Researchers are looking for a better way to treat people who have worsening of chronic heart failure, a long-term condition where the heart does not pump blood as well as it should. In this study researchers wanted to learn more about a new substance called finerenone (BAY94-8862). Finerenone is a substance that blocks the activation of a protein in the body called mineralocorticoid receptor (MR). An increased activation of MR is involved in the development of hypertension, organ damage and worsening of heart failure. Many patients with worsening chronic heart failure also suffer from chronic kidney disease. Chronic kidney disease is a long-term decrease in the kidneys' ability to work properly. The researchers studied how finerenone moves into, through and out of the body. The researchers also looked at how safe finerenone is and how it affects the body. The main purpose of this study was to help researchers develop recommendations for the amount of the substance (the dosing) to be given to patients with reduced kidney function.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
33
10 mg BAY94-8862 immediate release (IR) tablet, administered orally
Unnamed facility
Kiel, Schleswig-Holstein, Germany
Area under the plasma concentration vs time curve from zero to infinity for total (bound and unbound) drug after single dose administration of BAY94-8862 (AUC)
AUC for BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: Up to 96 hours post-dose
Maximum total (bound and unbound) drug concentration in plasma after single dose administration of BAY94-8862 (Cmax)
Cmax for BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: Up to 96 hours post-dose
AUC for unbound drug (AUCu)
AUCu for BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: Up to 96 hours post-dose
Cmax for unbound drug (Cmax,u)
Cmax,u BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: Up to 96 hours post-dose
AUC divided by dose per kg body weight (AUCnorm)
AUCnorm for BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: Up to 96 hours post-dose
AUCnorm for unbound drug (AUCu,norm)
AUCu, norm for BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: Up to 96 hours post-dose
Cmax divided by dose per body weight (Cmax,norm)
Cmax, norm for BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: Up to 96 hours post-dose
Cmax,norm for unbound drug (Cmax,u,norm)
Cmax,u,norm for BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: Up to 96 hours post-dose
Plasma renin activity (PRA)
Change from baseline in plasma renin activity
Time frame: Prior to dosing and 12 hours post-dose
Plasma angiotensin II
Change from baseline in plasma angiotensin II
Time frame: Prior to dosing and 12 hours post-dose
Serum aldosterone
Change from baseline in serum aldosterone
Time frame: Prior to dosing and 12 hours post-dose
Plasminogen activator inhibitor-1 (PAI-1)
Change from baseline in PAI-1
Time frame: Prior to dosing and 12 hours post-dose
Urinary volume
Change in volume of urine excreted
Time frame: Prior to dosing up to 24 hours post-dose
Urinary creatinine
Change in urine creatinine concentrations
Time frame: Prior to dosing up to 24 hours post-dose
Urinary electrolytes
Change in urinary electrolytes
Time frame: Prior to dosing up to 24 hours post-dose
Half-life associated with the terminal slope (t½)
t½ for BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: Up to 96 hours post-dose
Fraction unbound (fu)
fu for BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: 1 hour and 6 hours post-dose
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.
AUC divided by dose (AUC/D)
AUC/D for BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: Up to 96 hours post-dose
AUC from time 0 to the last data point (AUC(0-tlast))
AUC(0-tlast) for BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: Up to 96 hours post-dose
Cmax divided by dose (Cmax/D)
Cmax/D for BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: Up to 96 hours post-dose
Time to reach Cmax (tmax)
Time to reach Cmax (in case of two identical Cmax values, the first tmax was to be used) for BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: Up to 96 hours post-dose
Mean residence time (MRT)
MRT for BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: Up to 96 hours post-dose
Total body clearance of drug calculated after extravascular administration (CL/F)
CL/F for BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: Up to 96 hours post-dose
Total body clearance of unbound drug from plasma calculated after oral administration (apparent oral unbound clearance) (CLu/F)
CLu/F for BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: Up to 96 hours post-dose
Apparent volume of distribution during terminal phase after extravascular administration (Vz/F)
Vz/F for BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: Up to 96 hours post-dose
Amount excreted into urine from 0 to 96 h (end of urine sampling) after study drug administration (AE,ur)
AE,ur for BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: Up to 96 hours post-dose
Percent amount excreted into urine from 0 to 96 h (end of urine sampling) after study drug administration (%AE,ur)
%AE,ur for BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: Up to 96 hours post-dose
Renal body clearance of drug (CLR)
CLR of BAY94-8862 and its metabolites M1 (BAY1040818), M2 (BAY1088089) and M3 (BAY1088090)
Time frame: Up to 96 hours post-dose
Number of participants with adverse events
Time frame: Approximately 5 weeks