The study aimed to investigate the effect of BIRT 2584 XX and its metabolite BI 610100 on the Pharmacokinetics (PK) of five probe substrates for cytochrome P450 isozymes. The substrates used to monitor enzyme activity were oral warfarin (for CYP2C9), oral omeprazole (for CYP2C19), oral dextromethorphan (for CYP2D6), oral caffeine (for CYP1A2) and intravenous midazolam (for hepatic CYP3A)
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
20
AUC0-inf (Area under the concentration-time curve of midazolam IV and S-warfarin in plasma over the time interval from 0 extrapolated to infinity)
Time frame: up to day 19
AUC (Area under the concentration-time curve of the ratio of omeprazole to 5-hydroxyomeprazole in plasma)
Time frame: up to day 19
0-12 hr urinary molar ratio of caffeine metabolites (1-Methylxanthine + 1-Methylurate +5-Acetylamino-6-formylamino-3-methyluracil)/ 1,7-Dimethylurate
Time frame: up to 12 hours after administration
0-12 hr urinary dextromethorphan/dextrorphan ratio
Time frame: up to 12 hours after administration
AUC0-tz (Area under the concentration-time curve of the S-warfarin, omeprazole and midazolam IV in plasma over the time interval from 0 to the time of the last quantifiable data point)
Time frame: up to day 19
Cmax (Maximum measured concentration of the S-warfarin, omeprazole and midazolam IV in plasma)
Time frame: up to day 19
tmax (Time from dosing to the maximum concentration of the S-warfarin, omeprazole and midazolam IV in plasma)
Time frame: up to day 19
λz (Terminal rate constant of the S-warfarin, omeprazole and midazolam IV in plasma)
Time frame: up to day 19
t1/2 (Terminal rate constant of the S-warfarin, omeprazole and midazolam IV in plasma)
Time frame: up to day 19
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.
MRT (Mean residence time of the S-warfarin, omeprazole and midazolam IV in the body after administration)
Time frame: up to day 19
CL/F (Apparent clearance of the S-warfarin, omeprazole and midazolam IV in plasma after extravascular single dose administration)
Time frame: up to day 19
Vz/F (Apparent volume of distribution during the terminal phase λz following extravascular administration S-warfarin, omeprazole and midazolam IV)
Time frame: up to day 19
AUC0-inf (Area under the concentration-time curve of omeprazole in plasma over the time interval from 0 extrapolated to infinity)
Time frame: up to day 19
trough levels of BIRT 2584 XX and BI 610100
Time frame: up to day 19
approximate peak levels of BIRT 2584 XX and BI 610100
Time frame: up to day 19
Number of subjects with adverse events
Time frame: up to 48 days
Number of subjects with abnormal changes in laboratory parameters
Time frame: up to 48 days