Finerenone (Monograph)

Drug class: Nonsteroidal Mineralocorticoid Receptor Antagonists

Medically reviewed by Drugs.com on Nov 27, 2023. Written by ASHP.

Introduction

Nonsteroidal, selective antagonist of the mineralocorticoid receptor.

Uses for Finerenone

Kidney and Cardiovascular Disease Risk Reduction in Type 2 Diabetes

Used to reduce the 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.

Guidelines from the American Diabetes Association and Kidney Disease: Improving Global Outcomes recommend finerenone for patients with type 2 diabetes and CKD at high risk for CKD progression and cardiovascular events despite use of recommended therapies.

Finerenone Dosage and Administration

General

Pretreatment Screening

Measure serum potassium levels and eGFR prior to initiating treatment with finerenone. Do not initiate if serum potassium is >5 mEq/L.

Patient Monitoring

Measure serum potassium levels 4 weeks after treatment initiation, 4 weeks after any dose adjustment, upon initiation or dosage adjustment of moderate or weak CYP3A4 inhibitors, and periodically throughout treatment. More frequent monitoring is warranted in patients receiving concomitant treatment with drugs or supplements that increase potassium levels.
Monitor eGFR periodically throughout treatment.

Administration

Oral Administration

Administer orally once daily with or without food. Crush and mix tablets with water or soft foods such as applesauce for patients unable to swallow whole tablets. Administer immediately after mixing.

Take a missed dose as soon as possible. If unable to take the dose on the same day, skip the dose and resume with the next scheduled dose as prescribed.

Dosage

Adults

Kidney and Cardiovascular Disease Risk Reduction in Patients with Type 2 Diabetes

Oral

Recommended starting dosage is based on eGFR. For eGFR ≥60 mL/min/1.73m², starting dosage is 20 mg once daily. For eGFR ≥25 to <60 mL/min/1.73m², starting dosage is 10 mg once daily. Do not initiate if eGFR <25 mL/min/1.73m².

Target dose is 20 mg once daily.

Measure serum potassium 4 weeks after initiation and adjust dose based on potassium level (see Table 1). Monitor serum potassium 4 weeks after any dosage adjustment and throughout treatment, and adjust dose further as needed.

If eGFR has decreased by >30% compared to previous measurement, maintain 10 mg dose.

Table 1. Finerenone Dosage Adjustment Based on Current Serum Potassium Concentration and Current Dose.1
		Current Finerenone Dose 10 mg Once Daily	Current Finerenone Dose 20 mg Once Daily
Current Serum Potassium (mEq/L)	≤4.8	Increase dose to 20 mg once daily	Maintain dose of 20 mg once daily
>4.8–5.5	Maintain dose of 10 mg once daily	Maintain dose of 20 mg once daily
>5.5	Withhold finerenone Consider restarting finerenone at 10 mg once daily when the serum potassium is ≤5 mEq/L	Withhold finerenone Restart finerenone at 10 mg once daily when the serum potassium is ≤5 mEq/L

Special Populations

Hepatic Impairment

Mild impairment (Child Pugh A): no dosage adjustment required.

Moderate impairment (Child Pugh B): no dosage adjustment required; consider additional potassium monitoring.

Severe impairment (Child Pugh C): avoid use.

Renal Impairment

For eGFR ≥60 mL/min/1.73m², starting dosage is 20 mg once daily.

For eGFR ≥25 to <60 mL/min/1.73m², starting dosage is 10 mg once daily.

Do not initiate when eGFR <25 mL/min/1.73m².

Geriatric Use

No dosage adjustment required.

Cautions for Finerenone

Contraindications

Concomitant treatment with strong CYP3A4 inhibitors.
Adrenal insufficiency.

Warnings/Precautions

Hyperkalemia

Can cause hyperkalemia. Measure serum potassium and eGFR in all patients before initiation and periodically throughout treatment and adjust dose accordingly. Do not initiate if serum potassium is >5 mEq/L. More frequent monitoring may be necessary for patients at risk for hyperkalemia, including those on concomitant medications that impair potassium excretion or increase serum potassium.

Specific Populations

Pregnancy

No available data on use in pregnant women 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 about 4 times those expected in humans.

Lactation

No data on the presence of finerenone in human milk, the effects on the breast-fed infant, or the effect on milk production.

Likely present in human milk based on animal studies. Avoid breast-feeding during treatment and for 1 day after treatment.

Pediatric Use

Safety and efficacy not established in patients <18 years of age.

Geriatric Use

No overall difference in safety or efficacy was observed between older (≥65 years of age) and younger patients.

Renal Impairment

No clinically significant differences in AUC or C_max between patients with varying degrees of renal function (eGFR 15 to <90 mL/min/1.73m² compared to eGFR ≥90 mL/min/1.73m²).

Hepatic Impairment

Mild hepatic impairment: no clinically significant changes.

Moderate hepatic impairment: increase in finerenone AUC; no change in maximum plasma concentrations.

Severe hepatic impairment: not studied.

Common Adverse Effects

Adverse effects (≥1%) include hyperkalemia, hypotension, hyponatremia.

Drug Interactions

Specific Drugs

Drug	Interaction	Comments
Aluminum hydroxide and magnesium antacid	No clinically significant difference in finerenone pharmacokinetics when used concomitantly
Amiodarone	Increased finerenone AUC by 21%.	Monitor serum potassium during drug initiation or dosage adjustment of finerenone or any weak CYP3A4 inhibitor; adjust the finerenone dosage as appropriate
Digoxin	No clinically significant difference in pharmacokinetics of either agent when used concomitantly
Drugs affecting serum potassium	Increased serum potassium	Monitor serum potassium levels more frequently
Efavirenz	Decreased finerenone AUC by 80%	Avoid concomitant use of finerenone with moderate CYP3A4 inducers
Erythromycin	Increased finerenone AUC by 248% and C_max by 88%	Monitor serum potassium during drug initiation or dosage adjustment of finerenone or any moderate CYP3A4 inhibitor; adjust the finerenone dosage as appropriate
Gemfibrozil	No clinically significant difference in finerenone pharmacokinetics when used concomitantly
Itraconazole	Increased finerenone AUC by >400%	Concomitant use of finerenone with strong CYP3A4 inhibitors is contraindicated
Midazolam	No clinically significant difference in midazolam pharmacokinetics when used concomitantly
Omeprazole	No clinically significant difference in finerenone pharmacokinetics when used concomitantly
Repaglinide	No clinically significant difference in repaglinide pharmacokinetics when used concomitantly
Rifampin	Decreased finerenone AUC by 90%	Avoid concomitant use of finerenone with strong CYP3A4 inducers
Rosuvastatin	No clinically significant difference in rosuvastatin pharmacokinetics when used concomitantly
Warfarin	No clinically significant difference in pharmacokinetics of either agent when used concomitantly

Finerenone Pharmacokinetics

Absorption

Bioavailability

Finerenone exposure increased proportionally over a dose range of 1.25–80 mg (0.06–4 times the maximum approved dosage).

Bioavailability (absolute): 44%.

Time to maximum concentration: 0.5 to 1.25 hours.

Steady-state concentrations: after 2 days.

Food

No clinically significant effect on finerenone AUC when administered with high fat, high calorie food.

Distribution

Plasma Protein Binding

Protein binding (primarily albumin): 92%.

Elimination

Metabolism

Metabolized by CYP3A4 (90%) and CYP2C8 (10%) to inactive metabolites.

Elimination Route

Urine (80%; <1% unchanged); feces (20%; <0.2% unchanged).

Half-Life

Terminal half-life: 2–3 hours.

Special Populations

Age (18–79 years), sex, race/ethnicity (white, Asian, Black, and Hispanic), or weight (58–121 kg) do not have a clinically significant effect on the pharmacokinetics of finerenone.

Stability

Storage

Oral

Tablets, film-coated

Store tablets at 20–25°C (excursions permitted to 15–30°C).

Actions

Nonsteroidal, selective antagonist of the mineralocorticoid receptor (MR).
Blocks MR-mediated sodium reabsorption and MR overactivation in both epithelial and nonepithelial tissues.
Mineralocorticoid receptor overactivation is thought to contribute to fibrosis and inflammation.

Advice to Patients

Advise patients of the need for periodic monitoring of serum potassium levels. Advise patients to consult with their clinician before using potassium supplements or salt substitutes containing potassium.
Advise patients to avoid strong or moderate CYP3A4 inducers and to find alternative medicinal products with no or weak potential to induce CYP3A4.
Advise patients to avoid concomitant intake of grapefruit or grapefruit juice as it is expected to increase finerenone concentrations.
Advise women to inform their clinician if they are or plan to become pregnant or plan to breast-feed. Advise women that breast-feeding is not recommended during treatment with finerenone and for 1 day after treatment.
Advise patients to inform their clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses.
Inform patients of other important precautionary information.

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.