Not provided
| ID | Type | Description | Link |
|---|---|---|---|
| 2010-023604-27 | EudraCT Number | EudraCT |
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
The primary objective of the current study is to investigate the safety and tolerability of BI 409306 in healthy male genotyped volunteers following oral administration of single rising doses.
The secondary objectives are: (1) to explore dose proportionality of BI 409306 as immediate release solid oral dosage, (2) to explore the relative bioavailability of BI 409306 when administered as immediate release solid oral dosage compared to oral drinking solution and (3) to compare the safety and pharmacokinetic profiles between two different groups of genotyped subjects.
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
| Label | Type | Description | Intervention Names |
|---|---|---|---|
| BI 409306 0.5 mg PiB [EM] | Experimental | Extensive metaboliser [EM] subjects administered one single dose of 0.5 milligram (mg) BI 409306 powder in bottle (PiB) reconstituted for oral solution (0.5 mg /milliliter (mL)) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 mL drinking water) after an overnight fast of at least 10 hours. |
|
| BI 409306 2 mg PiB [EM] | Experimental | EM subjects administered one single dose of 2 mg BI 409306 PiB reconstituted for oral solution (0.5 mg/mL) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 milliliter drinking water) after an overnight fast of at least 10 hours. |
|
| BI 409306 5 mg PiB followed by BI 409306 5 mg Tablet [EM] | Experimental | EM subjects administered one single dose of 5 mg BI 409306 powder in bottle (PiB) reconstituted for oral solution (0.5 mg/ mL) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 mL drinking water) after an overnight fast of at least 10 hours in period 1; followed by a washout period of 5 days; followed by one single dose of 5 mg BI 409306 immediate release tablet administered orally with 240 mL water after an overnight fast of at least 10 hours in period 2. |
|
| BI 409306 10 mg Tablet [EM] |
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Placebo | Drug | Solution for oral administration |
| |
| Measure | Description | Time Frame |
|---|---|---|
| Percentage of Subjects With Drug-related Adverse Events | Percentage of subjects with investigator defined drug-related Adverse Events (AEs) | From first drug administration until 30 days after last drug administration; up to 31 days. |
| Percentage of Subjects With Clinical Relevant Abnormalities for Physical Examination, Vital Signs, Clinical Laboratory Tests, Oral Body Temperature and ECG | Percentage of subjects with Clinical Relevant abnormalities for Physical examination, Vital Signs blood pressure (BP), pulse rate (PR) respiratory rate (RR), orthostatic test), Clinical laboratory tests (haematology, clinical chemistry and urinalysis), Oral body temperature and ECG were reported. | Day 4 |
| Percentage of Subjects Per Category for Assessment of Tolerability by Investigator | The investigator assessed global clinical assessment and tolerability of BI 409306 were reported in possible categories were 'good', 'satisfactory', 'not satisfactory', and 'bad'. | Day 4 |
| Change From Baseline in Bond & Lader (B&L) Visual Analogue Scales (VAS) | The B&L VAS scores were calculated from 16 item with each has a score range from 0 to 10 [cm]. The score of each of the 3 categories of effects ("alertness", "calmness", and "contentment") is a weighted average of the scores from the 16 items. The VAS score for alertness/calmness/contentment ranges from 0 to 10 (more alertness/calmness/contentment). The B&L VAS data was analysed descriptively (change from baseline at 24 hour). The VAS assessment 2 h before drug administration was considered as baseline. | At 24 hours |
| Measure | Description | Time Frame |
|---|---|---|
| Area Under the Concentration-time Curve of the BI 409306 in Plasma From Time 0 to Time of Last Quantifiable Data Point (AUC0-24) | AUC0-24, Area under the concentration-time curve of the BI 409306 in plasma over the time interval from 0 to the time of the last quantifiable data point is presented as geometric mean (gMean) and geometric coefficient of variation (gCV%). Pharmacokinetic samples were also collected at 48:00 and 72:00 hours after the drug administration for dose groups 10 mg onwards. |
Not provided
Inclusion criteria:
Exclusion criteria:
Not provided
Not provided
Not provided
Not provided
Not provided
| Name | Affiliation | Role |
|---|---|---|
| Boehringer Ingelheim | Boehringer Ingelheim | Study Chair |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| 1289.1.1 Boehringer Ingelheim Investigational Site | Ingelheim | Germany |
Clinical studies sponsored by Boehringer Ingelheim, phases I to IV, interventional and non-interventional, are in scope for sharing of the raw clinical study data and clinical study documents. Exceptions might apply, e.g. studies in products where Boehringer Ingelheim is not the license holder; studies regarding pharmaceutical formulations and associated analytical methods, and studies pertinent to pharmacokinetics using human biomaterials; studies conducted in a single center or targeting rare diseases (in case of low number of patients and therefore limitations with anonymization).
For more details refer to: https://www.mystudywindow.com/msw/datatransparency
Not provided
Not provided
Not provided
Not provided
All subjects were screened for eligibility to participate in the trial. Subjects attended specialist sites which would then ensure that all subjects met all inclusion/exclusion criteria. Subjects were not to be randomised to trial treatment if any one of the specific entry criteria were not met.
In this Phase 1, single centre, placebo-controlled trial (within dose groups), total of 80 healthy subjects were entered and 79 (71 CYP2C19 Extensive metaboliser /8 Poor CYP2C19 metaboliser) subjects were treated in 10 sequential dose groups.
Not provided
| ID | Title | Description |
|---|---|---|
| FG000 | Placebo Matching to BI 409306 [EM and PM] | Extensive metaboliser [EM] subjects administered one single dose of placebo matching to BI 409306 powder in bottle (PiB) reconstituted for oral solution or one single dose of placebo matching to BI 409306 tablet orally with 240 mL water after an overnight fast of at least 10 hours. Poor metaboliser [PM] subjects administered one single dose of placebo matching to BI 409306 powder in bottle (PiB) reconstituted for oral solution or one single dose of placebo matching to BI 409306 tablet orally with 240 mL water after an overnight fast of at least 10 hours in period 1; followed by a washout period of 5 days; followed by one single dose of placebo to BI 409306 tablet administered orally with 240 mL water after an overnight fast of at least 10 hours in period 2. |
| FG001 | BI 409306 0.5 mg PiB [EM] | Extensive metaboliser [EM] subjects administered one single dose of 0.5 milligram (mg) BI 409306 powder in bottle (PiB) reconstituted for oral solution (0.5 mg /milliliter (mL)) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 mL drinking water) after an overnight fast of at least 10 hours. |
| FG002 | BI 409306 2 mg PiB [EM] | EM subjects administered one single dose of 2 mg BI 409306 PiB reconstituted for oral solution (0.5 mg/mL) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 milliliter drinking water) after an overnight fast of at least 10 hours. |
| FG003 | BI 409306 5 mg PiB Followed by BI 409306 5 mg Tablet [EM] | EM subjects administered one single dose of 5 mg BI 409306 powder in bottle (PiB) reconstituted for oral solution (0.5 mg/ mL) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 mL drinking water) after an overnight fast of at least 10 hours in period 1; followed by a washout period of 5 days; followed by one single dose of 5 mg BI 409306 immediate release tablet administered orally with 240 mL water after an overnight fast of at least 10 hours in period 2. |
| FG004 | BI 409306 10 mg Tablet [EM] | EM subjects administered 2 immediate release tablets of 5 mg BI 409306 as a single dose (total dosage: 10 mg) orally with 240 mL water after an overnight fast of at least 10 hours. |
| FG005 | BI 409306 25 mg Tablet [EM] | EM subjects administered 5 immediate release tablets of 5 mg BI 409306 as a single dose (total dosage: 25 mg) orally with 240 mL water after an overnight fast of at least 10 hours. |
| FG006 | BI 409306 50 mg Tablet Followed by BI 409306 50mg PiB [EM] | EM subjects administered one single dose of 50 mg BI 409306 immediate release tablet orally with 240 mL water in period 1; followed by a washout period of 5 days; followed by one single dose of 50 mg BI 409306 powder in bottle (PiB) reconstituted for oral solution (0.5 mg/mL) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution administered orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 mL drinking water) after an overnight fast of at least 10 hours in period 2. |
| FG007 | Placebo to BI 409306 50 mg Tablet Followed by BI 409306 50 mg PiB [EM] | EM subject administered one single dose of placebo matching to the 50 mg BI 409306 film-coated tablet orally with 240 mL water in period 1; followed by a washout period of 5 days; followed by 50 mg BI 409306 powder in bottle (PiB) reconstituted for oral solution administered orally with 240 mL water in period 2, both after an overnight fast of at least 10 hours. |
| FG008 | BI 409306 100 mg Tablet [EM] | EM subjects administered 2 immediate release tablets of 50 mg BI 409306 as single dose (total dosage: 100 mg) orally with 240 mL water after an overnight fast of at least 10 hours. |
| FG009 | BI 409306 200 mg Tablet [EM] | EM subjects administered 1 immediate release tablet of 150 mg and 1 immediate release tablet of 50 mg of BI 409306 together as single dose (total dosage: 200 mg) orally with 240 mL water after an overnight fast of at least 10 hours. |
| FG010 | BI 409306 350 mg Tablet [EM] | EM subjects administered 2 immediate release tablet of 150 mg and 1 immediate release tablet of 50 mg of BI 409306 together as single dose (total dosage: 350 mg) orally with 240 mL water after an overnight fast of at least 10 hours. |
| FG011 | BI 409306 10 mg Tablet Followed by BI 409306 100mg Tablet [PM] | Poor metaboliser [PM] subjects administered 2 immediate release tablets of 5 mg BI 409306 as single dose (total dosage: 10 mg) orally with 240 mL water after an overnight fast of at least 10 hours in period 1; followed by washout period of 5 days; followed by 2 immediate release tablets of 50 mg BI 409306 administered as single dose (total dosage: 100 mg) orally with 240 mL water after an overnight fast of at least 10 hours in period 2. |
| Title | Milestones | Reasons Not Completed | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Overall Study |
|
Treated set (TS): The treated set includes all subjects who were dispensed study medication and were documented to have taken at least one dose of investigational treatment.
Not provided
| ID | Title | Description |
|---|---|---|
| BG000 | Placebo Matching to BI 409306 [EM and PM] | Extensive metaboliser [EM] subjects administered one single dose of placebo matching to BI 409306 powder in bottle (PiB) reconstituted for oral solution or one single dose of placebo matching to BI 409306 tablet orally with 240 mL water after an overnight fast of at least 10 hours. Poor metaboliser [PM] subjects administered one single dose of placebo matching to BI 409306 powder in bottle (PiB) reconstituted for oral solution or one single dose of placebo matching to BI 409306 tablet orally with 240 mL water after an overnight fast of at least 10 hours in period 1; followed by a washout period of 5 days; followed by one single dose of placebo to BI 409306 tablet administered orally with 240 mL water after an overnight fast of at least 10 hours in period 2. |
| Units | Counts |
|---|---|
| Participants |
|
| Title | Description | Population Description | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Denominator Units Selected | Denominators | Classes |
|---|---|---|---|---|---|---|---|---|---|
| Age, Continuous | Age at the time of signing informed consent form is presented. |
| Type | Title | Description | Population Description | Reporting Status | Anticipated Posting Date | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Time Frame | Units Analyzed | Denominator Units Selected | Arm/Group Information | Denominators | Classes | Analyses | ||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Primary | Percentage of Subjects With Drug-related Adverse Events | Percentage of subjects with investigator defined drug-related Adverse Events (AEs) | Treated set (TS):This set includes all subjects who were dispensed study medication and were documented to have taken at least one dose of investigational treatment. | Posted | Number | Percentage of subjects | From first drug administration until 30 days after last drug administration; up to 31 days. |
|
From first drug administration until 30 days after last drug administration; up to 31 days.
The safety analysis was based on treated set (TS). TS includes all subjects who were dispensed study medication and were documented to have taken at least one dose of investigational treatment.
Not provided
| ID | Title | Description | Deaths (Affected) | Deaths (At Risk) | Serious Events (Affected) | Serious Events (At Risk) | Other Events (Affected) | Other Events (At Risk) |
|---|---|---|---|---|---|---|---|---|
| EG000 | Placebo Matching to BI (Period 1) | Extensive metaboliser [EM] and poor metaboliser [PM] subjects randomized to placebo treatment (in period 1 only, if having 2 periods). |
Not provided
| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Extrasystoles | Cardiac disorders | MedDRA 14.1 | Systematic Assessment |
Not provided
| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| Boehringer Ingelheim, Call Centre | Boehringer Ingelheim | 1-800-243-0127 | clintriage.rdg@boehringer-ingelheim.com |
Not provided
| ID | Term |
|---|---|
| C000630656 | BI 409306 |
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
| Experimental |
EM subjects administered 2 immediate release tablets of 5 mg BI 409306 as a single dose (total dosage: 10 mg) orally with 240 mL water after an overnight fast of at least 10 hours. |
|
| BI 409306 25 mg Tablet [EM] | Experimental | EM subjects administered 5 immediate release tablets of 5 mg BI 409306 as a single dose (total dosage: 25 mg) orally with 240 mL water after an overnight fast of at least 10 hours. |
|
| BI 409306 50 mg Tablet followed by BI 409306 50mg PiB [EM] | Experimental | EM subjects administered one single dose of 50 mg BI 409306 immediate release tablet orally with 240 mL water in period 1; followed by a washout period of 5 days; followed by one single dose of 50 mg BI 409306 powder in bottle (PiB) reconstituted for oral solution (0.5 mg/mL) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution administered orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 mL drinking water) after an overnight fast of at least 10 hours in period 2. |
|
| BI 409306 100 mg Tablet [EM] | Experimental | EM subjects administered 2 immediate release tablets of 50 mg BI 409306 as single dose (total dosage: 100 mg) orally with 240 mL water after an overnight fast of at least 10 hours. |
|
| BI 409306 200 mg Tablet [EM] | Experimental | EM subjects administered 1 immediate release tablet of 150 mg and 1 immediate release tablet of 50 mg of BI 409306 together as single dose (total dosage: 200 mg) orally with 240 mL water after an overnight fast of at least 10 hours. |
|
| BI 409306 350 mg Tablet [EM] | Experimental | EM subjects administered 2 immediate release tablet of 150 mg and 1 immediate release tablet of 50 mg of BI 409306 together as single dose (total dosage: 350 mg) orally with 240 mL water after an overnight fast of at least 10 hours. |
|
| BI 409306 10 mg Tablet followed by BI 409306 100mg Tablet [PM] | Experimental | Poor metaboliser [PM] subjects administered 2 immediate release tablets of 5 mg BI 409306 as single dose (total dosage: 10 mg) orally with 240 mL water after an overnight fast of at least 10 hours in period 1; followed by washout period of 5 days; followed by 2 immediate release tablets of 50 mg BI 409306 administered as single dose (total dosage: 100 mg) orally with 240 mL water after an overnight fast of at least 10 hours in period 2. |
|
| Placebo matching to BI 409306 PiB | Placebo Comparator | Subjects administered one single dose of placebo matching to BI 409306 powder in bottle (PiB) after an overnight fast of at least 10 hours. |
|
| Placebo matching to BI 409306 film-coated tablet | Placebo Comparator | Subjects administered one single dose of placebo matching to the BI 409306 film-coated tablet (5 milligrams (mg), 50 mg, and 150 mg) orally with 240 mL water after an overnight fast of at least 10 hours. |
|
| Placebo |
| Drug |
Immediate release solid oral dosage (film-coated tablet) |
|
| BI 409306 | Drug | Immediate release solid oral dosage (film-coated tablet) |
|
| BI 409306 | Drug | solution for oral administration |
|
| Pharmacokinetic samples were collected at 2:00 (hour: minute) before 0.167, 0.333, 0.5, 0.75, 1:00, 1.50, 2:00, 2.50, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, and 24:00 hours after the drug administration. |
| Area Under the Concentration-time Curve of the BI 409306 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) | AUC0-∞, Area under the concentration-time curve of the BI 409306 in plasma over the time interval from 0 extrapolated to infinity. Pharmacokinetic samples were also collected at 48:00 and 72:00 hours after the drug administration for dose groups 10 mg onwards. | Pharmacokinetic samples were collected at 2:00 (hour: minute) before 0.167, 0.333, 0.5, 0.75, 1:00, 1.50, 2:00, 2.50, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, and 24:00 hours after the drug administration. |
| Maximum Measured Concentration of the BI 409306 in Plasma (Cmax) | Cmax, Maximum measured concentration of the BI 409306 in plasma. Pharmacokinetic samples were also collected at 48:00 and 72:00 hours after the drug administration for dose groups 10 mg onwards. | Pharmacokinetic samples were collected at 2:00 (hour: minute) before 0.167, 0.333, 0.5, 0.75, 1:00, 1.50, 2:00, 2.50, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, and 24:00 hours after the drug administration. |
| Amount of BI 409306 Eliminated in Urine From the Time Point t1 to Time Point t2 (Ae0-4) | Ae0-4, Amount of BI 409306 eliminated in urine from the time point t1(0) to time point t2(4). Urine samples were obtained 24:00 to 48:00 and 48:00 to 72:00 hours after oral administration were obtained only from dose group 10 mg onwards. | Urine samples were obtained pre-dose and sampling intervals 0:00 to 4:00, 4:00 to 8:00, 8:00 to 12:00 and 12:00 to 24:00 hours after oral administration. |
| BG001 | BI 409306 0.5 mg PiB [EM] | Extensive metaboliser [EM] subjects administered one single dose of 0.5 milligram (mg) BI 409306 powder in bottle (PiB) reconstituted for oral solution (0.5 mg /milliliter (mL)) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 mL drinking water) after an overnight fast of at least 10 hours. |
| BG002 | BI 409306 2 mg PiB [EM] | EM subjects administered one single dose of 2 mg BI 409306 PiB reconstituted for oral solution (0.5 mg/mL) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 milliliter drinking water) after an overnight fast of at least 10 hours. |
| BG003 | BI 409306 5 mg PiB Followed by BI 409306 5 mg Tablet [EM] | EM subjects administered one single dose of 5 mg BI 409306 powder in bottle (PiB) reconstituted for oral solution (0.5 mg/ mL) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 mL drinking water) after an overnight fast of at least 10 hours in period 1; followed by a washout period of 5 days; followed by one single dose of 5 mg BI 409306 immediate release tablet administered orally with 240 mL water after an overnight fast of at least 10 hours in period 2. |
| BG004 | BI 409306 10 mg Tablet [EM] | EM subjects administered 2 immediate release tablets of 5 mg BI 409306 as a single dose (total dosage: 10 mg) orally with 240 mL water after an overnight fast of at least 10 hours. |
| BG005 | BI 409306 25 mg Tablet [EM] | EM subjects administered 5 immediate release tablets of 5 mg BI 409306 as a single dose (total dosage: 25 mg) orally with 240 mL water after an overnight fast of at least 10 hours. |
| BG006 | BI 409306 50 mg Tablet Followed by BI 409306 50mg PiB [EM] | EM subjects administered one single dose of 50 mg BI 409306 immediate release tablet orally with 240 mL water in period 1; followed by a washout period of 5 days; followed by one single dose of 50 mg BI 409306 powder in bottle (PiB) reconstituted for oral solution (0.5 mg/mL) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution administered orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 mL drinking water) after an overnight fast of at least 10 hours in period 2. |
| BG007 | Placebo to BI 409306 50 mg Tablet Followed by BI 409306 50 mg PiB [EM] | EM subject administered one single dose of placebo matching to the 50 mg BI 409306 film-coated tablet orally with 240 mL water in period 1; followed by a washout period of 5 days; followed by 50 mg BI 409306 powder in bottle (PiB) reconstituted for oral solution administered orally with 240 mL water in period 2, both after an overnight fast of at least 10 hours. |
| BG008 | BI 409306 100 mg Tablet [EM] | EM subjects administered 2 immediate release tablets of 50 mg BI 409306 as single dose (total dosage: 100 mg) orally with 240 mL water after an overnight fast of at least 10 hours. |
| BG009 | BI 409306 200 mg Tablet [EM] | EM subjects administered 1 immediate release tablet of 150 mg and 1 immediate release tablet of 50 mg of BI 409306 together as single dose (total dosage: 200 mg) orally with 240 mL water after an overnight fast of at least 10 hours. |
| BG010 | BI 409306 350 mg Tablet [EM] | EM subjects administered 2 immediate release tablet of 150 mg and 1 immediate release tablet of 50 mg of BI 409306 together as single dose (total dosage: 350 mg) orally with 240 mL water after an overnight fast of at least 10 hours. |
| BG011 | BI 409306 10 mg Tablet Followed by BI 409306 100mg Tablet [PM] | Poor metaboliser [PM] subjects administered 2 immediate release tablets of 5 mg BI 409306 as single dose (total dosage: 10 mg) orally with 240 mL water after an overnight fast of at least 10 hours in period 1; followed by washout period of 5 days; followed by 2 immediate release tablets of 50 mg BI 409306 administered as single dose (total dosage: 100 mg) orally with 240 mL water after an overnight fast of at least 10 hours in period 2. |
| BG012 | Total | Total of all reporting groups |
TS
| Mean |
| Standard Deviation |
| Years |
|
| Sex: Female, Male | Number of subjects is categorized as Male or Female. | TS | Count of Participants | Participants |
|
| Race (NIH/OMB) | Number of subjects is categorized for race data. Ethnicity data were not collected. | TS | Count of Participants | Participants |
|
Extensive metaboliser [EM] and poor metaboliser [PM] subjects administered placebo in period 2 (after a wash out period of 5 days).
| OG002 | BI 409306 0.5 mg PiB [EM] | Extensive metaboliser [EM] subjects administered one single dose of 0.5 milligram (mg) BI 409306 powder in bottle (PiB) reconstituted for oral solution (0.5 mg /milliliter (mL)) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 mL drinking water) after an overnight fast of at least 10 hours. |
| OG003 | BI 409306 2 mg PiB [EM] | EM subjects administered one single dose of 2 mg BI 409306 PiB reconstituted for oral solution (0.5 mg/mL) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 milliliter drinking water) after an overnight fast of at least 10 hours. |
| OG004 | BI 409306 5 mg PiB [EM] | EM subjects administered one single dose of 5 mg BI 409306 powder in bottle (PiB) reconstituted for oral solution (0.5 mg/ mL) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 mL drinking water) after an overnight fast of at least 10 hours in period 1. |
| OG005 | BI 409306 5 mg Tablet [EM] | EM subjects administered one single dose of 5 mg BI 409306 immediate release tablet administered orally with 240 mL water after an overnight fast of at least 10 hours in period 2 (after a washout period of 5 days). |
| OG006 | BI 409306 10 mg Tablet [EM] | Subjects administered 2 single doses of 10 mg BI 409306 immediate release tablets orally with 240 mL water after an overnight fast of at least 10 hours in extensive metabolizer [EM] group. |
| OG007 | BI 409306 25 mg Tablet [EM] | Subjects administered a single dose of 25 mg BI 409306 immediate release tablets orally with 240 mL water after an overnight fast of at least 10 hours in extensive metabolizer [EM] group. |
| OG008 | BI 409306 50 mg Tablet [EM] | EM subjects administered one single dose of 50 mg BI 409306 immediate release tablet orally with 240 mL water in period 1. |
| OG009 | BI 409306 50 mg PiB [EM] | Subjects administered one single dose 50 ml BI 409306 powder in bottle (PiB) reconstituted for oral solution (0.5 ml/mL) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 mL drinking water) after washout period of 5 days both after an overnight fast of at least 10 hours in extensive metabolizer [EM] group. |
| OG010 | BI 409306 100 mg Tablet [EM] | Subjects administered 2 single doses of 100 mg BI 409306 immediate release tablets orally with 240 mL water after an overnight fast of at least 10 hours in extensive metabolizer [EM] group. |
| OG011 | BI 409306 200 mg Tablet [EM] | Subjects administered a single dose of 200 mg BI 409306 immediate release tablets orally with 240 mL water after an overnight fast of at least 10 hours in extensive metabolizer [EM] group. |
| OG012 | BI 409306 350 mg Tablet [EM] | Subjects administered a single dose of 350 mg BI 409306 immediate release tablets orally with 240 mL water after an overnight fast of at least 10 hours in extensive metabolizer [EM] group. |
| OG013 | BI 409306 10 mg Tablet [PM] | Poor metaboliser [PM] subjects administered 2 immediate release tablets of 5 mg BI 409306 as single dose (total dosage: 10 mg) orally with 240 mL water after an overnight fast of at least 10 hours in period 1. |
| OG014 | BI 409306 100 mg Tablet [PM] | PM subjects administered 2 immediate release tablets of 50 mg BI 409306 as single dose (total dosage: 100 mg) orally with 240 mL water after an overnight fast of at least 10 hours in period 2 (after a washout period of 5 days). |
|
|
| Primary | Percentage of Subjects With Clinical Relevant Abnormalities for Physical Examination, Vital Signs, Clinical Laboratory Tests, Oral Body Temperature and ECG | Percentage of subjects with Clinical Relevant abnormalities for Physical examination, Vital Signs blood pressure (BP), pulse rate (PR) respiratory rate (RR), orthostatic test), Clinical laboratory tests (haematology, clinical chemistry and urinalysis), Oral body temperature and ECG were reported. | Treated set (TS):This set includes all subjects who were dispensed study medication and were documented to have taken at least one dose of investigational treatment. | Posted | Number | Percentage of subjects | Day 4 |
|
|
|
| Primary | Percentage of Subjects Per Category for Assessment of Tolerability by Investigator | The investigator assessed global clinical assessment and tolerability of BI 409306 were reported in possible categories were 'good', 'satisfactory', 'not satisfactory', and 'bad'. | Treated set (TS):This set includes all subjects who were dispensed study medication and were documented to have taken at least one dose of investigational treatment. | Posted | Number | Percentage of subjects | Day 4 |
|
|
|
| Primary | Change From Baseline in Bond & Lader (B&L) Visual Analogue Scales (VAS) | The B&L VAS scores were calculated from 16 item with each has a score range from 0 to 10 [cm]. The score of each of the 3 categories of effects ("alertness", "calmness", and "contentment") is a weighted average of the scores from the 16 items. The VAS score for alertness/calmness/contentment ranges from 0 to 10 (more alertness/calmness/contentment). The B&L VAS data was analysed descriptively (change from baseline at 24 hour). The VAS assessment 2 h before drug administration was considered as baseline. | Treated set (TS):This set includes all subjects who were dispensed study medication and were documented to have taken at least one dose of investigational treatment. | Posted | Least Squares Mean | Standard Deviation | Score on a scale | At 24 hours |
|
|
|
| Secondary | Area Under the Concentration-time Curve of the BI 409306 in Plasma From Time 0 to Time of Last Quantifiable Data Point (AUC0-24) | AUC0-24, Area under the concentration-time curve of the BI 409306 in plasma over the time interval from 0 to the time of the last quantifiable data point is presented as geometric mean (gMean) and geometric coefficient of variation (gCV%). Pharmacokinetic samples were also collected at 48:00 and 72:00 hours after the drug administration for dose groups 10 mg onwards. | Per protocol set for evaluation of PK (PPS-PK): This set included all evaluable subjects of the treated set who had no important protocol violations relevant to the evaluation of PK, who had no pre-dose value greater than 5% of Cmax and who did not vomit or had diarrhoea at or before two times median tmax. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanomol*hour/Litre [nmol*h/L] | Pharmacokinetic samples were collected at 2:00 (hour: minute) before 0.167, 0.333, 0.5, 0.75, 1:00, 1.50, 2:00, 2.50, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, and 24:00 hours after the drug administration. |
|
|
|
| Secondary | Area Under the Concentration-time Curve of the BI 409306 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) | AUC0-∞, Area under the concentration-time curve of the BI 409306 in plasma over the time interval from 0 extrapolated to infinity. Pharmacokinetic samples were also collected at 48:00 and 72:00 hours after the drug administration for dose groups 10 mg onwards. | Per protocol set for evaluation of PK (PPS-PK): This set included all evaluable subjects of the treated set who had no important protocol violations relevant to the evaluation of PK, who had no pre-dose value greater than 5% of Cmax and who did not vomit or had diarrhoea at or before two times median tmax. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanomol*hour/Litre [nmol*h/L] | Pharmacokinetic samples were collected at 2:00 (hour: minute) before 0.167, 0.333, 0.5, 0.75, 1:00, 1.50, 2:00, 2.50, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, and 24:00 hours after the drug administration. |
|
|
|
| Secondary | Maximum Measured Concentration of the BI 409306 in Plasma (Cmax) | Cmax, Maximum measured concentration of the BI 409306 in plasma. Pharmacokinetic samples were also collected at 48:00 and 72:00 hours after the drug administration for dose groups 10 mg onwards. | Per protocol set for evaluation of PK (PPS-PK): This set included all evaluable subjects of the treated set who had no important protocol violations relevant to the evaluation of PK, who had no pre-dose value greater than 5% of Cmax and who did not vomit or had diarrhoea at or before two times median tmax. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanomol/Litre (nmol/L) | Pharmacokinetic samples were collected at 2:00 (hour: minute) before 0.167, 0.333, 0.5, 0.75, 1:00, 1.50, 2:00, 2.50, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 14:00, and 24:00 hours after the drug administration. |
|
|
|
| Secondary | Amount of BI 409306 Eliminated in Urine From the Time Point t1 to Time Point t2 (Ae0-4) | Ae0-4, Amount of BI 409306 eliminated in urine from the time point t1(0) to time point t2(4). Urine samples were obtained 24:00 to 48:00 and 48:00 to 72:00 hours after oral administration were obtained only from dose group 10 mg onwards. | Per protocol set for evaluation of PK (PPS-PK): This set included all evaluable subjects of the treated set who had no important protocol violations relevant to the evaluation of PK, who had no pre-dose value greater than 5% of Cmax and who did not vomit or had diarrhoea at or before two times median tmax. Only participants with non-missing outcomes were included in the analysis. | Posted | Geometric Mean | Geometric Coefficient of Variation | nanomol [nmol] | Urine samples were obtained pre-dose and sampling intervals 0:00 to 4:00, 4:00 to 8:00, 8:00 to 12:00 and 12:00 to 24:00 hours after oral administration. |
|
|
|
| 0 |
| 20 |
| 0 |
| 20 |
| 2 |
| 20 |
| EG001 | Placebo Matching to BI (Period 2) | Extensive metaboliser [EM] and poor metaboliser [PM] subjects administered placebo in period 2 (after a wash out period of 5 days). | 0 | 4 | 0 | 4 | 1 | 4 |
| EG002 | BI 409306 0.5 mg PiB [EM] | Extensive metaboliser [EM] subjects administered one single dose of 0.5 milligram (mg) BI 409306 powder in bottle (PiB) reconstituted for oral solution (0.5 mg /milliliter (mL)) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 mL drinking water) after an overnight fast of at least 10 hours. | 0 | 6 | 0 | 6 | 0 | 6 |
| EG003 | BI 409306 2 mg PiB [EM] | EM subjects administered one single dose of 2 mg BI 409306 PiB reconstituted for oral solution (0.5 mg/mL) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 milliliter drinking water) after an overnight fast of at least 10 hours. | 0 | 6 | 0 | 6 | 2 | 6 |
| EG004 | BI 409306 5 mg PiB [EM] | EM subjects administered one single dose of 5 mg BI 409306 powder in bottle (PiB) reconstituted for oral solution (0.5 mg/ mL) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 mL drinking water) after an overnight fast of at least 10 hours in period 1. | 0 | 6 | 0 | 6 | 0 | 6 |
| EG005 | BI 409306 5 mg Tablet [EM] | EM subjects administered one single dose of 5 mg BI 409306 immediate release tablet administered orally with 240 mL water after an overnight fast of at least 10 hours in period 2 (after a washout period of 5 days). | 0 | 6 | 0 | 6 | 1 | 6 |
| EG006 | BI 409306 10 mg Tablet [EM] | EM subjects administered 2 immediate release tablets of 5 mg BI 409306 as a single dose (total dosage: 10 mg) orally with 240 mL water after an overnight fast of at least 10 hours. | 0 | 6 | 0 | 6 | 0 | 6 |
| EG007 | BI 409306 25 mg Tablet [EM] | EM subjects administered 5 immediate release tablets of 5 mg BI 409306 as a single dose (total dosage: 25 mg) orally with 240 mL water after an overnight fast of at least 10 hours. | 0 | 6 | 0 | 6 | 0 | 6 |
| EG008 | BI 409306 50 mg Tablet [EM] | EM subjects administered one single dose of 50 mg BI 409306 immediate release tablet orally with 240 mL water in period 1. | 0 | 6 | 0 | 6 | 2 | 6 |
| EG009 | BI 409306 50mg PiB [EM] | EM subjects administered one single dose of 50 mg BI 409306 powder in bottle (PiB) reconstituted for oral solution (0.5 mg/mL) in a volume of 80 mL of the solvent containing aqueous 0.5% tartaric acid solution orally with 240 mL water (160 mL containing the respective diluted volume of reconstituted solution and 80 mL drinking water) after an overnight fast of at least 10 hours in period 2 (after a washout period of 5 days). | 0 | 8 | 0 | 8 | 0 | 8 |
| EG010 | BI 409306 100 mg Tablet [EM] | EM subjects administered 2 immediate release tablets of 50 mg BI 409306 as single dose (total dosage: 100 mg) orally with 240 mL water after an overnight fast of at least 10 hours. | 0 | 5 | 0 | 5 | 2 | 5 |
| EG011 | BI 409306 200 mg Tablet [EM] | EM subjects administered 1 immediate release tablet of 150 mg and 1 immediate release tablet of 50 mg of BI 409306 together as single dose (total dosage: 200 mg) orally with 240 mL water after an overnight fast of at least 10 hours. | 0 | 6 | 0 | 6 | 4 | 6 |
| EG012 | BI 409306 350 mg Tablet [EM] | EM subjects administered 2 immediate release tablet of 150 mg and 1 immediate release tablet of 50 mg of BI 409306 together as single dose (total dosage: 350 mg) orally with 240 mL water after an overnight fast of at least 10 hours. | 0 | 6 | 0 | 6 | 4 | 6 |
| EG013 | BI 409306 10 mg Tablet [PM] | Poor metaboliser [PM] subjects administered 2 immediate release tablets of 5 mg BI 409306 as single dose (total dosage: 10 mg) orally with 240 mL water after an overnight fast of at least 10 hours in period 1. | 0 | 6 | 0 | 6 | 3 | 6 |
| EG014 | BI 409306 100 mg Tablet [PM] | PM subjects administered 2 immediate release tablets of 50 mg BI 409306 as single dose (total dosage: 100 mg) orally with 240 mL water after an overnight fast of at least 10 hours in period 2 (after a washout period of 5 days). | 0 | 6 | 0 | 6 | 3 | 6 |
| Palpitations | Cardiac disorders | MedDRA 14.1 | Systematic Assessment |
|
| Sinus tachycardia | Cardiac disorders | MedDRA 14.1 | Systematic Assessment |
|
| Chromatopsia | Eye disorders | MedDRA 14.1 | Systematic Assessment |
|
| Photophobia | Eye disorders | MedDRA 14.1 | Systematic Assessment |
|
| Photopsia | Eye disorders | MedDRA 14.1 | Systematic Assessment |
|
| Vision blurred | Eye disorders | MedDRA 14.1 | Systematic Assessment |
|
| Diarrhoea | Gastrointestinal disorders | MedDRA 14.1 | Systematic Assessment |
|
| Dry mouth | Gastrointestinal disorders | MedDRA 14.1 | Systematic Assessment |
|
| Nausea | Gastrointestinal disorders | MedDRA 14.1 | Systematic Assessment |
|
| Feeling hot | General disorders | MedDRA 14.1 | Systematic Assessment |
|
| Nasopharyngitis | Infections and infestations | MedDRA 14.1 | Systematic Assessment |
|
| Back pain | Musculoskeletal and connective tissue disorders | MedDRA 14.1 | Systematic Assessment |
|
| Dizziness | Nervous system disorders | MedDRA 14.1 | Systematic Assessment |
|
| Headache | Nervous system disorders | MedDRA 14.1 | Systematic Assessment |
|
| Paraesthesia | Nervous system disorders | MedDRA 14.1 | Systematic Assessment |
|
| Parosmia | Nervous system disorders | MedDRA 14.1 | Systematic Assessment |
|
| Presyncope | Nervous system disorders | MedDRA 14.1 | Systematic Assessment |
|
| Somnolence | Nervous system disorders | MedDRA 14.1 | Systematic Assessment |
|
Not provided
Not provided
Not provided
| Satisfactory |
|
| Not satisfactory |
|
| Bad |
|
| Not assessable |
|
| Contentment |
|
| Calmness |
|