Lyvelsa 10 Tablets

Lyvelsa tablet 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 chronic kidney disease (CKD) associated with type 2 diabetes (T2D).

Pharmacology

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. 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. 

Dosage & Administration

The recommended starting dosage: 10 mg or 20 mg orally once daily based on estimated glomerular filtration rate (eGFR) and serum potassium thresholds. Increase dosage after 4 weeks to the target dose of 20 mg once daily, based on eGFR and serum potassium thresholds. Tablets may be taken with or without food.

Recommended Dosage-

• eGFR ≥60 mL/min/1.73 m²: starting dose 20 mg once daily
• eGFR ≥25 to <60 mL/min/1.73 m²: starting dose 10 mg once daily
• eGFR <25 mL/min/1.73 m²: not recommended

For patients who are unable to swallow whole tablets, Finerenone may be crushed and mixed with water or soft foods.

Monitoring and Dose Adjustment: The target daily dose of Finerenone is 20 mg. Measure serum potassium 4 weeks after initiating treatment and adjust dose (see Table 2); if serum potassium levels are > 4.8 to 5.0 mEq/L, initiation of Finerenone treatment may be considered with additional serum potassium monitoring within the first 4 weeks based on clinical judgment and serum potassium levels. Monitor serum potassium 4 weeks after a dose adjustment and throughout treatment and adjust the dose as needed.

Missed doses: Direct a patient to take a missed dose as soon as possible after it is noticed, but only on the same day. If this is not possible, the patient should skip the dose and continue with the next dose as prescribed.

Interaction

Strong CYP3A4 Inhibitors: Lyvelsa is a CYP3A4 substrate. Concomitant use with a strong CYP3A4 inhibitor increases Lyvelsa exposure, which may increase the risk of Lyvelsa adverse reactions. Concomitant use of Lyvelsa with strong CYP3A4 inhibitors is contraindicated. Avoid concomitant intake of grapefruit or grapefruit juice.

Moderate and Weak CYP3A4 Inhibitors: Lyvelsa is a CYP3A4 substrate. Concomitant use with a moderate or weak CYP3A4 inhibitor increases Lyvelsa exposure, which may increase the risk of Lyvelsa adverse reactions. Monitor serum potassium during drug initiation or dosage adjustment of either Lyvelsa or the moderate or weak CYP3A4 inhibitor, and adjust Lyvelsa dosage as appropriate.

Strong and Moderate CYP3A4 Inducers: Lyvelsa is a CYP3A4 substrate. Concomitant use of Lyvelsa with a strong or moderate CYP3A4 inducer decreases Lyvelsa exposure, which may reduce the efficacy of Lyvelsa. Avoid concomitant use of Lyvelsa with strong or moderate CYP3A4 inducers.