To determine the basic pharmacokinetics of BI 1356 BS, its metabolite CD 1750 XX and radioactivity including excretion mass balance, excretion pathways and metabolism following the intravenous and oral administration of \[14C\] BI 1356 BS
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
12
Comparison of individual time course profiles of [14C] radioactivity in whole blood, plasma, urine and faeces
Time frame: before and up to 264 h after drug administration
Comparison of individual time course profiles of BI 1356 BS and its metabolite CD 1750 XX in plasma and urine
Time frame: before and up to 264 h after drug administration
Rate and extent of excretion mass balance based on the total radioactivity in urine and faeces
Time frame: prior to and up to 120 h after start of administration
CBlood cell/Cplasma ratio of [14C] -radioactivity
Time frame: 1:30, 3, 24 and 72 h after drug administration
Measurement of the plasma protein binding of total [14C] radioactivity in human plasma samples ex vivo
Time frame: 1:30 and 3 hours post drug administration
Cmax (maximum concentration of the analyte(s) in plasma)
Time frame: before and up to 264 h after drug administration
tmax (time from dosing to the maximum concentration of the analyte(s) in plasma)
Time frame: before and up to 264 h after drug administration
AUC0-tz (area under the concentration-time curve of the analyte(s) in plasma over the time interval from 0 to the time of the last quantifiable data point)
Time frame: before and up to 264 h after drug administration
AUC0-infinity (area under the concentration-time curve of the analyte(s) in plasma over the time interval from 0 to infinity)
Time frame: before and up to 264 h after drug administration
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λz (terminal rate constant in plasma)
Time frame: before and up to 264 h after drug administration
t1/2 (terminal half-life of the analyte(s) in plasma)
Time frame: before and up to 264 h after drug administration
MRTpo and MRT, respectively (mean residence time of the analyte(s) in the body after p.o. and i.v. administration)
Time frame: before and up to 264 h after drug administration
CL/F (apparent/total clearance of the analyte(s) in plasma following extravascular and intravenous administration)
Time frame: before and up to 264 h after drug administration
Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular or intravenous administration (F=1) respectively)
Time frame: before and up to 264 h after drug administration
feurine,0-tz (amount of analyte excreted in urine within the time interval zero to tz (=120 h) in % of dose)
Time frame: prior to and up to 120 h after start of administration
fefaeces,0-tz (amount of analyte excreted in faeces within the time interval zero to tz (=120 h) in % of dose)
Time frame: up to 120 h after drug administration
CLR,0-tz (renal clearance of analyte)
Time frame: prior to and up to 120 h after start of administration
Fa (drug absorption based on radioactivity data)
Time frame: up to 264 h after drug administration
Number of patients with adverse events
Time frame: up to 47 days
Global assessment of tolerability by investigator on a 4-point scale
Time frame: on day 12 during ambulant visit or on day of discharge on day 13, 14 or 15
Evaluation of local tolerability of the infusion by investigator on a 6-point scale
Time frame: after start of infusion up to day 15