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Trial to Investigate Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single Oral Doses of BI135585 XX Administered as Tablet and as Solution in Healthy Volunteers

Phase 1
Completed
Conditions
Diabetes Mellitus, Type 2
Interventions
Drug: BI 135585
Drug: Placebo to BI 135585
Registration Number
NCT01146886
Lead Sponsor
Boehringer Ingelheim
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)

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
Male
Target Recruitment
60
Inclusion Criteria

Not provided

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Exclusion Criteria

Not provided

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Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
BI 135585BI 1355851 single dose per subject as oral solution in Part 1, or 3 single doses per subject as oral solution and 2 different tablet formulations in Part 2
Placebo to BI 135585Placebo to BI 1355851 single dose per subject as oral solution in Part 1
Primary Outcome Measures
NameTimeMethod
Assessment of tolerability by the investigatorup to 14 days post treatment
Change from baseline in Vital signs (blood pressure [BP], pulse rate [PR], respiratory rate [RR])up to 14 days post treatment
Change from baseline in 12-lead ECG with special attention to QTc prolongationup to 14 days post treatment
Change from baseline in Physical examination (occurrence of findings)up to 14 days post treatment
Cardiopulmonary monitoring resulting in clinically relevant findingsup to 14 days post treatment
Change from baseline in Clinical laboratory parameters including hormones of the HPA axis and thyroid glandup to 14 days post treatment
Number of patients with Adverse events (AE)up to 14 days post treatment
Secondary Outcome Measures
NameTimeMethod
tmax (time from dosing to maximum measured concentration)up to 72 hours post treatment
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)up to 72 hours post treatment
t1/2 (terminal half-life of the analyte in plasma)up to 72 hours post treatment
Cmax (maximum measured concentration of the analyte in plasma)up to 72 hours post treatment
AUC0-∞ (area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity)up to 72 hours post treatment
%AUCtz-∞ (percentage of the AUC0-∞ that was obtained by extrapolation)up to 72 hours post treatment
λz (terminal rate constant in plasma)up to 72 hours post treatment
CLR,t1-t2 (renal clearance of the analyte from timepoint t1 to timepoint t2) SRD part only[up to 72 hours post treatment
UFF/UFE ratio as an indicator of 11β-HSD2 inhibitionup to 24h
(5α-THF + 5β-THF)/THE ratio as an indicator of 11β-HSD1 inhibitionup to 24h
CL/F (total/apparent clearance of the analyte in plasma after extravascular administration)up to 72 hours post treatment
Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose)up to 72 hours post treatment
MRToral (mean residence time of the analyte in the body after oral administration)up to 72 hours post treatment
Aet1-t2 (amount of analyte eliminated in urine from timepoint t1 to timepoint t2) SRD part onlyup to 72 hours post treatment
fet1-t2 (fraction of analyte eliminated in urine from timepoint t1 to timepoint t2) SRD part onlyup to 72 hours post treatment
Total urinary corticosteroids (5α-THF + 5β-THF + THE + UFF + UFE) as an indicator of the activation of the HPA axisup to 24h

Trial Locations

Locations (1)

1283.1.1 Boehringer Ingelheim Investigational Site

🇩🇪

Biberach, Germany

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