Evaluation of safety, tolerability and PK of single rising oral doses of BI 34021 FU2 in healthy male volunteers; comparison of 100 mg drinking solution vs. tablet, assessment of food effect by re-dosing at 50 mg and 150 mg
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
DOUBLE
Enrollment
63
dose group 4 only
Number of participants with clinically significant findings on physical examination
Time frame: up to 10 days after last drug administration
Number of participants with clinically significant findings in vital signs
blood pressure (BP), pulse rate (PR) respiratory rate (RR), oral body temperature, orthostatic test
Time frame: up to 10 days after last drug administration
Number of participants with clinically significant findings in 12-lead electrocardiogram (ECG)
Time frame: up to 10 days after last drug administration
Number of participants with clinically significant findings in laboratory tests
Time frame: up to 10 days after last drug administration
Number of participants with clinically significant findings in safety markers
laboratory results for kidney and liver function
Time frame: up to 10 days after last drug administration
Number of participants with adverse events
Time frame: up to 10 days after last drug administration
Assessment of tolerability by investigator on a 4-point scale
Time frame: up to 10 days after last drug administration
Cmax (maximum measured concentration of the analyte in plasma)
Time frame: up to 72 hours after last drug administration
tmax (time from dosing to maximum measured concentration)
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only for dose groups 3 and 5
Time frame: up to 72 hours after last drug administration
AUC0-∞ (area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity)
Time frame: up to 72 hours after last drug administration
%AUCtz-∞ (the percentage of the AUC0-∞ that is obtained by extrapolation)
Time frame: up to 72 hours after last drug administration
AUC0-tz (area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the time of the last quantifiable data point)
Time frame: up to 72 hours after last drug administration
AUC0-2h (area under the concentration-time curve of the analytes in plasma over the time interval 0 to 2 hours after drug administration)
Time frame: up to 2 hours after last drug administration
λz (terminal rate constant in plasma)
Time frame: up to 72 hours after last drug administration
t1/2 (terminal half-life of the analyte in plasma)
Time frame: up to 72 hours after last drug administration
MRTp.o. (mean residence time of the analyte in the body after p.o. administration)
Time frame: up to 72 hours after last drug administration
CL/F (total/apparent clearance of the analyte in plasma after extravascular administration)
Time frame: up to 72 hours after last drug administration
Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose)
Time frame: up to 72 hours after last drug administration
Aet1-t2 (amount of analyte eliminated in urine from the time point t1 to time point t2)
Time frame: up to 48 hours after last drug administration
fet1-t2 (fraction of analyte eliminated in urine from time point t1 to time point t2)
Time frame: up to 48 hours after last drug administration
CLR,t1-t2 (renal clearance of the analyte from the time point t1 until the time point t2)
Time frame: up to 48 hours after last drug administration