Trial Outcomes & Findings for Metabolism and Pharmacokinetics of [14C]-BI 409306 After Administration as Oral Solution in Healthy Male Volunteers (NCT NCT02597998)

Last Updated: 2024-03-07

Results Overview

Mass balance recovery of total radioactivity in urine and faeces: Amount excreted within the time interval from 0 to the time of the last quantifiable data point as a percentage of the administered dose (fe0-tz) for urine and faeces. Urine collection intervals: -17:00-0:00 hours before drug administration and, 0-4, 4-8, 8-12, 12-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, 168-192 and 192-216 hours after drug administration. Faeces collection intervals: -17:00-0:00, 0-24, 24-48, 48-72, 72-96, 96- 20, 120-144, 144-168, 168-192 and 192-216 hours after drug administration.

Recruitment status

COMPLETED

Study phase

PHASE1

Target enrollment

6 participants

Primary outcome timeframe

Urine and faeces sample collection: 17 hours before and up to 216 hours after drug administration. The details are mentioned in description section.

Results posted on

2024-03-07

Participant Flow

The study was an open-label, single-arm, single-dose Phase I trial with healthy male subjects.

All subjects were screened for eligibility prior to participation in the trial. Subjects attended a specialist site which ensured that they (the subjects) strictly met all inclusion and none of the exclusion criteria. Subjects were not to be allocated to a treatment group if any of the entry criteria were violated.

Participant milestones

Participant milestones
Measure	14C-BI 409306 - 25 mg Healthy subjects received one single dose of oral solution containing 25 milligram (mg) of \[14C\]-BI 409306 containing a radioactive dose of approximately 2.00 Megabecquerel (MBq), reconstituted in 50 milliliter (mL) solvent (5 mg/mL tartaric acid solution)
Overall Study STARTED	6
Overall Study COMPLETED	6
Overall Study NOT COMPLETED	0

Reasons for withdrawal

Withdrawal data not reported

Baseline Characteristics

Metabolism and Pharmacokinetics of [14C]-BI 409306 After Administration as Oral Solution in Healthy Male Volunteers

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure	14C-BI 409306 - 25 mg n=6 Participants Healthy subjects received one single dose of oral solution containing 25 milligram (mg) of \[14C\]-BI 409306 containing a radioactive dose of approximately 2.00 Megabecquerel (MBq), reconstituted in 50 milliliter (mL) solvent (5 mg/mL tartaric acid solution)
Age, Continuous	46.0 Years STANDARD_DEVIATION 6.1 • n=5 Participants
Sex: Female, Male Female	0 Participants n=5 Participants
Sex: Female, Male Male	6 Participants n=5 Participants
Ethnicity (NIH/OMB) Hispanic or Latino	1 Participants n=5 Participants
Ethnicity (NIH/OMB) Not Hispanic or Latino	5 Participants n=5 Participants
Ethnicity (NIH/OMB) Unknown or Not Reported	0 Participants n=5 Participants
Race (NIH/OMB) American Indian or Alaska Native	0 Participants n=5 Participants
Race (NIH/OMB) Asian	0 Participants n=5 Participants
Race (NIH/OMB) Native Hawaiian or Other Pacific Islander	0 Participants n=5 Participants
Race (NIH/OMB) Black or African American	0 Participants n=5 Participants
Race (NIH/OMB) White	6 Participants n=5 Participants
Race (NIH/OMB) More than one race	0 Participants n=5 Participants
Race (NIH/OMB) Unknown or Not Reported	0 Participants n=5 Participants

PRIMARY outcome

Timeframe: Urine and faeces sample collection: 17 hours before and up to 216 hours after drug administration. The details are mentioned in description section.

Population: The pharmacokinetic parameter analysis set (PKS) included all subjects in the treated set (TS) who provided at least one primary or secondary pharmacokinetic endpoint value, which was not flagged for exclusion.

Outcome measures

Outcome measures
Measure	14C-BI 409306 - 25 mg n=6 Participants Healthy subjects received one single dose of oral solution containing 25 milligram (mg) of \[14C\]-BI 409306 containing a radioactive dose of approximately 2.00 Megabecquerel (MBq), reconstituted in 50 milliliter (mL) solvent (5 mg/mL tartaric acid solution)
Mass Balance Recovery of Total Radioactivity in Urine and Faeces: Amount Excreted Within the Time Interval From 0 to the Time of the Last Quantifiable Data Point as a Percentage of the Administered Dose (fe0-tz) for Urine and Faeces Urine	84.0 Percentage (%) of dose administered Geometric Coefficient of Variation 4.42
Mass Balance Recovery of Total Radioactivity in Urine and Faeces: Amount Excreted Within the Time Interval From 0 to the Time of the Last Quantifiable Data Point as a Percentage of the Administered Dose (fe0-tz) for Urine and Faeces Faeces	10.4 Percentage (%) of dose administered Geometric Coefficient of Variation 10.5
Mass Balance Recovery of Total Radioactivity in Urine and Faeces: Amount Excreted Within the Time Interval From 0 to the Time of the Last Quantifiable Data Point as a Percentage of the Administered Dose (fe0-tz) for Urine and Faeces Urine and Faeces	94.4 Percentage (%) of dose administered Geometric Coefficient of Variation 4.45

SECONDARY outcome

Timeframe: PK plasma samples were taken at: 2:00 (hour: minute) before drug administration and 0:10, 0:20, 0:30, 0:45, 1, 1:30, 2, 2:30, 3, 4, 6, 8, 10, 12, 14, 24, 36, 48, 72, 96, 120, 144, 168 hours after drug administration.

Maximum measured concentration of BI 409306 in plasma (Cmax).

Outcome measures

Outcome measures
Measure	14C-BI 409306 - 25 mg n=6 Participants Healthy subjects received one single dose of oral solution containing 25 milligram (mg) of \[14C\]-BI 409306 containing a radioactive dose of approximately 2.00 Megabecquerel (MBq), reconstituted in 50 milliliter (mL) solvent (5 mg/mL tartaric acid solution)
Maximum Measured Concentration of BI 409306 in Plasma (Cmax)	275 nanomole (nmol) / Litre (L) Geometric Coefficient of Variation 24.3

SECONDARY outcome

Maximum measured concentration of 14C-BI 409306 related radioactivity in plasma (Cmax).

Outcome measures

Outcome measures
Measure	14C-BI 409306 - 25 mg n=6 Participants Healthy subjects received one single dose of oral solution containing 25 milligram (mg) of \[14C\]-BI 409306 containing a radioactive dose of approximately 2.00 Megabecquerel (MBq), reconstituted in 50 milliliter (mL) solvent (5 mg/mL tartaric acid solution)
Maximum Measured Concentration of 14C-BI 409306 Related Radioactivity in Plasma (Cmax)	1600 nanomole (nmol) / Litre (L) Geometric Coefficient of Variation 15.6

SECONDARY outcome

Area under the concentration-time curve over the time interval from 0 to the last quantifiable data point (AUC0-tz) for BI 409306 in plasma.

Outcome measures

Outcome measures
Measure	14C-BI 409306 - 25 mg n=6 Participants Healthy subjects received one single dose of oral solution containing 25 milligram (mg) of \[14C\]-BI 409306 containing a radioactive dose of approximately 2.00 Megabecquerel (MBq), reconstituted in 50 milliliter (mL) solvent (5 mg/mL tartaric acid solution)
Area Under the Concentration-time Curve Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) for BI 409306 in Plasma	357 nanomole (nmol) * hour(h) / Litre (L) Geometric Coefficient of Variation 36.8

SECONDARY outcome

Area under the concentration-time curve over the time interval from 0 to the last quantifiable data point (AUC0-tz) for 14C-BI 409306 related radioactivity in plasma.

Outcome measures

Outcome measures
Measure	14C-BI 409306 - 25 mg n=6 Participants Healthy subjects received one single dose of oral solution containing 25 milligram (mg) of \[14C\]-BI 409306 containing a radioactive dose of approximately 2.00 Megabecquerel (MBq), reconstituted in 50 milliliter (mL) solvent (5 mg/mL tartaric acid solution)
Area Under the Concentration-time Curve Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) for 14C-BI 409306 Related Radioactivity in Plasma	3560 nanomole (nmol) * hour(h) / Litre (L) Geometric Coefficient of Variation 9.6

Adverse Events

14C-BI 409306 - 25 mg

Serious events: 0 serious events

Other events: 2 other events

Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Other adverse events
Measure	14C-BI 409306 - 25 mg n=6 participants at risk Healthy subjects received one single dose of oral solution containing 25 milligram (mg) of \[14C\]-BI 409306 containing a radioactive dose of approximately 2.00 Megabecquerel (MBq), reconstituted in 50 milliliter (mL) solvent (5 mg/mL tartaric acid solution)
Nervous system disorders Headache	33.3% 2/6 • From first drug administration until 7 days after the last drug administration, up to 21 days Treated Set: (TS) This subject set includes all subjects in the randomized set who received \[at least\] one dose of study drug. This was the full analysis set population in the sense of ICH-E9.

Additional Information

Boehringer Ingelheim, Call Center

Boehringer Ingelheim

Phone: 1-800-243-0127

Email: [email protected]

Results disclosure agreements

Principal investigator is a sponsor employee Boehringer Ingelheim (BI) acknowledges that investigators have the right to publish the study results. Investigators shall provide BI with a copy of any publication or presentation for review prior to any submission. Such review will be done with regard to proprietary information, information related to patentable inventions, medical, scientific, and statistical accuracy within 60 days. BI may request a delay of the publication in order to protect BI's intellectual property rights.
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