Finerenone
Indications
Finerenone is used for:
Chronic Kidney Disease
Adult Dose
Chronic Kidney Disease
Indicated to reduce risk of sustained estimated glomerular filtration rate (eGFR) decline, end-stage kidney disease, cardiovascular death, nonfatal myocardial infarction, and hospitalization for heart failure in adults with chronic kidney disease (CKD) associated with type 2 diabetes
Starting dose
Determine starting dose by eGFR (mL/min/1.73m2)
eGFR >60: 20 mg PO once daily
eGFR 25-60: 10 mg PO once daily
eGFR <25: Not recommended
Increase dosage after 4 weeks to the target dose of 20 mg once daily based on eGFR and serum potassium thresholds.
Dose adjustment
Dose adjustment based on current serum potassium concentration (mEq/L) and current dose
Currently taking 10 mg qDay
<4.8 mEq/L: Increase dose to 20 mg qDay; if eGFR has decreased by more than 30% compared to previous measurement, maintain 10 mg dose
>4.8-5.5 mEq/L: Maintain 10 mg/day
>5.5 mEq/L: Withhold dose; consider restarting at 10 mg qDay when potassium <5 mEq/L
Currently taking 20 mg qDay
<4.8 mEq/L: Maintain 20 mg qDay
>4.8-5.5 mEq/L: Maintain 20 mg/day
>5.5 mEq/L: Withhold dose; restart at 10 mg qDay when potassium <5 mEq/L
Hepatic impairment
Mild or moderate (Child-Pugh A or B): No dosage adjustment recommended
Severe (Child-Pugh C): Avoid
Child Dose
Renal Dose
Administration
May take with or without food
Contra Indications
Concomitant treatment with strong CYP3A4 inhibitors
Adrenal insufficiency
Precautions
Hyperkalemia
Can cause hyperkalemia
Risk increases with decreasing kidney function and is greater with higher baseline potassium levels or other risk factors for hyperkalemia
Measure serum potassium and eGFR before initiating; adjust dose accordingly
Do not initiate if serum potassium 5 mEq/L
Periodically measure serum potassium during treatment and adjust dose as necessary; more frequent monitoring needed for patients at risk for hyperkalemia, including those on concomitant medications that impair potassium excretion or increase serum potassium
Pregnancy-Lactation
Pregnancy
Data are not available on use in pregnancy to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes
Animal studies have shown developmental toxicity at exposures ~4 times those expected in humans; clinical significance of these findings is unclear
Lactation
Data are unavailable on presence in human milk, effects on breastfed infants, or effects on milk production
Based on animal studies and potential risk to breastfed infants from exposure, avoid breastfeeding during treatment and for 1 day after last dose
Animal studies
In a prenatal and postnatal developmental toxicity study in rats, increased pup mortality and lower pup weight were observed at ~4 times the AUC unbound expected in humans
These findings suggest that finerenone is present in rat milk
When a drug is present in animal milk, it is likely that the drug will be present in human milk
Interactions
Side Effects
Side effects of Finerenone :
>10%
Hyperkalemia (18.3%)
1-10%
Hypotension (4.8%)
Hyponatremia (1.4%)
Mode of Action
Nonsteroidal, selective mineralocorticoid receptor (MR) antagonist, which is activated by aldosterone and cortisol and regulates gene transcription
Finerenone blocks MR-mediated sodium reabsorption and MR overactivation in both epithelial (eg, kidney) and nonepithelial (eg, heart, blood vessels) tissues
MR overactivation is thought to contribute to fibrosis and inflammation
Finerenone has a high potency and selectivity for the MR and has no relevant affinity for androgen, progesterone, estrogen, and glucocorticoid receptors