The purpose of the study is to evaluate the pharmacokinetics of vilaprisan in subjects with moderate to severe renal impairment compared with matched subjects with normal renal function.
This is a multiple-center, open-label, non-randomized, single-dose study in 3 parallel groups of subjects with moderately or severely impaired renal function or normal renal function matched with regard to sex, age, race and weight. PK blood and urine sampling for determination of vilaprisan concentrations in plasma and urine, respectively, will be preformed at pre-defined time points up to 14 days post-dose. Safety and tolerability will be assessed through adverse events, clinical laboratory tests, vital signs, 12-lead electrocardiograms and physical examinations.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
OTHER
Masking
NONE
Enrollment
26
Single oral dose (1 x 2 mg immediate-release, film-coated tablet)
Clinical Pharmacology of Miami, Inc.
Miami, Florida, United States
Orlando Clinical Research Center
Orlando, Florida, United States
Area under the concentration versus time curve from zero to infinity after single (first) dose (AUC) of BAY1002670
Area under the concentration versus time curve from zero to the last data point above the lower limit of quantitation \[AUC(0-tlast)\], if AUC cannot be estimated in all subjects. In subjects with normal and moderately reduced renal function.
Time frame: -1hour (h), 30minutes (min), 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1day (d), 2d, 3d, 4d, 7d, 10d, 14d
Maximum observed drug concentration in measured matrix after single dose administration (Cmax) of BAY1002670
In subjects with normal and moderately reduced renal function.
Time frame: -1h, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1d, 2d, 3d, 4d, 7d, 10d, 14d
Number of participants with adverse events
In subjects with normal, moderately, and severely reduced renal function.
Time frame: Up to 6 weeks
AUC
In subjects with normal, moderately, and severely reduced renal function.
Time frame: -1h, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1d, 2d, 3d, 4d, 7d, 10d, 14d
unbound AUC (AUCu)
In subjects with normal, moderately, and severely reduced renal function.
Time frame: -1h, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1d, 2d, 3d, 4d, 7d, 10d, 14d
Cmax
In subjects with normal, moderately, and severely reduced renal function.
Time frame: -1h, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1d, 2d, 3d, 4d, 7d, 10d, 14d
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Unbound Cmax (Cmax,u)
In subjects with normal, moderately, and severely reduced renal function.
Time frame: -1h, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1d, 2d, 3d, 4d, 7d, 10d, 14d
Apparent oral clearance (CL/F)
In subjects with normal, moderately, and severely reduced renal function.
Time frame: -1h, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1d, 2d, 3d, 4d, 7d, 10d, 14d
Unbound CL/F (CLu/F)
In subjects with normal, moderately, and severely reduced renal function.
Time frame: -1h, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1d, 2d, 3d, 4d, 7d, 10d, 14d
Half-life associated with the terminal slope (t1/2)
In subjects with normal, moderately, and severely reduced renal function.
Time frame: -1h, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1d, 2d, 3d, 4d, 7d, 10d, 14d
Renal clearance (CLR)
In subjects with normal, moderately, and severely reduced renal function.
Time frame: -1h, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1d, 2d, 3d, 4d, 7d, 10d, 14d
Fraction of free (unbound) drug in plasma (fu)
In subjects with normal, moderately, and severely reduced renal function.
Time frame: -1h, 30min, 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h ,16h, 1d, 2d, 3d, 4d, 7d, 10d, 14d