Study to investigate the relative bioavailability of 5 new 400 mg tablet formulations (trial formulation II prototypes) of BI 207127 compared to the current 200 mg BI 207127 tablet formulation (trial formulation I) in healthy male volunteers with the aim to identify the best formulation for further drug development (formulation finding part / trial part 1) and to investigate the effect of food on the relative bioavailability of the most promising one of these trial formulation II prototypes (food-effect part / trial part 2).
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
42
200 mg tablet
400 mg tablet
400 mg tablet
400 mg tablet
400 mg tablet
400 mg tablet
AUC0-∞ (area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity) for BI 207127
Time frame: up to 48 hours after drug administration
Cmax (maximum measured concentration of the analyte in plasma) for BI 207127
Time frame: up to 48 hours after drug administration
AUCt1-t2 (area under the concentration-time curve of the analyte in plasma over the time interval from t1 to t2)
Time frame: up to 24 hours after drug administration
tmax (time from dosing to the maximum concentration of the analyte in plasma)
Time frame: up to 48 hours after drug administration
λz (terminal rate constant in plasma)
Time frame: up to 48 hours after drug administration
t1/2 (terminal half-life of the analyte in plasma)
Time frame: up to 48 hours after drug administration
MRTpo (mean residence time of the analyte in the body after p.o. administration)
Time frame: up to 48 hours after drug administration
CL/F (apparent clearance of the analyte in the plasma after extravascular administration)
Time frame: up to 48 hours after drug administration
Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose)
Time frame: up to 48 hours after drug administration
The fluctuation parameter Cmax/C12 for the ER (Extended release) formulations only
Time frame: up to 48 hours after drug administration
Aet1-t2 (amount of analyte eliminated in urine from the time point t1 to time point t2)
Time frame: up to 24 hours after drug administration in the food-effect part
fet1-t2 (fraction of analyte eliminated in urine compared to oral dose administered from time point t1 to time point t2)
Time frame: up to 24 hours after drug administration in the food-effect part
CLR,t1-t2 (renal clearance of the analyte from the time point t1 until the time point t2)
Time frame: up to 24 hours after drug administration in the food-effect part
RCmax,Met (the ratio of Cmax of the metabolite, CD 6168 to Cmax of the parent compound, BI207127)
Time frame: up to 48 hours after drug administration
RAUC0-∞,Met (the ratio of AUC0-∞ of the metabolite, CD 6168 to AUC0-∞ of the parent compound, BI207127)
Time frame: up to 48 hours after drug administration
AUC0-∞ for CD 6168
Time frame: up to 48 hours after drug administration
Cmax for CD 6168
Time frame: up to 48 hours after drug administration
Measurement of protein binding in human plasma for BI 207127
Time frame: up to 48 hours after drug administration in the food-effect part
Number of patients with adverse events
Time frame: up to 9 weeks
Assessment of tolerability on a 4-point scale
Time frame: 48 h after each drug administration
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