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

This study has been completed.
Sponsor:
Information provided by:
Boehringer Ingelheim
ClinicalTrials.gov Identifier:
NCT01146886
First received: June 14, 2010
Last updated: October 31, 2013
Last verified: October 2013

June 14, 2010
October 31, 2013
June 2010
September 2010   (final data collection date for primary outcome measure)
  • Change from baseline in Physical examination (occurrence of findings) [ Time Frame: up to 14 days post treatment ] [ Designated as safety issue: No ]
  • Change from baseline in Vital signs (blood pressure [BP], pulse rate [PR], respiratory rate [RR]) [ Time Frame: up to 14 days post treatment ] [ Designated as safety issue: No ]
  • Change from baseline in 12-lead ECG with special attention to QTc prolongation [ Time Frame: up to 14 days post treatment ] [ Designated as safety issue: No ]
  • Cardiopulmonary monitoring resulting in clinically relevant findings [ Time Frame: up to 14 days post treatment ] [ Designated as safety issue: No ]
  • Change from baseline in Clinical laboratory parameters including hormones of the HPA axis and thyroid gland [ Time Frame: up to 14 days post treatment ] [ Designated as safety issue: No ]
  • Number of patients with Adverse events (AE) [ Time Frame: up to 14 days post treatment ] [ Designated as safety issue: No ]
  • Assessment of tolerability by the investigator [ Time Frame: up to 14 days post treatment ] [ Designated as safety issue: No ]
Safety and tolerability of BI 135585 XX will be assessed in a descriptive way using physical examinations (occurence of findings), vital signs, ECGs, cardiopulmonary monitoring, laboratory tests, and incidence and severity of adverse events. [ Time Frame: up to 14 days post treatment ] [ Designated as safety issue: Yes ]
Complete list of historical versions of study NCT01146886 on ClinicalTrials.gov Archive Site
  • 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 ] [ Designated as safety issue: No ]
  • (5α-THF + 5β-THF)/THE ratio as an indicator of 11β-HSD1 inhibition [ Time Frame: up to 24h ] [ Designated as safety issue: No ]
  • 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) [ Time Frame: up to 72 hours post treatment ] [ Designated as safety issue: No ]
  • Cmax (maximum measured concentration of the analyte in plasma) [ Time Frame: up to 72 hours post treatment ] [ Designated as safety issue: No ]
  • tmax (time from dosing to maximum measured concentration) [ Time Frame: up to 72 hours post treatment ] [ Designated as safety issue: No ]
  • %AUCtz-∞ (percentage of the AUC0-∞ that was obtained by extrapolation) [ Time Frame: up to 72 hours post treatment ] [ Designated as safety issue: No ]
  • λz (terminal rate constant in plasma) [ Time Frame: up to 72 hours post treatment ] [ Designated as safety issue: No ]
  • t1/2 (terminal half-life of the analyte in plasma) [ Time Frame: up to 72 hours post treatment ] [ Designated as safety issue: No ]
  • MRToral (mean residence time of the analyte in the body after oral administration) [ Time Frame: up to 72 hours post treatment ] [ Designated as safety issue: No ]
  • CL/F (total/apparent clearance of the analyte in plasma after extravascular administration) [ Time Frame: up to 72 hours post treatment ] [ Designated as safety issue: No ]
  • Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose) [ Time Frame: up to 72 hours post treatment ] [ Designated as safety issue: No ]
  • 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 ] [ Designated as safety issue: No ]
  • 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 ] [ Designated as safety issue: No ]
  • 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 ] [ Designated as safety issue: No ]
  • UFF/UFE ratio as an indicator of 11β-HSD2 inhibition [ Time Frame: up to 24h ] [ Designated as safety issue: No ]
  • 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 ] [ Designated as safety issue: No ]
  • To characterize the pharmacokinetics of BI 135585 XX in plasma and urine following oral administration [ Time Frame: up to 72 hours post treatment ] [ Designated as safety issue: No ]
  • To assess the pharmacodynamics of BI 135585XX by measuring of cortisol and cortisone and their metabolites in urine [ Time Frame: up to 24 hours post treatment ] [ Designated as safety issue: No ]
Not Provided
Not Provided
 
Trial to Investigate Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single Oral Doses of BI135585 XX Administered as Tablet and as Solution in Healthy Volunteers
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)

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)

Not Provided
Interventional
Phase 1
Allocation: Randomized
Endpoint Classification: Safety Study
Intervention Model: Parallel Assignment
Masking: Double-Blind
Primary Purpose: Treatment
Diabetes Mellitus, Type 2
  • Drug: Placebo to BI 135585
    Part 1 - oral doses given to approximately 9 parallel groups of 8 subjects (6 on active and 2 on on placebo) on Day 1
  • Drug: BI 135585
    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
  • Experimental: BI 135585
    1 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
    Intervention: Drug: BI 135585
  • Placebo Comparator: Placebo to BI 135585
    1 single dose per subject as oral solution in Part 1
    Intervention: Drug: Placebo to BI 135585
Not Provided

*   Includes publications given by the data provider as well as publications identified by ClinicalTrials.gov Identifier (NCT Number) in Medline.
 
Completed
60
Not Provided
September 2010   (final data collection date for primary outcome measure)

Inclusion criteria:

- healthy male volunteers

Male
18 Years to 45 Years
Yes
Contact information is only displayed when the study is recruiting subjects
Germany
 
NCT01146886
1283.1, 2010-018856-28
Not Provided
Boehringer Ingelheim, Study Chair, Boehringer Ingelheim
Boehringer Ingelheim
Not Provided
Study Chair: Boehringer Ingelheim Boehringer Ingelheim
Boehringer Ingelheim
October 2013

ICMJE     Data element required by the International Committee of Medical Journal Editors and the World Health Organization ICTRP