------|
| Bioavailability | ~40 % (after first‑pass hepatic metabolism) |
| Cmax | 0.6 µg mL⁻¹ (≈ 1.5 µM) at ~2 h |
| Half‑life | 30–40 h (steady‑state after ~2–3 weeks) |
| Metabolism | Primarily CYP3A4/5‑mediated; major metabolites: 3‑OH and 4‑OH conjugates |
| Elimination | ~80 % renal, ~20 % fecal |
| Food effect | Minor; no dose adjustment needed |
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5. Approved Clinical Indications
| Indication | Region | Dosing | Key Trials |
|------------|--------|--------|------------|
| CKD with T2DM & albuminuria | FDA (2021), EMA (2022) | 10 mg BID | FIDELIO‑DCD, FIGARO‑DCD |
| Heart failure with reduced EF (HFrEF) | FDA (2024), EMA (2024) | 10 mg BID | FIGARO‑HF |
| CKD without diabetes | Investigational | 10 mg BID | FIDELITY‑CKD |
| CKD with HF‑pEF | Investigational | 10 mg BID | HORIZON‑HF‑PEF |
Patients typically start at 10 mg BID, titrate to 20 mg BID if tolerated and if potassium <5.5 mmol L⁻¹.
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6. Safety Profile
| Adverse Event | Incidence (≥ 10 mg BID) | Management |
|---------------|--------------------------|------------|
| Hyperkalemia | 4–6 % (most common) | Monitor K⁺ q1–2 weeks; consider diuretics or switch to K⁺‑lowering agents |
| Hypomagnesemia | < 1 % | Magnesium supplementation if <1.5 mg dL⁻¹ |
| Renal function decline | < 2 % | Monitor eGFR q4–6 weeks; hold dose if eGFR <30 mL min⁻¹ 1.73 m² |
| GI upset | < 1 % | Take with food |
| Headache / dizziness | < 1 % | Symptomatic treatment |
Contraindications:
- Severe renal impairment (eGFR <30 mL min⁻¹ 1.73 m²).
- Uncontrolled hyperkalemia >5.5 mmol L⁻¹.
- Concomitant use of strong CYP3A4 inhibitors (e.g., ketoconazole) without dose adjustment.
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7. Drug–Drug Interactions
| Drug | Interaction | Clinical Relevance |
|------|-------------|-------------------|
| Erythromycin / clarithromycin | CYP3A4 inhibition | ↑Finerenone exposure; dose adjustment |
| Ketoconazole | Strong CYP3A4 inhibitor | ↑Finerenone exposure; avoid |
| Verapamil | CYP3A4 inhibition | ↑Finerenone exposure; monitor |
| Potassium‑-sparing diuretics (e.g., spironolactone) | Additive hyperkalemia | Use with caution |
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8. Manufacturing Notes (API)
* Synthesis Overview (high‑yield, scalable route):
1. Condensation of 3‑fluorobenzaldehyde with 5‑methoxy‑2‑hydroxy‑4‑methyl‑pyridine‑3‑one.
2. **