Clinical trial NCT01146886: Trial to Investigate Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single Oral Doses of BI135585 XX Administered as Tablet and as Solution in Healthy Volunteers
Official title: A Randomised, Double-blind, Placebo-controlled Trial to Investigate Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single Rising Oral Doses of 10 mg to 1200 mg of BI 135585 XX Administered as a Solution to Healthy Male Volunteers (Trial Part 1), Followed by an Open, Randomised, Single-dose, Intra-individual Bioavailability Comparison of 200 mg BI 135585 XX as Tablet and as Solution (Trial Part 2)
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Diabetes Mellitus, Type 2
Lead sponsor: Boehringer Ingelheim
Sponsor class: INDUSTRY
First posted: 2010-06-22
Enrollment: 60
Sex: MALE
Minimum age (years): 18
Maximum age (years): 45
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: PARALLEL
Primary purpose: TREATMENT

Brief summary: 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)


Eligibility criteria: Inclusion criteria:

- healthy male volunteers

Primary outcomes:
measure: Change from baseline in Physical examination (occurrence of findings)
timeFrame: up to 14 days post treatment
measure: Change from baseline in Vital signs (blood pressure [BP], pulse rate [PR], respiratory rate [RR])
timeFrame: up to 14 days post treatment
measure: Change from baseline in 12-lead ECG with special attention to QTc prolongation
timeFrame: up to 14 days post treatment
measure: Cardiopulmonary monitoring resulting in clinically relevant findings
timeFrame: up to 14 days post treatment
measure: Change from baseline in Clinical laboratory parameters including hormones of the HPA axis and thyroid gland
timeFrame: up to 14 days post treatment
measure: Number of patients with Adverse events (AE)
timeFrame: up to 14 days post treatment
measure: Assessment of tolerability by the investigator
timeFrame: up to 14 days post treatment
Secondary outcomes:
measure: AUC0-∞ (area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity)
timeFrame: up to 72 hours post treatment
measure: (5α-THF + 5β-THF)/THE ratio as an indicator of 11β-HSD1 inhibition
timeFrame: up to 24h
measure: 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)
timeFrame: up to 72 hours post treatment
measure: Cmax (maximum measured concentration of the analyte in plasma)
timeFrame: up to 72 hours post treatment
measure: tmax (time from dosing to maximum measured concentration)
timeFrame: up to 72 hours post treatment
measure: %AUCtz-∞ (percentage of the AUC0-∞ that was obtained by extrapolation)
timeFrame: up to 72 hours post treatment
measure: λz (terminal rate constant in plasma)
timeFrame: up to 72 hours post treatment
measure: t1/2 (terminal half-life of the analyte in plasma)
timeFrame: up to 72 hours post treatment
measure: MRToral (mean residence time of the analyte in the body after oral administration)
timeFrame: up to 72 hours post treatment
measure: CL/F (total/apparent clearance of the analyte in plasma after extravascular administration)
timeFrame: up to 72 hours post treatment
measure: Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose)
timeFrame: up to 72 hours post treatment
measure: Aet1-t2 (amount of analyte eliminated in urine from timepoint t1 to timepoint t2) SRD part only
timeFrame: up to 72 hours post treatment
measure: fet1-t2 (fraction of analyte eliminated in urine from timepoint t1 to timepoint t2) SRD part only
timeFrame: up to 72 hours post treatment
measure: CLR,t1-t2 (renal clearance of the analyte from timepoint t1 to timepoint t2) SRD part only[
timeFrame: up to 72 hours post treatment
measure: UFF/UFE ratio as an indicator of 11β-HSD2 inhibition
timeFrame: up to 24h
measure: Total urinary corticosteroids (5α-THF + 5β-THF + THE + UFF + UFE) as an indicator of the activation of the HPA axis
timeFrame: up to 24h
Other outcomes:
Locations:
city: Biberach
country: Germany
facility: 1283.1.1 Boehringer Ingelheim Investigational Site
Study officials:
affiliation: Boehringer Ingelheim
name: Boehringer Ingelheim
role: STUDY_CHAIR
References: