Healthy
Conditions
Brief summary
The primary objective of this trial is to investigate the absolute oral bioavailability of BI 425809 administered as tablet (Test, T) compared to \[C-14\]-BI 425809 administered as intravenous microtracer (Reference, R).
Interventions
DRUGBI 425809
One 25 mg film coated tablet administered with 240 milliliters of water after an overnight fast of at least 10 hours.
DRUG[C-14]-BI 425809
Intravenous micro-tracer infusion of 30 μg BI 425809 (14-C) administered 4 hours after treatment T.
Sponsors
Boehringer Ingelheim
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 65 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy male subjects according to the assessment of the investigator, 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 * Age of 18 to 65 years (incl.) * Body mass index (BMI) of 18.5 to 29.9 kg/m2 (incl.) * Signed and dated written informed consent prior to admission to the study in accordance with Good Clinical Practice (GCP) and local legislation * Subjects who are sexually active must use, with their partner, highly effective contraception from the time of administration of trial medication until 4 months after administration of trial medication. Adequate methods are: * Condoms plus use of hormonal contraception by the female partner that started at least 2 months prior to administration of trial medication (e.g., implants, injectables, combined oral or vaginal contraceptives, intrauterine device) or * Condoms plus surgical sterilization (vasectomy at least 1 year prior to enrolment) or * Condoms plus surgically sterilised partner (including hysterectomy) or * Condoms plus intrauterine device or * Condoms plus partner of non-childbearing potential (including homosexual men) Subjects are required to use condoms to prevent unintended exposure of the partner to the study drug via seminal fluid. * Alternatively, true abstinence is acceptable when it is in line with the subject's preferred and usual lifestyle. If a subject is usually not sexually active but becomes active, with their partner, they must comply with the contraceptive requirements detailed above.
Exclusion criteria
* Any finding in the medical examination (including Blood Pressure (BP), Pulse Rate (PR) or Electrocardiogram (ECG)) is deviating from normal and judged as clinically relevant by the investigator * Repeated measurement of systolic blood pressure outside the range of 90 to 139 mmHg, diastolic blood pressure outside the range of 45 to 89 mmHg, or pulse rate outside the range of 40 to 100 bpm * Any laboratory value outside the reference range that the investigator considers to be of clinical relevance * Any evidence of a concomitant disease judged as clinically relevant by the investigator * Clinically significant gastrointestinal, hepatic, renal, respiratory (including but not limited to interstitial lung disease), cardiovascular, metabolic, immunological or hormonal disorders * Further
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Area Under the Concentration-time Curve of the Analyte ([14C]-BI 425809 After iv Administration as Well as for BI 425809 After Oral Administration) Over the Time Interval From 0 to Infinity (AUC0-∞, Norm) | Pharmacokinetic samples were collected within 2 h before and up to 168 h after single oral administration of unlabelled BI 425809. Further details are in description. | The dose-normalised area under the concentration-time curve of the analyte (\[14C\]-BI 425809 after iv administration as well as for BI 425809 after oral administration) over the time interval from 0 to infinity (AUC0-∞, norm) is presented. Geometric least square mean (adjusted geometric mean) and adjusted geometric standard error were calculated using an analysis of variance (ANOVA) model performed on the logarithmic scale, including 'formulation' as a fixed effect and 'subject' as a random effect. For treatment T, pharmacokinetic samples were collected within 2 h prior to the drug administration and at 1, 2, 3, 4.083, 6, 8, 12, 24, 72, 120 and at 168 h after single oral administration of unlabelled BI 425809. For treatment R, samples were collected at 3, 4.083, 4.167, 4.25, 4.5, 5, 6, 7, 8, 12, 16, 24, 72, 120 and 168 h after single oral administration of unlabelled BI 425809. |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Maximum Measured Concentration of the BI 425809 in Plasma After a Single Oral Dose (Cmax) | Pharmacokinetic samples were collected within 2:00 h:m prior to the drug administration and at 1:00, 2:00, 3:00, 4:05, 6:00, 8:00, 12:00, 24:00, 72:00, 120:00 and at 168:00 h:m after drug administration. | Cmax, maximum measured concentration of the BI 425809 in plasma after a single oral dose is presented. |
Countries
Netherlands
Participant flow
Recruitment details
It was an open-label, non-randomized, single period, single arm Phase I trial in healthy participants. All participants received a single dose of 25 milligram (mg) unlabelled BI 425809 tablet plus a single intravenous (iv) micro-tracer infusion of 30 microgram (μg) BI 425809 (C-14), containing 27 μg BI 425809 mixed with 3 μg \[C-14\]-BI 425809.
Pre-assignment details
All participants were screened for eligibility to participate in the trial. Participants attended specialist site which would then ensured that all participants met all inclusion/exclusion criteria. Participants were not to be administered to trial treatment if any one of the specific entry criteria were not met.
Baseline characteristics
| Characteristic | — |
|---|---|
| Age, Continuous | 35.0 Years STANDARD_DEVIATION 14.5 |
| Ethnicity (NIH/OMB) Hispanic or Latino | 0 Participants |
| Ethnicity (NIH/OMB) Not Hispanic or Latino | 6 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 | 1 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 | 5 Participants |
| Sex: Female, Male Female | 0 Participants |
| Sex: Female, Male Male | 6 Participants |
Adverse events
| Event type | EG000 affected / at risk |
|---|---|
| deaths Total, all-cause mortality | 0 / 6 |
| other Total, other adverse events | 3 / 6 |
| serious Total, serious adverse events | 0 / 6 |
Outcome results
None listed