Finerenone

Finerenone is a nonsteroidal, selective antagonist of the mineralocorticoid receptor (MR), which is activated by aldosterone and cortisol and regulates gene transcription. Finerenone blocks MR mediated sodium reabsorption and MR overactivation in both epithelial (e.g., kidney) and nonepithelial (e.g., heart, and blood vessels) tissues.

Finerenone is indicated to reduce the risk of sustained eGFR decline, end-stage kidney disease, cardiovascular death, nonfatal myocardial infarction, and hospitalization for heart failure in adult patients with CKD associated with T2D.

• CKD Associated with Type 2 Diabetes: Used to reduce risk of sustained eGFR decline, ESRD, cardiovascular death, nonfatal MI, and hospitalization for heart failure in adult patients.

Mineralocorticoid Receptor Antagonists

Nonsteroidal Mineralocorticoid Receptor Antagonist

Finerenone is a nonsteroidal, selective antagonist of the mineralocorticoid receptor (MR), which is activated by aldosterone and cortisol and regulates gene transcription. Finerenone blocks MR mediated sodium reabsorption and MR overactivation in both epithelial (kidney) and nonepithelial (heart, blood vessels) tissues.

Finerenone blocks mineralocorticoid receptors to reduce aldosterone-mediated inflammation and fibrosis, slowing progression of CKD and cardiovascular disease.

Adult Dose (Oral):

• eGFR >=60 mL/min/1.73 m²: 20 mg once daily.
• eGFR >=25 to <60 mL/min/1.73 m²: 10 mg once daily (may increase to target dose 20 mg after 4 weeks).
• eGFR <25 mL/min/1.73 m²: Not recommended.

Take 1 tablet orally once daily at the same time each day. May be taken with or without food. For patients unable to swallow whole tablets, may be crushed and mixed with water or soft foods.

If a dose is missed, take as soon as possible on the same day; if not possible, skip the dose and continue with the next dose as prescribed.

Common Side Effects (>=1%):

• Hyperkalemia
• Hypotension
• Hyponatremia

Precautions:

• Hyperkalemia: Finerenone can cause hyperkalemia; risk increases with decreasing kidney function; measure serum potassium and eGFR before initiation; do not initiate if serum potassium >5.0 mEq/L; monitor serum potassium periodically during treatment.

Contraindications:

• Concomitant use with strong CYP3A4 inhibitors
• Adrenal insufficiency

Drug Interactions:

• Strong CYP3A4 Inhibitors: Increase finerenone exposure; concomitant use contraindicated; avoid grapefruit or grapefruit juice.
• Moderate and Weak CYP3A4 Inhibitors: Increase finerenone exposure; monitor serum potassium and adjust dose.
• Strong and Moderate CYP3A4 Inducers: Decrease finerenone exposure; avoid concomitant use.

Food Interactions: Avoid grapefruit or grapefruit juice; may be taken with or without food.

Use in Pregnancy: No data on use in pregnant women; animal studies showed developmental toxicity.

Use in Lactation: No data on presence in human milk; avoid breastfeeding during treatment and for 1 day after treatment.

Pediatric Use: Safety and efficacy not established in patients below 18 years.

Geriatric Use: 58% of patients were >=65 years; no overall differences in safety or efficacy observed; no dose adjustment required.

Renal Impairment: eGFR >=60: 20 mg/day; eGFR >=25-60: 10 mg/day; eGFR <25: not recommended; severe renal impairment or ESRD: contraindicated.

Hepatic Impairment: Avoid in severe hepatic impairment (Child-Pugh C); mild-moderate (Child-Pugh A or B): no dosage adjustment; moderate: consider additional serum potassium monitoring.

Overdose: Suspected overdose: immediately interrupt treatment; most likely manifestation is hyperkalemia; if hyperkalemia develops, standard treatment should be initiated; finerenone is unlikely to be efficiently removed by hemodialysis (90% plasma protein bound).

Storage: Keep below 30 degree C, away from light and moisture. Keep out of reach of children.

Finerenone