Loading…
KERENDIA is a brand name for Finerenone, supplied as a tablet. The medicine, its uses, side effects and dosage are the same regardless of brand.
Verbatim from this product's HC label. Tap a section to expand.
).
Legend:
C=Case Study; CT=Clinical Trial; T=Theoretical Note: The effects of itraconazole, clarithromycin, fluvoxamine, rifampicin and efavirenz on finerenone exposure are predictions based on PBPK simulations. No clinical data was available to evaluate effects of strong and weak CYP3A4 inhibitors or strong and moderate CYP3A4 inducers on finerenone exposure.
75 h), compared to administration under fasted conditions. This was paralleled by an increase in extent of absorption (AUC). 75 h), and increase in AUC. 3 Pharmacokinetics, Effect of food). 25 hours and Cmax decreased by approximately 23%.
4 Administration). Concomitant intake of grapefruit or grapefruit juice is expected to increase the plasma concentration of finerenone and should be avoided (see 4 Dosage and Administration and 7 Warnings and Precautions, General). 6 Drug-Herb Interactions Avoid concomitant use of KERENDIA with St John’s Wort (a strong CYP3A4 inducer) which may markedly decrease finerenone exposure and result in reduced therapeutic effect.
7 Drug-Laboratory Test Interactions Interactions with laboratory tests have not been established. 1 Mechanism of Action Finerenone is a nonsteroidal, selective antagonist of the mineralocorticoid receptor (MR). Finerenone binds to the MR and blocks the binding of aldosterone, a component of the renin-angiotensin- aldosterone-system (RAAS).
Aldosterone plays a central role in the homeostatic regulation of blood pressure, plasma sodium and potassium levels. The mechanisms of action contributing to reduction of renal and cardiovascular events with KERENDIA are not completely understood and may be due to multi-factorial effects in different tissues.
Potential mechanisms of action reported under certain experimental conditions include: attenuation of inflammation and fibrosis that are thought to be mediated by MR overactivation. In vitro, finerenone dose-dependently inhibited MR interaction with transcriptional coactivators implicated in the expression of pro-inflammatory and pro-fibrotic mediators.
Blocking of MR by finerenone in vivo counteracts sodium retention in the kidneys and hypertrophic processes in the kidneys, heart and blood vessels. , gynecomastia). , reversible increases of plasma renin activity and serum aldosterone concentrations with baseline values reached again within 48 hours after the last dose.
Following activation of the MR with the agonist fludrocortisone, single doses of finerenone up to 20 mg showed natriuretic effects while decreasing urinary potassium excretion as compared to placebo. The highest single dose of 80 mg and the highest multiple dose of 40 mg of finerenone did not affect vital signs parameters in healthy participants.
Effects on urinary albumin-to-creatinine ratio In randomized, double-blind, placebo-controlled, multicenter phase III studies in adults with CKD and T2D (FIDELIO-DKD and FIGARO-DKD), the placebo-corrected relative reduction in urinary albumin-to- creatinine ratio (UACR) in patients randomized to finerenone at month 4 was 31% and 32%, respectively and UACR remained reduced throughout both studies for at least 48 months.
). Effect of moderate CYP3A4 inhibitors on finerenone Erythromycin (500 mg thrice daily) CT AUC ↑ 248% Cmax ↑ 88% Serum potassium may increase, and therefore, additional monitoring of serum potassium is recommended and dose adjustment may be needed (see 4 Dosage and Administration and 7 Warnings and Precautions).
Verapamil (240 mg controlled- release tablet once daily) CT AUC ↑ 170% Cmax ↑ 120% Serum potassium may increase, and therefore, additional monitoring of serum potassium AND PRECAUTIONS). Effect of weak CYP3A4 inhibitors on finerenone Fluvoxamine (100 mg BID) T AUC ↑ 57% Cmax ↑ 38% Serum potassium may increase, and therefore, monitoring of serum potassium is recommended (see 4 Dosage and Administration and 7 Warnings and Precautions).
, phenobarbital) should be avoided (see 7 Warnings and Precautions. , carbamazepine, phenytoin, St John’s Wort) or with efavirenz, phenobarbital and other moderate CYP3A4 inducers should be avoided (see 7 WARNINGS AND PRECAUTIONS).
Legend:
C=Case Study; CT=Clinical Trial; T=Theoretical Note: The effects of itraconazole, clarithromycin, fluvoxamine, rifampicin and efavirenz on finerenone exposure are predictions based on PBPK simulations. No clinical data was available to evaluate effects of strong and weak CYP3A4 inhibitors or strong and moderate CYP3A4 inducers on finerenone exposure.
75 h), compared to administration under fasted conditions. This was paralleled by an increase in extent of absorption (AUC). 75 h), and increase in AUC. 3 Pharmacokinetics, Effect of food). 25 hours and Cmax decreased by approximately 23%.
4 Administration). Concomitant intake of grapefruit or grapefruit juice is expected to increase the plasma concentration of finerenone and should be avoided (see 4 Dosage and Administration and 7 Warnings and Precautions, General). 6 Drug-Herb Interactions Avoid concomitant use of KERENDIA with St John’s Wort (a strong CYP3A4 inducer) which may markedly decrease finerenone exposure and result in reduced therapeutic effect.
Not medical advice. Always read the patient information leaflet and follow your prescriber or pharmacist.
Know a brand we are missing in Canada? Suggest a brand →
Brand names are compiled from public regulatory records for active-ingredient mapping only. Drugvu is not affiliated with any manufacturer. This is not medical advice.
In FINEARTS-HF, randomized, double-blind, placebo-controlled, multicenter phase III study in adults with heart failure (LVEF ≥40%), the placebo-corrected relative reduction in UACR in patients randomized to finerenone at month 6 was 30%, and UACR remained reduced up to the last measurement at 24 months.
In MinerAlocorticoid Receptor Antagonist Tolerability Study - Diabetic Nephropathy (ARTS DN), a randomized, double-blind, placebo-controlled, multicenter phase IIb dose-finding study in adults with CKD and T2D, the placebo-corrected relative reduction in UACR at Day 90 was 25% and 38% in patients treated with finerenone 10 mg and 20 mg once daily, respectively.
KERENDIA® (finerenone) Page 23 of 48 Cardiac electrophysiology In a dedicated randomized, blinded, placebo- and positive-controlled four-way crossover QT study in 57 healthy participants, there was no indication of a clinically relevant QT/QTc prolonging effect of finerenone after single doses of 20 mg (therapeutic) or 80 mg (supratherapeutic).
25 to 80 mg. A summary of finerenone pharmacokinetic parameters after single dose of KERENDIA in healthy volunteers is shown in Table 9. Table 9 – Summary of Finerenone Pharmacokinetic Parameters in Plasma After Single Dose in Fasted State (Healthy Volunteers (Geometric Mean (Geometric Coefficient of Variation), or Median (Range) for tmax) Cmax [μg/L] Tmax [h] T½ […]
7 Drug-Laboratory Test Interactions Interactions with laboratory tests have not been established. 1 Mechanism of Action Finerenone is a nonsteroidal, selective antagonist of the mineralocorticoid receptor (MR). Finerenone binds to the MR and blocks the binding of aldosterone, a component of the renin-angiotensin- aldosterone-system (RAAS).
Aldosterone plays a central role in the homeostatic regulation of blood pressure, plasma sodium and potassium levels. The mechanisms of action contributing to reduction of renal and cardiovascular events with KERENDIA are not completely understood and may be due to multi-factorial effects in different tissues.
Potential mechanisms of action reported under certain experimental conditions include: attenuation of inflammation and fibrosis that are thought to be mediated by MR overactivation. In vitro, finerenone dose-dependently inhibited MR interaction with transcriptional coactivators implicated in the expression of pro-inflammatory and pro-fibrotic mediators.
Blocking of MR by finerenone in vivo counteracts sodium retention in the kidneys and hypertrophic processes in the kidneys, heart and blood vessels. , gynecomastia). , reversible increases of plasma renin activity and serum aldosterone concentrations with baseline values reached again within 48 hours after the last dose.
Following activation of the MR with the agonist fludrocortisone, single doses of finerenone up to 20 mg showed natriuretic effects while decreasing urinary potassium excretion as compared to placebo. The highest single dose of 80 mg and the highest multiple dose of 40 mg of finerenone did not affect vital signs parameters in healthy participants.
Effects on urinary albumin-to-creatinine ratio In randomized, double-blind, placebo-controlled, multicenter phase III studies in adults with CKD and T2D (FIDELIO-DKD and FIGARO-DKD), the placebo-corrected relative reduction in urinary albumin-to- creatinine ratio (UACR) in patients randomized to […]