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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

Primary Purpose

Diabetes Mellitus, Type 2

Status

Completed

Phase

Phase 1

Locations

Germany

Study Type

Interventional

Intervention

Placebo to BI 135585

BI 135585

About this trial

This is an interventional treatment trial for Diabetes Mellitus, Type 2

Eligibility Criteria

18 Years - 45 Years (Adult)MaleAccepts Healthy Volunteers

Inclusion criteria:

- healthy male volunteers

Sites / Locations

1283.1.1 Boehringer Ingelheim Investigational Site

Arms of the Study

Arm 1

Arm 2

Arm Type

Experimental

Placebo Comparator

Arm Label

BI 135585

Placebo to BI 135585

Arm Description

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

1 single dose per subject as oral solution in Part 1

Outcomes

Primary Outcome Measures

Change from baseline in Physical examination (occurrence of findings)

Change from baseline in Vital signs (blood pressure [BP], pulse rate [PR], respiratory rate [RR])

Change from baseline in 12-lead ECG with special attention to QTc prolongation

Cardiopulmonary monitoring resulting in clinically relevant findings

Change from baseline in Clinical laboratory parameters including hormones of the HPA axis and thyroid gland

Number of patients with Adverse events (AE)

Assessment of tolerability by the investigator

Secondary Outcome Measures

AUC0-∞ (area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity)

(5α-THF + 5β-THF)/THE ratio as an indicator of 11β-HSD1 inhibition

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)

Cmax (maximum measured concentration of the analyte in plasma)

tmax (time from dosing to maximum measured concentration)

%AUCtz-∞ (percentage of the AUC0-∞ that was obtained by extrapolation)

λz (terminal rate constant in plasma)

t1/2 (terminal half-life of the analyte in plasma)

MRToral (mean residence time of the analyte in the body after oral administration)

CL/F (total/apparent clearance of the analyte in plasma after extravascular administration)

Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose)

Aet1-t2 (amount of analyte eliminated in urine from timepoint t1 to timepoint t2) SRD part only

fet1-t2 (fraction of analyte eliminated in urine from timepoint t1 to timepoint t2) SRD part only

CLR,t1-t2 (renal clearance of the analyte from timepoint t1 to timepoint t2) SRD part only[

UFF/UFE ratio as an indicator of 11β-HSD2 inhibition

Total urinary corticosteroids (5α-THF + 5β-THF + THE + UFF + UFE) as an indicator of the activation of the HPA axis

Full Information

NCT ID

NCT01146886

First Posted

June 14, 2010

Last Updated

October 31, 2013

Sponsor

Boehringer Ingelheim

1. Study Identification

Unique Protocol Identification Number

NCT01146886

Brief Title

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

2. Study Status

Record Verification Date

October 2013

Overall Recruitment Status

Completed

Study Start Date

June 2010 (undefined)

Primary Completion Date

September 2010 (Actual)

Study Completion Date

undefined (undefined)

3. Sponsor/Collaborators

Name of the Sponsor

Boehringer Ingelheim

4. Oversight

5. Study Description

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)

6. Conditions and Keywords

Primary Disease or Condition Being Studied in the Trial, or the Focus of the Study

Diabetes Mellitus, Type 2

7. Study Design

Primary Purpose

Treatment

Study Phase

Phase 1

Interventional Study Model

Parallel Assignment

Masking

Double

Allocation

Randomized

Enrollment

60 (Actual)

8. Arms, Groups, and Interventions

Arm Title

BI 135585

Arm Type

Experimental

Arm Description

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

Arm Title

Placebo to BI 135585

Arm Type

Placebo Comparator

Arm Description

1 single dose per subject as oral solution in Part 1

Intervention Type

Drug

Intervention Name(s)

Placebo to BI 135585

Intervention Description

Part 1 - oral doses given to approximately 9 parallel groups of 8 subjects (6 on active and 2 on on placebo) on Day 1

Intervention Type

Drug

Intervention Name(s)

BI 135585

Intervention Description

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

Primary Outcome Measure Information:

Title

Change from baseline in Physical examination (occurrence of findings)

Time Frame

up to 14 days post treatment

Title

Change from baseline in Vital signs (blood pressure [BP], pulse rate [PR], respiratory rate [RR])

Time Frame

up to 14 days post treatment

Title

Change from baseline in 12-lead ECG with special attention to QTc prolongation

Time Frame

up to 14 days post treatment

Title

Cardiopulmonary monitoring resulting in clinically relevant findings

Time Frame

up to 14 days post treatment

Title

Change from baseline in Clinical laboratory parameters including hormones of the HPA axis and thyroid gland

Time Frame

up to 14 days post treatment

Title

Number of patients with Adverse events (AE)

Time Frame

up to 14 days post treatment

Title

Assessment of tolerability by the investigator

Time Frame

up to 14 days post treatment

Secondary Outcome Measure Information:

Title

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

Title

(5α-THF + 5β-THF)/THE ratio as an indicator of 11β-HSD1 inhibition

Time Frame

up to 24h

Title

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

Title

Cmax (maximum measured concentration of the analyte in plasma)

Time Frame

up to 72 hours post treatment

Title

tmax (time from dosing to maximum measured concentration)

Time Frame

up to 72 hours post treatment

Title

%AUCtz-∞ (percentage of the AUC0-∞ that was obtained by extrapolation)

Time Frame

up to 72 hours post treatment

Title

λz (terminal rate constant in plasma)

Time Frame

up to 72 hours post treatment

Title

t1/2 (terminal half-life of the analyte in plasma)

Time Frame

up to 72 hours post treatment

Title

MRToral (mean residence time of the analyte in the body after oral administration)

Time Frame

up to 72 hours post treatment

Title

CL/F (total/apparent clearance of the analyte in plasma after extravascular administration)

Time Frame

up to 72 hours post treatment

Title

Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose)

Time Frame

up to 72 hours post treatment

Title

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

Title

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

Title

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

Title

UFF/UFE ratio as an indicator of 11β-HSD2 inhibition

Time Frame

up to 24h

Title

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

10. Eligibility

Sex

Male

Minimum Age & Unit of Time

18 Years

Maximum Age & Unit of Time

45 Years

Accepts Healthy Volunteers

Eligibility Criteria

Inclusion criteria: - healthy male volunteers

Overall Study Officials:

First Name & Middle Initial & Last Name & Degree

Boehringer Ingelheim

Organizational Affiliation

Boehringer Ingelheim

Official's Role

Study Chair

Facility Information:

Facility Name

1283.1.1 Boehringer Ingelheim Investigational Site

City

Biberach

Country

Germany

12. IPD Sharing Statement

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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

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