Study to determine the pharmacokinetics (PK) of BI 201335 and total radioactivity including excretion mass balance, excretion pathways and metabolism following the oral administration of \[14C\]-BI 201335 at steady state.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
8
Individual concentration-time profiles of [14C]-radioactivity in whole blood, plasma, saliva, urine, and faeces
Time frame: up to 28 days
Individual concentration-time profiles of BI 201335 ZW in plasma and urine
Time frame: up to 28 days
Rate and extent of excretion mass balance based on the total radioactivity in urine and faeces
Time frame: up to 28 days
Elucidation of metabolite structures and identification of major metabolites in urine, faeces, and plasma in comparison with various animal species
Time frame: up to 28 days
Cblood cell/Cplasma ratio of [14C]-radioactivity
Time frame: up to 28 days
Measurement of the plasma protein binding of total [14C]-radioactivity in human plasma samples ex vivo
Time frame: up to day 28
Cmax,ss (maximum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ)
Time frame: up to day 28
tmax,ss (time from last dosing to maximum concentration of the analyte in plasma at steady state)
Time frame: up to day 28
Cmin,ss (minimum concentration of the analyte in plasma at steady state over a uniform dosing interval τ)
Time frame: up to day 28
AUCτ,ss (area under the concentration-time curve of the analyte in plasma at steady state over a uniform dosing interval τ)
Time frame: up to day 28
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λz,ss (terminal rate constant of the analyte in plasma at steady state)
Time frame: up to day 28
t1/2,ss (terminal half-life of the analyte in plasma at steady state)
Time frame: up to day 28
MRTpo,ss (mean residence time of the analyte in the body at steady state after oral administration)
Time frame: up to day 28
CL/F,ss (apparent clearance of the analyte in the plasma at steady state following multiple oral dose administration)
Time frame: up to day 28
Vz/F,ss (apparent volume of distribution of the analyte during the terminal phase λz at steady state following oral administration)
Time frame: up to day 28
Ae,urine,0-tz,ss (amount of analyte that is eliminated in urine at steady state from the time point 0 to time point tz)
Time frame: up to day 28
fe,urine,t1-t2,ss (fraction of the analyte in % of dose that is eliminated in urine at steady state from the time point 0 to time point tz)
Time frame: up to day 28
Ae,feces,t1-t2,ss (fraction of the analyte that is eliminated in faeces at steady state from time point 0 to time point tz)
Time frame: up to day 28
fe,feces,0-tz,ss (fraction of the analyte eliminated in faeces at steady state from time point 0 to time point tz)
Time frame: up to day 28
CLR,t1-t2,ss (renal clearance of the analyte at steady state from the time point 0 to time point tz)
Time frame: up to day 28
Number of patients with abnormal findings in physical examination
Time frame: Baseline and day 28
Number of patients with clinically significant changes in vital signs (blood pressure, pulse rate)
Time frame: Baseline, day 1, 10, 16 and 28
Number of patients with clinically significant changes in 12-lead electrocardiogram (ECG)
Time frame: Baseline, day 1, 10, 16 and 28
Number of patients with clinically significant changes in clinical laboratory tests (haematology, clinical chemistry, urinalysis)
Time frame: Baseline, day 10 and 28
Number of patients with adverse events
Time frame: up to 28 days
Assessment of tolerability on a 4-point scale by the investigator
Time frame: Day 28