The purpose of the study is to investigate the safety, tolerability, pharmacokinetics incl. dose proportionality, and pharmacodynamics of BI 135585 XX (Part 1), as well as the relative bioavailability of two different immediate release tablet formulations versus oral solution (Part 2)
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
DOUBLE
Enrollment
60
Part 1 - oral doses given to approximately 9 parallel groups of 8 subjects (6 on active and 2 on on placebo) on Day 1
Part 1 - oral doses given to approximately 9 parallel groups of 8 subjects (6 on active and 2 on placebo) on Day 1; Part 2 - oral doses given to 12 subjects on Day 1
1283.1.1 Boehringer Ingelheim Investigational Site
Biberach, Germany
Change from baseline in Physical examination (occurrence of findings)
Time frame: up to 14 days post treatment
Change from baseline in Vital signs (blood pressure [BP], pulse rate [PR], respiratory rate [RR])
Time frame: up to 14 days post treatment
Change from baseline in 12-lead ECG with special attention to QTc prolongation
Time frame: up to 14 days post treatment
Cardiopulmonary monitoring resulting in clinically relevant findings
Time frame: up to 14 days post treatment
Change from baseline in Clinical laboratory parameters including hormones of the HPA axis and thyroid gland
Time frame: up to 14 days post treatment
Number of patients with Adverse events (AE)
Time frame: up to 14 days post treatment
Assessment of tolerability by the investigator
Time frame: up to 14 days post treatment
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 post treatment
(5α-THF + 5β-THF)/THE ratio as an indicator of 11β-HSD1 inhibition
Time frame: up to 24h
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)
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Time frame: up to 72 hours post treatment
Cmax (maximum measured concentration of the analyte in plasma)
Time frame: up to 72 hours post treatment
tmax (time from dosing to maximum measured concentration)
Time frame: up to 72 hours post treatment
%AUCtz-∞ (percentage of the AUC0-∞ that was obtained by extrapolation)
Time frame: up to 72 hours post treatment
λz (terminal rate constant in plasma)
Time frame: up to 72 hours post treatment
t1/2 (terminal half-life of the analyte in plasma)
Time frame: up to 72 hours post treatment
MRToral (mean residence time of the analyte in the body after oral administration)
Time frame: up to 72 hours post treatment
CL/F (total/apparent clearance of the analyte in plasma after extravascular administration)
Time frame: up to 72 hours post treatment
Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose)
Time frame: up to 72 hours post treatment
Aet1-t2 (amount of analyte eliminated in urine from timepoint t1 to timepoint t2) SRD part only
Time frame: up to 72 hours post treatment
fet1-t2 (fraction of analyte eliminated in urine from timepoint t1 to timepoint t2) SRD part only
Time frame: up to 72 hours post treatment
CLR,t1-t2 (renal clearance of the analyte from timepoint t1 to timepoint t2) SRD part only[
Time frame: up to 72 hours post treatment
UFF/UFE ratio as an indicator of 11β-HSD2 inhibition
Time frame: up to 24h
Total urinary corticosteroids (5α-THF + 5β-THF + THE + UFF + UFE) as an indicator of the activation of the HPA axis
Time frame: up to 24h