title: Pharmacokinetics of the Novel Nonsteroidal Mineralocorticoid Receptor Antagonist Finerenone (BAY 94-8862) in Individuals With Renal Impairment.
abstract: Finerenone (BAY 94-8862) is a nonsteroidal mineralocorticoid receptor antagonist in development for the treatment of diabetic kidney disease. This observational trial compared the pharmacokinetics of a single oral dose of finerenone 10 mg (immediate-release tablet) in adults with mild (creatinine clearance [CLCR] 50-80 mL/min; n = 8), moderate (CLCR30 to < 50 mL/min; n = 8), or severe (CLCR< 30 mL/min; n  =  9) renal impairment with those in adults with normal renal function (CLCR> 80 mL/min; n  = 8) over 96 hours postdose. Exposure to finerenone was not affected by mild renal impairment. In participants with moderate or severe renal impairment, exposure to finerenone was increased compared with those with normal renal function (increase in area under the curve for unbound finerenone, 57.1% [outlier excluded] and 46.5%, respectively), with moderate to high interindividual variability. Renal impairment had no consistent effect on the maximum plasma concentration, Cmax(differences in Cmaxfor unbound finerenone of +12% and -7% with moderate [outlier excluded] and severe impairment vs normal renal function, respectively). Renal elimination of finerenone is minimal. However, changes in exposure may occur because of the effects of renal impairment on nonrenal routes of elimination.
authors.affiliation: Bayer Pharma AG, Clinical Sciences, Clinical Pharmacology, Cardiovascular and Hematology, Pharma Research Centre, Wuppertal, Germany.
authors.forename: Roland
authors.initials: R
authors.lastname: Heinig
authors.affiliation: Bayer Pharma AG, Global Research & Development Statistics, Pharma Research Centre, Wuppertal, Germany.
authors.forename: Nina
authors.initials: N
authors.lastname: Kimmeskamp-Kirschbaum
authors.affiliation: CRS Clinical Research Services Kiel GmbH, Kiel, Germany.
authors.forename: Atef
authors.initials: A
authors.lastname: Halabi
authors.affiliation: Bayer Pharma AG, Clinical Sciences, Clinical Pharmacology, Cardiovascular and Hematology, Pharma Research Centre, Wuppertal, Germany.
authors.forename: Silvia
authors.initials: S
authors.lastname: Lentini
mesh_terms: D000328:Adult; D000368:Aged; D019540:Area Under Curve; D001711:Biotransformation; D003928:Diabetic Nephropathies / Q000378:metabolism; D005260:Female; D006207:Half-Life; D006801:Humans; D007677:Kidney Function Tests; D008297:Male; D008875:Middle Aged; D000451:Mineralocorticoid Receptor Antagonists / Q000009:adverse effects / Q000493:pharmacokinetics*; D009287:Naphthyridines / Q000009:adverse effects / Q000493:pharmacokinetics*; D051437:Renal Insufficiency / Q000378:metabolism*
chemical_list: D000451:Mineralocorticoid Receptor Antagonists; D009287:Naphthyridines; C576501:finerenone
keywords: finerenone (BAY 94-8862); mineralocorticoid receptor antagonist; pharmacokinetics; renal impairment