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| ID | Type | Description | Link |
|---|---|---|---|
| 2019-002358-22 | EudraCT Number |
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The main objectives of this trial are to investigate safety, tolerability and pharmacokinetics (PK) of BI 474121 in healthy male subjects following oral administration of single rising doses.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| SRD: Placebo matching BI 474121 oral solution (OS) | Placebo Comparator | This arm comprises all placebo treated participants of the single rising dose (SRD) part treated with an oral solution (placebo treated participants of the two lowest dose group (DG)s). Participants receiving placebo were equally distributed across dose groups. A single dose of BI 474121 matching placebo powder for oral solution was administered after an overnight fast together with 240 milliliter (mL) of water to participants who were in a standing position. |
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| SRD: Placebo matching BI 474121 tablet (T) | Placebo Comparator | This arm comprises all placebo treated participants of the SRD part treated with a tablet (placebo treated participants of the five upper DGs). Participants receiving placebo were equally distributed across dose groups. A single dose of BI 474121 matching placebo tablet was administered after an overnight fast together with 240 mL of water to subjects who were in a standing position. |
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| SRD: 0.25 milligram (mg) BI 474121 - OS | Experimental | A single dose of 0.25 mg BI 474121 was solved in 0.5 mL of water and was administered after an overnight fast together with 240 mL of water to participants who were in a standing position. |
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| SRD: 1 mg BI 474121 - OS | Experimental | A single dose of 1 mg BI 474121 was solved in 2mL of water and was administered after an overnight fast together with 240 mL of water to participants who were in a standing position. |
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| BI 474121 tablet | Drug | BI 474121 tablet |
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| Measure | Description | Time Frame |
|---|---|---|
| Single Rising Dose (SRD): Percentage of Subjects With Drug-related Adverse Events. | For assessment of safety and tolerability of BI 474121 the percentage of participants with drug-related adverse events (AE) was calculated. All AEs occurring between first drug intake till 7 days after last drug intake were assigned to the randomised treatment. | From drug administration until 7 days after drug administration, 7 days. |
| Bioavailability (BA): Area Under the Concentration-time Curve of BI 474121 in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz). | Area under the concentration-time curve of BI 474121 in plasma over the time interval from 0 to the last quantifiable data point (AUC0-tz) was analyzed after single dose administration of BI 474121 as: an oral solution in fasted conditions (reference treatment), an uncoated tablet in fed conditions (treatment 1) and an uncoated tablet in fasted conditions (treatment 2). The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis. | Within 3 hours (h) before drug administration and 15 minutes (min), 30min, 1h, 1h 30min, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, and 96h after drug administration. |
| BA: Maximum Measured Concentration of BI 474121 in Plasma (Cmax ) | Maximum measured concentration of of BI 474121 in plasma (Cmax). The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis. | Within 3 hours (h) before drug administration and 15 minutes (min), 30min, 1h, 1h 30min, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, and 96h after drug administration. |
| Measure | Description | Time Frame |
|---|---|---|
| SRD: Area Under the Concentration-time Curve of BI 474121 in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz). | Area under the concentration-time curve of BI 474121 in plasma over the time interval from 0 to the last quantifiable data point (AUC0-tz) was analyzed after single dose administration of BI 474121. The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis. |
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Inclusion criteria:
Exclusion criteria:
Highly effective methods of birth control are:
Male subject is sexually abstinent
Male subjects is vasectomised (vasectomy at least 1 year prior to enrolment), plus condom in male subject
Use of intrauterine device (IUD) or intrauterine hormone-releasing system (IUS)
Use of progestogen-only hormonal contraception by female partner that inhibits ovulation (only injectables or implants), plus condom in male subject
Use of combined (estrogen and progestogen containing) hormonal contraception by female partner that prevents ovulation (oral, intravaginal or transdermal), plus condom in male subject
Female partner is surgically sterilised (including hysterectomy)
Female partner is postmenopausal, defined as no menses for 1 year without an alternative medical cause (in questionable cases a blood sample with FSH above 40 U/L and estradiol below 30 ng/L is confirmatory) Sperm donation is not allowed from the time point of drug administration until 30 days thereafter.
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Humanpharmakologisches Zentrum Biberach | Biberach | 88397 | Germany |
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| Label | URL |
|---|---|
| Related Info | View source |
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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
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All subjects were screened for eligibility prior to participation in the trial. Participants attended a specialist site which ensured that they (the subjects) strictly met all inclusion and none of the exclusion criteria. Participants were not to be allocated to a treatment group if any of the entry criteria were violated.
This was a two part trial in healthy male subjects: A single-blind, randomized, placebo-controlled single rising dose (SRD) scheme of BI 474121 (=SRD part); An open-label, randomized, 6-sequence cross-over to assess bioavailability (BA) of BI 474121 as oral solution (fasted state), tablet (fasted state) and tablet (fed state) (=BA part).
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| ID | Title | Description |
|---|---|---|
| FG000 | SRD: Placebo Matching BI 474121 Oral Solution (OS) | This arm comprises all placebo treated participants of the single rising dose (SRD) part treated with an oral solution (placebo treated participants of the two lowest dose group (DG)s). Participants receiving placebo were equally distributed across dose groups. A single dose of BI 474121 matching placebo powder for oral solution was administered after an overnight fast together with 240 milliliter (mL) of water to participants who were in a standing position. |
| Title | Milestones | Reasons Not Completed | |||||
|---|---|---|---|---|---|---|---|
| Treatment Period 1 (SRD and BA Part) |
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| Type | Includes Protocol | Includes SAP | Includes ICF | Document Label | Document Date | Document Uploaded Date | Document File Name |
|---|---|---|---|---|---|---|---|
| Prot | Yes | No | No | Study Protocol | Oct 8, 2020 | Jul 20, 2023 |
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| SRD: 2.5 mg BI 474121 - T | Experimental | A single dose of 2.5 mg BI 474121 was administered as 1 uncoated 2.5 mg tablet after an overnight fast together with 240 mL of water to participants who were in a standing position. |
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| SRD: 5 mg BI 474121 - T | Experimental | A single dose of 5.0 mg BI 474121 was administered as 2 uncoated 2.5 mg tablets after an overnight fast together with 240 mL of water to participants who were in a standing position. |
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| SRD: 10 mg BI 474121 - T | Experimental | A single dose of 10.0 mg BI 474121 was administered as 1 uncoated 10.0 mg tablet after an overnight fast together with 240 mL of water to participants who were in a standing position. |
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| SRD: 20 mg BI 474121 - T | Experimental | A single dose of 20.0 mg BI 474121 was administered as 2 uncoated 10.0 mg tablets after an overnight fast together with 240 mL of water to participants who were in a standing position. |
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| SRD: 40 mg BI 474121 - T | Experimental | A single dose of 40.0 mg BI 474121 was administered as 4 uncoated 10.0 mg tablets after an overnight fast together with 240 mL of water to participants who were in a standing position. |
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| BA: BI 474121 10 mg as: OS fasted (Reference (R)) / T fasted (T2) / T fed (T1) | Experimental | Participants received a single dose of 10.0 mg BI 474121 in each period, in period 1 as oral solution solved in 20 mL of water with 240 mL of water after an overnight fast (Reference (R)), in period 2 as 1 uncoated tablet with 240 mL of water after an overnight fast (Test 2 (T2)) and in period 3 as 1 uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water (Test 1 (T1)). Between periods was a wash-out period of at least 7 days. |
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| BA: BI 474121 10 mg as: R / T1 / T2 | Experimental | Participants received a single dose of 10.0 mg BI 474121 in each period, in period 1 as oral solution solved in 20 mL of water with 240 mL of water after an overnight fast (R), in period 2 as 1 uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water (T1) and in period 3 as 1 uncoated tablet with 240 mL of water after an overnight fast (T2). Between periods was a wash-out period of at least 7 days. |
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| BA: BI 474121 10mg as: T2 / R / T1 | Experimental | Participants received a single dose of 10.0 mg BI 474121 in each period, in period 1 as 1 uncoated tablet with 240 mL of water after an overnight fast (T2), in period 2 as oral solution solved in 20 mL of water with 240 mL of water after an overnight fast (R) and in period 3 as 1 uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water (T1). Between periods was a wash-out period of at least 7 days. |
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| BA: BI 474121 10mg as: T2 / T1 / R | Experimental | Participants received a single dose of 10.0 mg BI 474121 in each period, in period 1 as 1 uncoated tablet with 240 mL of water after an overnight fast (T2), in period 2 as 1 uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water (T1) and in period 3 as oral solution solved in 20 mL water with 240 mL of water after an overnight fast (R). Between periods was a wash-out period of at least 7 days. |
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| BA: BI 474121 10mg: T1 / R / T2 | Experimental | Participants received a single dose of 10.0 mg BI 474121 in each period, in period 1 as 1 uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water (T1), in period 2 as oral solution solved in 20 mL of water with 240 mL of water after an overnight fast (R) and in period 3 as 1 uncoated tablet with 240 mL of water after an overnight fast (T2). Between periods was a wash-out period of at least 7 days. |
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| BA: BI 474121 10mg: T1 / T2 / R | Experimental | Participants received a single dose of 10.0 mg BI 474121 in each period, in period 1 as 1 uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water (T1), in period 2 as 1 uncoated tablet with 240 mL of water after an overnight fast (T2) and in period 3 as oral solution solved in 20 mL of water with 240 mL of water after an overnight fast (R). Between periods was a wash-out period of at least 7 days. |
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| Placebo tablet | Drug | Placebo tablet |
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| BI 474121 oral solution | Drug | BI 474121 oral solution |
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| Placebo solution | Drug | Placebo solution |
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| Within 3 hours (h) before drug administration and 15 minutes (min), 30min, 1h, 1h 30min, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, and 96h after drug administration. |
| SRD: Maximum Measured Concentration of of BI 474121 in Plasma (Cmax). | Maximum measured concentration of of BI 474121 in plasma (Cmax). The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis. | Within 3 hours (h) before drug administration and 15 minutes (min), 30min, 1h, 1h 30min, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, and 96h after drug administration. |
| BA: Area Under the Concentration-time Curve of BI 474121 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞). | Area under the concentration-time curve of BI 474121 in plasma over the time interval from 0 extrapolated to infinity (AUC0-∞). The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis. | Within 3 hours (h) before drug administration and 15 minutes (min), 30min, 1h, 1h 30min, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, and 96h after drug administration. |
| FG001 | SRD: Placebo Matching BI 474121 Tablet (T) | This arm comprises all placebo treated participants of the SRD part treated with a tablet (placebo treated participants of the five upper DGs). Participants receiving placebo were equally distributed across dose groups. A single dose of BI 474121 matching placebo tablet was administered after an overnight fast together with 240 mL of water to subjects who were in a standing position. |
| FG002 | SRD: 0.25 Milligram (mg) BI 474121 - OS | A single dose of 0.25 mg BI 474121 was solved in 0.5 mL of water and was administered after an overnight fast together with 240 mL of water to participants who were in a standing position. |
| FG003 | SRD: 1 mg BI 474121 - OS | A single dose of 1 mg BI 474121 was solved in 2mL of water and was administered after an overnight fast together with 240 mL of water to participants who were in a standing position. |
| FG004 | SRD: 2.5 mg BI 474121 - T | A single dose of 2.5 mg BI 474121 was administered as 1 uncoated 2.5 mg tablet after an overnight fast together with 240 mL of water to participants who were in a standing position. |
| FG005 | SRD: 5 mg BI 474121 - T | A single dose of 5.0 mg BI 474121 was administered as 2 uncoated 2.5 mg tablets after an overnight fast together with 240 mL of water to participants who were in a standing position. |
| FG006 | SRD: 10 mg BI 474121 - T | A single dose of 10.0 mg BI 474121 was administered as 1 uncoated 10.0 mg tablet after an overnight fast together with 240 mL of water to participants who were in a standing position. |
| FG007 | SRD: 20 mg BI 474121 - T | A single dose of 20.0 mg BI 474121 was administered as 2 uncoated 10.0 mg tablets after an overnight fast together with 240 mL of water to participants who were in a standing position. |
| FG008 | SRD: 40 mg BI 474121 - T | A single dose of 40.0 mg BI 474121 was administered as 4 uncoated 10.0 mg tablets after an overnight fast together with 240 mL of water to participants who were in a standing position. |
| FG009 | BA: BI 474121 10 mg as: OS Fasted (Reference (R)) / T Fasted (T2) / T Fed (T1) | Participants received a single dose of 10.0 mg BI 474121 in each period, in period 1 as oral solution solved in 20 mL of water with 240 mL of water after an overnight fast (Reference (R)), in period 2 as 1 uncoated tablet with 240 mL of water after an overnight fast (Test 2 (T2)) and in period 3 as 1 uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water (Test 1 (T1)). Between periods was a wash-out period of at least 7 days. |
| FG010 | BA: BI 474121 10 mg as: R / T1 / T2 | Participants received a single dose of 10.0 mg BI 474121 in each period, in period 1 as oral solution solved in 20 mL of water with 240 mL of water after an overnight fast (R), in period 2 as 1 uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water (T1) and in period 3 as 1 uncoated tablet with 240 mL of water after an overnight fast (T2). Between periods was a wash-out period of at least 7 days. |
| FG011 | BA: BI 474121 10mg as: T2 / R / T1 | Participants received a single dose of 10.0 mg BI 474121 in each period, in period 1 as 1 uncoated tablet with 240 mL of water after an overnight fast (T2), in period 2 as oral solution solved in 20 mL of water with 240 mL of water after an overnight fast (R) and in period 3 as 1 uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water (T1). Between periods was a wash-out period of at least 7 days. |
| FG012 | BA: BI 474121 10mg as: T2 / T1 / R | Participants received a single dose of 10.0 mg BI 474121 in each period, in period 1 as 1 uncoated tablet with 240 mL of water after an overnight fast (T2), in period 2 as 1 uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water (T1) and in period 3 as oral solution solved in 20 mL water with 240 mL of water after an overnight fast (R). Between periods was a wash-out period of at least 7 days. |
| FG013 | BA: BI 474121 10mg: T1 / R / T2 | Participants received a single dose of 10.0 mg BI 474121 in each period, in period 1 as 1 uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water (T1), in period 2 as oral solution solved in 20 mL of water with 240 mL of water after an overnight fast (R) and in period 3 as 1 uncoated tablet with 240 mL of water after an overnight fast (T2). Between periods was a wash-out period of at least 7 days. |
| FG014 | BA: BI 474121 10mg: T1 / T2 / R | Participants received a single dose of 10.0 mg BI 474121 in each period, in period 1 as 1 uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water (T1), in period 2 as 1 uncoated tablet with 240 mL of water after an overnight fast (T2) and in period 3 as oral solution solved in 20 mL of water with 240 mL of water after an overnight fast (R). Between periods was a wash-out period of at least 7 days. |
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| NOT COMPLETED |
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| Wash-out Period 1 (BA Part Only) |
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| Treatment Period 2 (BA Part Only) |
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| Wash-out Period 2 (BA Part Only) |
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| Treatment Period 3 (BA Part Only) |
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Treated set (TS) The TS included all participants who were randomized and treated with at least 1 dose of trial drug. The treatment assignment was determined based on the first treatment the participant received. The TS was used for safety analyses.
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| ID | Title | Description |
|---|---|---|
| BG000 | SRD: Placebo Matching BI 474121 Oral Solution (OS) | This arm comprises all placebo treated participants of the single rising dose (SRD) part treated with an oral solution (placebo treated participants of the two lowest dose group (DG)s). Participants receiving placebo were equally distributed across dose groups. A single dose of BI 474121 matching placebo powder for oral solution was administered after an overnight fast together with 240 milliliter (mL) of water to participants who were in a standing position. |
| BG001 | SRD: Placebo Matching BI 474121 Tablet (T) | This arm comprises all placebo treated participants of the SRD part treated with a tablet (placebo treated participants of the five upper DGs). Participants receiving placebo were equally distributed across dose groups. A single dose of BI 474121 matching placebo tablet was administered after an overnight fast together with 240 mL of water to subjects who were in a standing position. |
| BG002 | SRD: 0.25 Milligram (mg) BI 474121 - OS | A single dose of 0.25 mg BI 474121 was solved in 0.5 mL water and was administered after an overnight fast together with 240 mL of water to participants who were in a standing position. |
| BG003 | SRD: 1 mg BI 474121 - OS | A single dose of 1 mg BI 474121 was solved in 2mL water and was administered after an overnight fast together with 240 mL of water to participants who were in a standing position. |
| BG004 | SRD: 2.5 mg BI 474121 - T | A single dose of 2.5 mg BI 474121 was administered as 1 uncoated 2.5 mg tablet after an overnight fast together with 240 mL of water to participants who were in a standing position. |
| BG005 | SRD: 5 mg BI 474121 - T | A single dose of 5.0 mg BI 474121 was administered as 2 uncoated 2.5 mg tablets after an overnight fast together with 240 mL of water to participants who were in a standing position. |
| BG006 | SRD: 10 mg BI 474121 - T | A single dose of 10.0 mg BI 474121 was administered as 1 uncoated 10.0 mg tablet after an overnight fast together with 240 mL of water to participants who were in a standing position. |
| BG007 | SRD: 20 mg BI 474121 - T | A single dose of 20.0 mg BI 474121 was administered as 2 uncoated 10.0 mg tablets after an overnight fast together with 240 mL of water to participants who were in a standing position. |
| BG008 | SRD: 40 mg BI 474121 - T | A single dose of 40.0 mg BI 474121 was administered as 4 uncoated 10.0 mg tablets after an overnight fast together with 240 mL of water to participants who were in a standing position. |
| BG009 | BA: BI 474121 10 mg as: OS Fasted (Reference (R)) / T Fasted (T2) / T Fed (T1) | Participants received a single dose of 10.0 mg BI 474121 in each period, in period 1 as oral solution solved in 20 mL of water with 240 mL of water after an overnight fast (Reference (R)), in period 2 as 1 uncoated tablet with 240 mL of water after an overnight fast (Test 2 (T2)) and in period 3 as 1 uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water (Test 1 (T1)). Between periods was a wash-out period of at least 7 days. |
| BG010 | BA: BI 474121 10 mg as: R / T1 / T2 | Participants received a single dose of 10.0 mg BI 474121 in each period, in period 1 as oral solution solved in 20 mL of water with 240 mL of water after an overnight fast (R), in period 2 as 1 uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water (T1) and in period 3 as 1 uncoated tablet with 240 mL of water after an overnight fast (T2). Between periods was a wash-out period of at least 7 days. |
| BG011 | BA: BI 474121 10mg as: T2 / R / T1 | Participants received a single dose of 10.0 mg BI 474121 in each period, in period 1 as 1 uncoated tablet with 240 mL of water after an overnight fast (T2), in period 2 as oral solution solved in 20 mL of water with 240 mL of water after an overnight fast (R) and in period 3 as 1 uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water (T1). Between periods was a wash-out period of at least 7 days. |
| BG012 | BA: BI 474121 10mg as: T2 / T1 / R | Participants received a single dose of 10.0 mg BI 474121 in each period, in period 1 as 1 uncoated tablet with 240 mL of water after an overnight fast (T2), in period 2 as 1 uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water (T1) and in period 3 as oral solution solved in 20 mL water with 240 mL of water after an overnight fast (R). Between periods was a wash-out period of at least 7 days. |
| BG013 | BA: BI 474121 10mg: T1 / R / T2 | Participants received a single dose of 10.0 mg BI 474121 in each period, in period 1 as 1 uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water (T1), in period 2 as oral solution solved in 20 mL of water with 240 mL of water after an overnight fast (R) and in period 3 as 1 uncoated tablet with 240 mL of water after an overnight fast (T2). Between periods was a wash-out period of at least 7 days. |
| BG014 | BA: BI 474121 10mg: T1 / T2 / R | Participants received a single dose of 10.0 mg BI 474121 in each period, in period 1 as 1 uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water (T1), in period 2 as 1 uncoated tablet with 240 mL of water after an overnight fast (T2) and in period 3 as oral solution solved in 20 mL of water with 240 mL of water after an overnight fast (R). Between periods was a wash-out period of at least 7 days. |
| BG015 | Total | Total of all reporting groups |
| Units | Counts |
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| Participants |
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| Title | Description | Population Description | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Denominator Units Selected | Denominators | Classes | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Age, Continuous | Mean | Standard Deviation | Years |
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| Sex/Gender, Customized | Count of Participants | Participants |
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| Ethnicity (NIH/OMB) | Count of Participants | Participants |
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| Race (NIH/OMB) | Count of Participants | Participants |
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| 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 | ||||||||||||||||||||||||||||||||||||||||||||
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| Primary | Single Rising Dose (SRD): Percentage of Subjects With Drug-related Adverse Events. | For assessment of safety and tolerability of BI 474121 the percentage of participants with drug-related adverse events (AE) was calculated. All AEs occurring between first drug intake till 7 days after last drug intake were assigned to the randomised treatment. | Treated set (TS) The TS included all participants who were randomized and treated with at least 1 dose of trial drug. The treatment assignment was determined based on the first treatment the participant received. The TS was used for safety analyses. | Posted | Number | Percentage of participants | From drug administration until 7 days after drug administration, 7 days. |
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| Primary | Bioavailability (BA): Area Under the Concentration-time Curve of BI 474121 in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz). | Area under the concentration-time curve of BI 474121 in plasma over the time interval from 0 to the last quantifiable data point (AUC0-tz) was analyzed after single dose administration of BI 474121 as: an oral solution in fasted conditions (reference treatment), an uncoated tablet in fed conditions (treatment 1) and an uncoated tablet in fasted conditions (treatment 2). The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis. | Pharmacokinetic parameter analysis set (PKS): The PKS included all participants in the TS who provided at least 1 primary or secondary pharmacokinetic (PK) endpoint that were not excluded due to a protocol deviation relevant to the evaluation of PK or due to PK non-evaluability. Thus, a participant was included in the PKS, even if he contributed only 1 PK parameter value for 1 period to the statistical assessment. Descriptive and model-based analyses of PK parameters were based on the PKS. | Posted | Geometric Mean | Geometric Coefficient of Variation | Hour times nanomole per litre | Within 3 hours (h) before drug administration and 15 minutes (min), 30min, 1h, 1h 30min, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, and 96h after drug administration. |
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| Primary | BA: Maximum Measured Concentration of BI 474121 in Plasma (Cmax ) | Maximum measured concentration of of BI 474121 in plasma (Cmax). The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis. | Pharmacokinetic parameter analysis set (PKS): The PKS included all participants in the TS who provided at least 1 primary or secondary pharmacokinetic (PK) endpoint that were not excluded due to a protocol deviation relevant to the evaluation of PK or due to PK non-evaluability. Thus, a participant was included in the PKS, even if he contributed only 1 PK parameter value for 1 period to the statistical assessment. Descriptive and model-based analyses of PK parameters were based on the PKS. | Posted | Geometric Mean | Geometric Coefficient of Variation | Nanomole per litre | Within 3 hours (h) before drug administration and 15 minutes (min), 30min, 1h, 1h 30min, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, and 96h after drug administration. |
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| Secondary | SRD: Area Under the Concentration-time Curve of BI 474121 in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz). | Area under the concentration-time curve of BI 474121 in plasma over the time interval from 0 to the last quantifiable data point (AUC0-tz) was analyzed after single dose administration of BI 474121. The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis. | Pharmacokinetic parameter analysis set (PKS) The PKS included all participants in the TS who provided at least 1 primary or secondary pharmacokinetic (PK) endpoint that were not excluded due to a protocol deviation relevant to the evaluation of PK or due to PK non-evaluability. Thus, a participant was included in the PKS, even if he contributed only 1 PK parameter value for 1 period to the statistical assessment. Descriptive and model-based analyses of PK parameters were based on the PKS. | Posted | Geometric Mean | Geometric Coefficient of Variation | Hour times nanomole per litre | Within 3 hours (h) before drug administration and 15 minutes (min), 30min, 1h, 1h 30min, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, and 96h after drug administration. |
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| Secondary | SRD: Maximum Measured Concentration of of BI 474121 in Plasma (Cmax). | Maximum measured concentration of of BI 474121 in plasma (Cmax). The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis. | Pharmacokinetic parameter analysis set (PKS) The PKS included all participants in the TS who provided at least 1 primary or secondary pharmacokinetic (PK) endpoint that were not excluded due to a protocol deviation relevant to the evaluation of PK or due to PK non-evaluability. Thus, a participant was included in the PKS, even if he contributed only 1 PK parameter value for 1 period to the statistical assessment. Descriptive and model-based analyses of PK parameters were based on the PKS. | Posted | Geometric Mean | Geometric Coefficient of Variation | Nanomole per litre | Within 3 hours (h) before drug administration and 15 minutes (min), 30min, 1h, 1h 30min, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, and 96h after drug administration. |
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| Secondary | BA: Area Under the Concentration-time Curve of BI 474121 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞). | Area under the concentration-time curve of BI 474121 in plasma over the time interval from 0 extrapolated to infinity (AUC0-∞). The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis. | Pharmacokinetic parameter analysis set (PKS): The PKS included all participants in the TS who provided at least 1 primary or secondary pharmacokinetic (PK) endpoint that were not excluded due to a protocol deviation relevant to the evaluation of PK or due to PK non-evaluability. Thus, a participant was included in the PKS, even if he contributed only 1 PK parameter value for 1 period to the statistical assessment. Descriptive and model-based analyses of PK parameters were based on the PKS. | Posted | Geometric Mean | Geometric Coefficient of Variation | Hour times nanomole per litre | Within 3 hours (h) before drug administration and 15 minutes (min), 30min, 1h, 1h 30min, 2h, 3h, 4h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, and 96h after drug administration. |
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SRD part: From drug administration until the end of residual effect period, up to 168 hours (7 days). BA part: From drug administration until the end of residual effect period, up to 168 hours (7 days).
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| ID | Title | Description | Deaths (Affected) | Deaths (At Risk) | Serious Events (Affected) | Serious Events (At Risk) | Other Events (Affected) | Other Events (At Risk) |
|---|---|---|---|---|---|---|---|---|
| EG000 | SRD: Placebo Matching BI 474121 Oral Solution (OS) | This arm comprises all placebo treated participants of the single rising dose (SRD) part treated with an oral solution (placebo treated participants of the two lowest dose group (DG)s). Participants receiving placebo were equally distributed across dose groups. A single dose of BI 474121 matching placebo powder for oral solution was administered after an overnight fast together with 240 milliliter (mL) of water to participants who were in a standing position. | 0 | 4 | 0 | 4 | 0 | 4 |
| EG001 | SRD: Placebo Matching BI 474121 Tablet (T) | This arm comprises all placebo treated participants of the single rising dose (SRD) part treated with a tablet (placebo treated participants of the five upper DGs). Participants receiving placebo were equally distributed across dose groups. A single dose of BI 474121 matching placebo tablet was administered after an overnight fast together with 240 mL of water to subjects who were in a standing position. | 0 | 9 | 0 | 9 | 4 | 9 |
| EG002 | SRD: 0.25 Milligram (mg) BI 474121 - OS | A single dose of 0.25 mg BI 474121 was solved in 0.5 mL water and was administered after an overnight fast together with 240 mL of water to participants who were in a standing position. | 0 | 6 | 0 | 6 | 0 | 6 |
| EG003 | SRD: 1 mg BI 474121 - OS | A single dose of 1 mg BI 474121 was solved in 2mL water and was administered after an overnight fast together with 240 mL of water to participants who were in a standing position. | 0 | 6 | 0 | 6 | 1 | 6 |
| EG004 | SRD: 2.5 mg BI 474121 - T | A single dose of 2.5 mg BI 474121 was administered as 1 uncoated 2.5 mg tablet after an overnight fast together with 240 mL of water to participants who were in a standing position. | 0 | 6 | 0 | 6 | 2 | 6 |
| EG005 | SRD: 5 mg BI 474121 - T | A single dose of 5.0 mg BI 474121 was administered as 2 uncoated 2.5 mg tablets after an overnight fast together with 240 mL of water to participants who were in a standing position. | 0 | 6 | 0 | 6 | 1 | 6 |
| EG006 | SRD: 10 mg BI 474121 - T | A single dose of 10.0 mg BI 474121 was administered as 1 uncoated 10.0 mg tablet after an overnight fast together with 240 mL of water to participants who were in a standing position. | 0 | 6 | 0 | 6 | 0 | 6 |
| EG007 | SRD: 20 mg BI 474121 - T | A single dose of 20.0 mg BI 474121 was administered as 2 uncoated 10.0 mg tablets after an overnight fast together with 240 mL of water to participants who were in a standing position. | 0 | 5 | 0 | 5 | 1 | 5 |
| EG008 | SRD: 40 mg BI 474121 - T | A single dose of 40.0 mg BI 474121 was administered as 4 uncoated 10.0 mg tablets after an overnight fast together with 240 mL of water to participants who were in a standing position. | 0 | 6 | 0 | 6 | 3 | 6 |
| EG009 | BA: 10 mg BI 474121 - Oral Solution - Fasted (Reference (R)) | One single dose of 10 mg BI 474121 was administered as oral solution solved in 20 milliliter (mL) of water with 240 mL of water after an overnight fast. | 0 | 12 | 0 | 12 | 3 | 12 |
| EG010 | BA: 10 mg BI 474121 - Tablet - Fasted (Test 2 (T2)) | One single dose of 10 mg BI 474121 was administered as uncoated tablet with 240 mL of water after an overnight fast. | 0 | 12 | 0 | 12 | 3 | 12 |
| EG011 | BA: 10 mg BI 474121 - Tablet - Fed (Test 1 (T1)) | One single dose of 10 mg BI 474121 was administered as uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water. | 0 | 11 | 0 | 11 | 1 | 11 |
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| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Photophobia | Eye disorders | MedDRA 23.1 | Systematic Assessment |
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| Flatulence | Gastrointestinal disorders | MedDRA 23.1 | Systematic Assessment |
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| Fatigue | General disorders | MedDRA 23.1 | Systematic Assessment |
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| Nasopharyngitis | Infections and infestations | MedDRA 23.1 | Systematic Assessment |
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| Rhinitis | Infections and infestations | MedDRA 23.1 | Systematic Assessment |
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| Thermal burn | Injury, poisoning and procedural complications | MedDRA 23.1 | Systematic Assessment |
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| Arthralgia | Musculoskeletal and connective tissue disorders | MedDRA 23.1 | Systematic Assessment |
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| Back pain | Musculoskeletal and connective tissue disorders | MedDRA 23.1 | Systematic Assessment |
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| Myalgia | Musculoskeletal and connective tissue disorders | MedDRA 23.1 | Systematic Assessment |
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| Headache | Nervous system disorders | MedDRA 23.1 | Systematic Assessment |
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| Paraesthesia | Nervous system disorders | MedDRA 23.1 | Systematic Assessment |
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| Abnormal dreams | Psychiatric disorders | MedDRA 23.1 | Systematic Assessment |
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| Initial insomnia | Psychiatric disorders | MedDRA 23.1 | Systematic Assessment |
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Due to the current COVID-19 pandemic, the recruitment of new subjects was temporarily discontinued. Ongoing, randomised patients were managed as per Trial Protocol.
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| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| Boehringer Ingelheim, Call Center | Boehringer Ingelheim | 1-800-243-0127 | clintriage.rdg@boehringer-ingelheim.com |
| Prot_000.pdf |
| SAP | No | Yes | No | Statistical Analysis Plan | Apr 26, 2021 | Jul 20, 2023 | SAP_001.pdf |
| Female |
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| Not Hispanic or Latino |
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| Unknown or Not Reported |
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| Asian |
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| Native Hawaiian or Other Pacific Islander |
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| Black or African American |
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| White |
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| More than one race |
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| Unknown or Not Reported |
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| OG001 |
| BA: 10 mg BI 474121 - Tablet - Fasted (Test 2 (T2)) |
One single dose of 10 mg BI 474121 was administered as uncoated tablet with 240 mL of water after an overnight fast. |
| OG002 | BA: 10 mg BI 474121 - Tablet - Fed (Test 1 (T1)) | One single dose of 10 mg BI 474121 was administered as uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water. |
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| OG002 | BA: 10 mg BI 474121 - Tablet - Fed (Test 1 (T1)) | One single dose of 10 mg BI 474121 was administered as uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water. |
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A single dose of 1 mg BI 474121 was solved in 2mL water and was administered after an overnight fast together with 240 mL of water to participants who were in a standing position. |
| OG002 | SRD: 2.5 mg BI 474121 - Tablet (T) | A single dose of 2.5 mg BI 474121 was administered as 1 uncoated 2.5 mg tablet after an overnight fast together with 240 mL of water to participants who were in a standing position. |
| OG003 | SRD: 5 mg BI 474121 - T | A single dose of 5.0 mg BI 474121 was administered as 2 uncoated 2.5 mg tablets after an overnight fast together with 240 mL of water to participants who were in a standing position. |
| OG004 | SRD: 10 mg BI 474121 - T | A single dose of 10.0 mg BI 474121 was administered as 1 uncoated 10.0 mg tablet after an overnight fast together with 240 mL of water to participants who were in a standing position. |
| OG005 | SRD: 20 mg BI 474121 - T | A single dose of 20.0 mg BI 474121 was administered as 2 uncoated 10.0 mg tablets after an overnight fast together with 240 mL of water to participants who were in a standing position. |
| OG006 | SRD: 40 mg BI 474121 - T | A single dose of 40.0 mg BI 474121 was administered as 4 uncoated 10.0 mg tablets after an overnight fast together with 240 mL of water to participants who were in a standing position. |
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| OG002 | SRD: 2.5 mg BI 474121 - Tablet (T) | A single dose of 2.5 mg BI 474121 was administered as 1 uncoated 2.5 mg tablet after an overnight fast together with 240 milliliter (mL) of water to participants who were in a standing position. |
| OG003 | SRD: 5 mg BI 474121 - T | A single dose of 5.0 mg BI 474121 was administered as 2 uncoated 2.5 mg tablets after an overnight fast together with 240 milliliter (mL) of water to participants who were in a standing position. |
| OG004 | SRD: 10 mg BI 474121 - T | A single dose of 10.0 mg BI 474121 was administered as 1 uncoated 10.0 mg tablet after an overnight fast together with 240 milliliter (mL) of water to participants who were in a standing position. |
| OG005 | SRD: 20 mg BI 474121 - T | A single dose of 20.0 mg BI 474121 was administered as 2 uncoated 10.0 mg tablets after an overnight fast together with 240 milliliter (mL) of water to participants who were in a standing position. |
| OG006 | SRD: 40 mg BI 474121 - T | A single dose of 40.0 mg BI 474121 was administered as 4 uncoated 10.0 mg tablets after an overnight fast together with 240 milliliter (mL) of water to participants who were in a standing position. |
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| OG002 | BA: 10 mg BI 474121 - Tablet - Fed (Test 1 (T1)) | One single dose of 10 mg BI 474121 was administered as uncoated tablet in fed conditions after a high-fat / high-caloric breakfast with 240 mL of water. |
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