Renfit

Approved Indications:

• Chronic Kidney Disease (CKD) associated with Type 2 Diabetes Mellitus (T2DM): To reduce the risk of sustained decline in estimated glomerular filtration rate (eGFR), end-stage kidney disease, cardiovascular death, nonfatal myocardial infarction, and hospitalization for heart failure in adult patients with CKD associated with T2DM.
• Heart Failure with Reduced Ejection Fraction (HFrEF): Treatment to reduce the risk of cardiovascular death and hospitalization for heart failure in patients with chronic heart failure and reduced ejection fraction.

Off-label / Clinically Accepted Uses:

• Investigational use in other forms of heart failure or renal impairment is ongoing but not yet approved.

• Adults:
• Starting dose is typically 10 mg orally once daily for patients with serum potassium ≤4.8 mmol/L and eGFR ≥60 mL/min/1.73 m².
• For patients with eGFR between 25 and <60 mL/min/1.73 m², starting dose is 10 mg once daily.
• For patients with serum potassium 4.9–5.0 mmol/L or moderate renal impairment, initiate at 5 mg once daily.
• Dose may be increased to 20 mg once daily after 4 weeks if serum potassium and renal function allow.
• Dose Adjustments:
• Monitor serum potassium and renal function closely; withhold or reduce dose if hyperkalemia occurs.
• Avoid initiation if serum potassium >5.0 mmol/L.
• Use caution and adjust dosing in patients with impaired renal function.
• Pediatrics: Safety and efficacy not established; not recommended.
• Elderly: No specific dosage adjustments; monitor renal function and potassium.
• Administration:
• Take orally with or without food, preferably at the same time each day.

Finerenone is a selective, non-steroidal mineralocorticoid receptor antagonist (MRA) that blocks the binding of aldosterone to mineralocorticoid receptors in the kidney, heart, and vasculature. By inhibiting mineralocorticoid receptor activation, finerenone reduces inflammation, fibrosis, and hypertrophy in cardiovascular and renal tissues. This mechanism leads to decreased progression of kidney damage and reduced cardiovascular events in patients with CKD and heart failure.

• Absorption:
  Finerenone is rapidly absorbed with peak plasma concentrations reached approximately 1 to 2 hours post-dose. Oral bioavailability is moderate but specific percentages are not routinely reported.
• Distribution:
  The drug is highly protein-bound (>90%), primarily to albumin.
• Metabolism:
  Finerenone is extensively metabolized primarily by CYP3A4 enzyme in the liver to inactive metabolites.
• Elimination:
  The terminal half-life is approximately 2 to 3 hours. Elimination occurs mainly via hepatic metabolism, with metabolites excreted in urine and feces.

• Pregnancy:
  There is no adequate and well-controlled data in pregnant women. Animal studies have shown potential fetal harm related to mineralocorticoid receptor antagonism. Use during pregnancy is not recommended unless benefits outweigh risks.
• Lactation:
  It is unknown whether finerenone is excreted in human milk. Due to potential for serious adverse reactions in nursing infants, breastfeeding is not recommended during treatment.

• Primary Class: Mineralocorticoid receptor antagonist (MRA)
• Subclass: Non-steroidal selective MRA

• Known hypersensitivity to finerenone or any excipients
• Hyperkalemia (serum potassium >5.0 mmol/L) at baseline
• Severe renal impairment (eGFR <25 mL/min/1.73 m²)
• Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole)
• Pregnancy and lactation

• Hyperkalemia: Risk increased; serum potassium must be monitored regularly. Discontinue or reduce dose if potassium exceeds safe thresholds.
• Renal Function: Monitor renal parameters closely; use cautiously in moderate renal impairment.
• Hypotension: Monitor blood pressure; symptomatic hypotension may occur.
• Drug Interactions: Avoid strong CYP3A4 inhibitors; they increase finerenone plasma levels.
• Electrolyte Imbalance: Monitor sodium and potassium levels periodically.
• Cardiovascular: Caution in unstable heart failure patients.
• Monitoring: Regular lab tests are critical to avoid adverse events.

Common Adverse Effects:

• Hyperkalemia
• Hypotension
• Increased serum creatinine
• Dizziness
• Fatigue

Serious/Rare Side Effects:

• Severe hyperkalemia leading to cardiac arrhythmias
• Acute kidney injury
• Angioedema (rare)
• Allergic reactions including rash

• Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin): Increase finerenone levels; avoid concomitant use.
• Potassium-sparing diuretics, potassium supplements, or salt substitutes containing potassium: Increase risk of hyperkalemia.
• ACE inhibitors and ARBs: Combined use increases risk of hyperkalemia and renal impairment; monitor closely.
• Other mineralocorticoid receptor antagonists: Avoid concurrent use.
• CYP3A4 inducers (e.g., rifampin): May reduce finerenone efficacy by lowering plasma levels.

• Recent cardiovascular and nephrology guidelines endorse finerenone as a treatment to reduce kidney disease progression and cardiovascular risk in patients with CKD associated with T2DM.
• FDA approval includes expanded indication for reducing cardiovascular events in CKD patients with T2DM.
• Emphasis on close monitoring of potassium and renal function to mitigate risks.
• Ongoing research is assessing finerenone’s potential benefits in broader heart failure populations.

• Store at controlled room temperature between 20°C and 25°C (68°F to 77°F).
• Protect from moisture and light.
• Keep in original packaging until use.
• Do not freeze.
• Keep out of reach of children.