Healthy
Conditions
Brief summary
The main objectives of this trial are: * To investigate basic pharmacokinetics of BI 1569912 and total radioactivity, including mass balance, excretion pathways and metabolism following oral administration of BI 1569912 (C-14) to healthy male subjects (test treatment, T). * To investigate the absolute bioavailability of BI 1569912 as single oral solution dose, using a single, concomitant intravenous micro-tracer administration of BI 1569912 (C-13) (reference treatment, R)
Interventions
DRUGBI 1569912 (C-14)
10 milligram (mg) \[14C\]-labeled BI 1569912 mixed with unlabeled BI 1569912 taken as an oral solution.
DRUGBI 1569912 (C-13)
A single dose of 100 microgram (µg) \[13C\]-labeled BI 1569912 taken as an intravenous (i.v.) infusion.
Sponsors
Boehringer Ingelheim
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
: Subjects will only be included in the trial if they meet the following criteria: 1. Healthy male subjects according to the assessment of the investigator, as based on a complete medical history including a physical examination, vital signs (blood pressure (BP), pulse rate (PR)), 12-lead electrocardiogram (ECG), and clinical laboratory tests 2. Age of 18 to 55 years (inclusive) 3. Body mass index (BMI) of 18.5 to 29.9 kg/m 2 (inclusive) 4. Signed and dated written informed consent in accordance with ICH-GCP and local legislation prior to admission to the trial
Exclusion criteria
: Subjects will not be allowed to participate, if any of the following general criteria apply: 1. Any finding in the medical examination (including BP, PR or ECG) deviating from normal and assessed as clinically relevant by the investigator 2. Repeated measurement of systolic blood pressure outside the range of 90 to 140 mmHg, diastolic blood pressure outside the range of 50 to 90 mmHg, or pulse rate outside the range of 40 to 100 beats per minute (bpm) 3. Any laboratory value outside the reference range that the investigator considers to be of clinical relevance, in particular hepatic parameters (alanine aminotransferase (ALT), aspartate aminotransferase (AST), total bilirubin) or renal parameters (creatinine) exceeding the upper limit of normal (ULN) after repeated measurements 4. Any evidence of a concomitant disease assessed as clinically relevant by the investigator 5. Further
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Fraction Excreted in Urine as Percentage of the Administered Dose Over the Time Interval From 0 to the Last Quantifiable Time Point (fe Urine,0-tz) of [14C]-Radioactivity | Up to 14 days. | Mass balance recovery for \[14C\]-radioactivity in urine after oral administration of BI 1569912 (C-14): Fraction excreted in urine as percentage of the administered dose over the time interval from 0 to the last quantifiable time point (fe urine,0-tz). |
| Fraction Excreted in Faeces as Percentage of the Administered Dose Over the Time Interval From 0 to the Last Quantifiable Time Point (fe Faeces,0-tz) of [14C]-Radioactivity | Up to 14 days. | Mass balance recovery for \[14C\]-radioactivity in faeces after oral administration of BI 1569912 (C-14): Fraction excreted in faeces as percentage of the administered dose over the time interval from 0 to the last quantifiable time point (fe faeces,0-tz) of \[14C\]-radioactivity. |
| Total Recovery of [14C]-Radioactivity | Up to 14 days. | Mass balance recovery for \[14C\]-radioactivity in urine and faeces after oral administration of BI 1569912 (C-14). The total recovery is calculated based on the individual values and hence can differ from the sum of the urine and faeces gMean values. |
| Area Under the Concentration-time Curve of BI 1569912 Over the Time Interval From 0 Extrapolated to Infinity in Plasma (AUC0-∞) | Within 3 hours before and 0.25*, 0.5#, 0.58, 0.66*, 0.75, 0.92*, 1.08, 1.25*, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 34, 48, 72, 96, 120, 192# and 288# hours following drug administration. *reference treatment only, #test treatment only. | Area under the concentration-time curve of BI 1569912 over the time interval from 0 extrapolated to infinity in plasma (AUC0-∞) for BI 1569912 and \[13C\]-BI 1569912 after a single oral administration of BI 1569912 (C-14) (test treatment) and a single concomitant intravenous administration of BI 1569912 (C-13) (reference treatment). The presented data was derived from an analysis of variance (ANOVA) on the logarithmic scale including the fixed effect for 'treatment' and 'subject' as a random effect. |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Maximum Measured Concentration of BI 1569912 in Plasma (Cmax) | Within 3 hours before and 0.25*, 0.5#, 0.58, 0.66*, 0.75, 0.92*, 1.08, 1.25*, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 34, 48, 72, 96, 120, 192# and 288# hours following drug administration. *reference treatment only, #test treatment only. | Cmax (maximum measured concentration in plasma) of BI 1569912 and \[14C\]-radioactivity after a single oral administration of BI 1569912 (C-14) and of \[13C\]-BI 1569912 after a single intravenous administration of BI 1569912 (C-13). |
| Area Under the Concentration-time Curve of BI 1569912 Over the Time Interval From 0 to the Last Quantifiable Time Point in Plasma (AUC 0-tz) | Within 3 hours before and 0.25*, 0.5#, 0.58, 0.66*, 0.75, 0.92*, 1.08, 1.25*, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 34, 48, 72, 96, 120, 192# and 288# hours following drug administration. *reference treatment only, #test treatment only. | AUC0-tz (area under the concentration-time curve over the time interval from 0 to the last quantifiable time point in plasma) of BI 1569912 and \[14C\]-radioactivity after a single oral administration of BI 1569912 (C-14) and of \[13C\]-BI 1569912 after a single intravenous administration of BI 1569912 (C-13). |
Countries
Netherlands
Participant flow
Recruitment details
This was a non-randomised, open-label, single-dose, fixed sequence trial in healthy male participants.
Pre-assignment details
All subjects were screened for eligibility prior to participation in the trial. Subjects attended a specialist site which ensured that they (the subjects) strictly met all inclusion and none of the exclusion criteria. Subjects were not to be allocated to a treatment group if any of the entry criteria were violated.
Baseline characteristics
| Characteristic | — |
|---|---|
| Age, Continuous | 34.9 Years STANDARD_DEVIATION 8.6 |
| Ethnicity (NIH/OMB) Hispanic or Latino | 0 Participants |
| Ethnicity (NIH/OMB) Not Hispanic or Latino | 8 Participants |
| Ethnicity (NIH/OMB) Unknown or Not Reported | 0 Participants |
| Race (NIH/OMB) American Indian or Alaska Native | 0 Participants |
| Race (NIH/OMB) Asian | 0 Participants |
| Race (NIH/OMB) Black or African American | 0 Participants |
| Race (NIH/OMB) More than one race | 0 Participants |
| Race (NIH/OMB) Native Hawaiian or Other Pacific Islander | 0 Participants |
| Race (NIH/OMB) Unknown or Not Reported | 0 Participants |
| Race (NIH/OMB) White | 8 Participants |
| Sex: Female, Male Female | 0 Participants |
| Sex: Female, Male Male | 8 Participants |
Adverse events
| Event type | EG000 affected / at risk |
|---|---|
| deaths Total, all-cause mortality | 0 / 8 |
| other Total, other adverse events | 5 / 8 |
| serious Total, serious adverse events | 0 / 8 |
Outcome results
None listed