Healthy
Conditions
Brief summary
To evaluate the effect of food on the pharmacokinetics of BI 409306 and to investigate the pharmacokinetics of BI 409306 when given at bed time.
Interventions
DRUGBI 409306
film-coated tablet
Sponsors
Boehringer Ingelheim
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 50 Years
Healthy volunteers
Yes
Inclusion criteria
1. Healthy male and female volunteers 2. Age 18 (incl.) to 50 (incl.) years 3. Body mass index (BMI) range: 18.5 (incl.) to 29.9 (incl.) kg/m2
Exclusion criteria
1. Any evidence of a clinically relevant concomitant disease 2. Any finding of the medical examination (including BP, PR and ECG) deviating from normal and of clinical relevance 3. Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders 4. Surgery of the gastrointestinal tract (except appendectomy) 5. Diseases of the central nervous system (including but not limited to any kind of seizures, stroke or psychiatric disorders) 6. History or evidence of relevant orthostatic reaction, fainting spells or blackouts, occurrence of syncopes, brady- or tachycardia in the anamnesis. 7. Positive pregnancy test 8. No adequate contraception during the study and until 1 month of study completion, i.e. intrauterine device (IUD), sexual abstinence (for at least 1 month prior to enrolment), or surgical sterilisation (incl. hysterectomy). Females, who are not surgically sterile will be asked to additionally use barrier contraception methods (e.g. condom, diaphragm with spermicide)
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Maximum Measured Concentration of BI 409306 in Plasma (Cmax) | Treatment A/B: -1:00, 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00h; treatment C: -1:00, 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00h | Cmax is the maximum measured concentration of BI 409306 in plasma. More detailed time frame information: 1 hour (h) before administration of BI 409306 and 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00 h after administration of BI 409306 at treatment A/B; 1h before administration of BI 409306 and 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00 h after administration of BI 409306 at treatment C |
| Area Under the Concentration-time Curve of BI 409306 in Plasma From Time 0 to Time of Last Quantifiable Data Point (AUC0-tz) | Treatment A/B: -1:00, 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00h; treatment C: -1:00, 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00h | AUC0-tz is the area under the concentration-time curve of the BI 409306 in plasma from time 0 to time of last quantifiable data point. More detailed time frame information: 1 hour (h) before administration of BI 409306 and 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00 h after administration of BI 409306 at treatment A/B; 1h before administration of BI 409306 and 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00 h after administration of BI 409306 at treatment C |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Area Under the Concentration-time Curve of BI 409306 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-infinity) | Treatment A/B: -1:00, 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00h; treatment C: -1:00, 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00h | AUC0-infinity is the area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity. More detailed time frame information: 1 hour (h) before administration of BI 409306 and 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00 h after administration of BI 409306 at treatment A/B; 1h before administration of BI 409306 and 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00 h after administration of BI 409306 at treatment C. |
Countries
Germany
Participant flow
Recruitment details
Eighteen healthy subjects were entered and treated and completed the planned observation time. All 18 subjects received study medication (open-label) under fasted (Treatment A) and fed (Treatment B) conditions in a two-way crossover fashion followed by a fixed sequence administered at bed time (Treatment C).
Pre-assignment details
All subjects were screened for eligibility to participate in the trial. Subjects attended specialist sites which would then ensure that the subject met all strictly implemented inclusion/exclusion criteria. Subjects were not to be randomised to trial treatment if any one of the specific entry criteria were violated.
Participants by arm
| Arm | Count |
|---|---|
| BI 409306 Fasted/Fed/Bed Time Single oral dose of 25 mg BI 409306 film-coated tablet, with 240 ml water in the morning under fasted then under fed condition and last administered at bed-time with a washout period of at least 3 days between the administrations. | 9 |
| BI 409306 Fed/Fasted/Bed Time Single oral dose of 25 mg BI 409306 film-coated tablet, with 240 ml water in the morning under fed then under fast condition and last administered at bed-time with a washout period of at least 3 days between the administrations. | 9 |
| Total | 18 |
Baseline characteristics
| Characteristic | BI 409306 Fed/Fasted/Bed Time | Total | BI 409306 Fasted/Fed/Bed Time |
|---|---|---|---|
| Age, Continuous | 44.3 years STANDARD_DEVIATION 9.1 | 37.3 years STANDARD_DEVIATION 10.3 | 30.2 years STANDARD_DEVIATION 5.4 |
| Race (NIH/OMB) American Indian or Alaska Native | 0 Participants | 2 Participants | 2 Participants |
| Race (NIH/OMB) Asian | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) Black or African American | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) More than one race | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) Native Hawaiian or Other Pacific Islander | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) Unknown or Not Reported | 0 Participants | 0 Participants | 0 Participants |
| Race (NIH/OMB) White | 9 Participants | 16 Participants | 7 Participants |
| Sex: Female, Male Female | 3 Participants | 7 Participants | 4 Participants |
| Sex: Female, Male Male | 6 Participants | 11 Participants | 5 Participants |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk | EG002 affected / at risk |
|---|---|---|---|
| deaths Total, all-cause mortality | 0 / 18 | 0 / 18 | 0 / 18 |
| other Total, other adverse events | 1 / 18 | 4 / 18 | 1 / 18 |
| serious Total, serious adverse events | 0 / 18 | 0 / 18 | 0 / 18 |
Outcome results
Primary
Area Under the Concentration-time Curve of BI 409306 in Plasma From Time 0 to Time of Last Quantifiable Data Point (AUC0-tz)
AUC0-tz is the area under the concentration-time curve of the BI 409306 in plasma from time 0 to time of last quantifiable data point. More detailed time frame information: 1 hour (h) before administration of BI 409306 and 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00 h after administration of BI 409306 at treatment A/B; 1h before administration of BI 409306 and 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00 h after administration of BI 409306 at treatment C
Time frame: Treatment A/B: -1:00, 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00h; treatment C: -1:00, 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00h
Population: The Pharmacokinetic set (PKS): This set included all treated subjects who provided at least one observation for at least one primary endpoint without important protocol violations with respect to the statistical evaluation of PK endpoints. All 18 subjects were included in the PKS.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| BI 409306 Fasted | Area Under the Concentration-time Curve of BI 409306 in Plasma From Time 0 to Time of Last Quantifiable Data Point (AUC0-tz) | 273 Hour times nanomole per litre | Geometric Coefficient of Variation 118 |
| BI 409306 Fed | Area Under the Concentration-time Curve of BI 409306 in Plasma From Time 0 to Time of Last Quantifiable Data Point (AUC0-tz) | 293 Hour times nanomole per litre | Geometric Coefficient of Variation 96.4 |
| BI 409306 at Bed-time | Area Under the Concentration-time Curve of BI 409306 in Plasma From Time 0 to Time of Last Quantifiable Data Point (AUC0-tz) | 259 Hour times nanomole per litre | Geometric Coefficient of Variation 117 |
Comparison: No formal hypothesis was tested.90% CI: [96.697, 119.318]
Comparison: No formal hypothesis was tested.90% CI: [85.028, 105.875]
Primary
Maximum Measured Concentration of BI 409306 in Plasma (Cmax)
Cmax is the maximum measured concentration of BI 409306 in plasma. More detailed time frame information: 1 hour (h) before administration of BI 409306 and 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00 h after administration of BI 409306 at treatment A/B; 1h before administration of BI 409306 and 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00 h after administration of BI 409306 at treatment C
Time frame: Treatment A/B: -1:00, 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00h; treatment C: -1:00, 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00h
Population: The Pharmacokinetic set (PKS): This set included all treated subjects who provided at least one observation for at least one primary endpoint without important protocol violations with respect to the statistical evaluation of PK endpoints. All 18 subjects were included in the PKS.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| BI 409306 Fasted | Maximum Measured Concentration of BI 409306 in Plasma (Cmax) | 183 Nanomole per litre | Geometric Coefficient of Variation 118 |
| BI 409306 Fed | Maximum Measured Concentration of BI 409306 in Plasma (Cmax) | 175 Nanomole per litre | Geometric Coefficient of Variation 69.5 |
| BI 409306 at Bed-time | Maximum Measured Concentration of BI 409306 in Plasma (Cmax) | 150 Nanomole per litre | Geometric Coefficient of Variation 119 |
Comparison: No formal hypothesis was tested.90% CI: [72.593, 126.682]
Comparison: No formal hypothesis was tested.90% CI: [66.37, 101.639]
Secondary
Area Under the Concentration-time Curve of BI 409306 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-infinity)
AUC0-infinity is the area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity. More detailed time frame information: 1 hour (h) before administration of BI 409306 and 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00 h after administration of BI 409306 at treatment A/B; 1h before administration of BI 409306 and 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00 h after administration of BI 409306 at treatment C.
Time frame: Treatment A/B: -1:00, 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00h; treatment C: -1:00, 0:10, 0:20, 0:30, 0:45, 1:00, 1:30, 2:00, 2:30, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, 24:00h
Population: The Pharmacokinetic set (PKS): This set included all treated subjects who provided at least one observation for at least one primary endpoint without important protocol violations with respect to the statistical evaluation of PK endpoints. All 18 subjects were included in the PKS.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| BI 409306 Fasted | Area Under the Concentration-time Curve of BI 409306 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-infinity) | 273 Hour times nanomole per litre | Geometric Coefficient of Variation 118 |
| BI 409306 Fed | Area Under the Concentration-time Curve of BI 409306 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-infinity) | 293 Hour times nanomole per litre | Geometric Coefficient of Variation 96.3 |
| BI 409306 at Bed-time | Area Under the Concentration-time Curve of BI 409306 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-infinity) | 259 Hour times nanomole per litre | Geometric Coefficient of Variation 116 |
Comparison: No formal hypothesis was tested.90% CI: [96.709, 119.301]
Comparison: No formal hypothesis was tested.90% CI: [85.061, 105.921]