Trial Outcomes & Findings for A Study in Healthy Men to Test How BI 1265162 is Taken up and Processed by the Body (NCT NCT04267276)
NCT ID: NCT04267276
Last Updated: 2022-06-01
Results Overview
Mass balance recovery assessed as amount of (C-14) BI 1265162-radioactivity excreted as a percentage of the single intravenous administered dose of BI 1265162 (C-14) over the time interval from 0 to 192 hours. The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis.
TERMINATED
PHASE1
7 participants
On Day -1 or Day 1 pre-dose (blank) sample, on Day 1 prior to start of urine collection voiding of the bladder, 0-4 , 4-8, 8-12, 12-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, and 168-192 hours after administration of BI 1265162 (C-14).
2022-06-01
Participant Flow
This was a non-randomised, open-label, single-dose, single arm, mass balance trial in healthy male subjects. The trial had 2 parts. Part 1 was investigating metabolism and pharmacokinetics of (C-14 (radiocarbon labelled)) BI 1265162 after intravenous administration. Part 2 was investigating metabolism and pharmacokinetics of (C-14) BI 1265162 after oral administration. Part 2 was not conducted due to premature discontinuation of the trial.
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
| Measure |
BI 1265162 - Intravenous
Participants received a single intravenous infusion (i.v.) of 50 microgram (μg) of BI 1265162, consisting of 45 μg unlabeled BI 1265162 mixed with 5 μg Carbon 14 labelled BI 1265162 (\[14C\]BI 1265162) (radocarbon as 10 milliliter (mL) in i.v. solution (5 μg BI 1265162 (C-14)/mL) over 1 hour (h) was administered after an overnight fast of at least 10 h.
The radioactive dose per infusion was calculated to not exceed 0.018 megabecquerel (MBq).
Participants received 240 mL of fluid 1 h and 4 h after administration. Participants also received lunch 4 h after administration.
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Overall Study
STARTED
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7
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Overall Study
Treated
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7
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Overall Study
COMPLETED
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7
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Overall Study
NOT COMPLETED
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0
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Reasons for withdrawal
Withdrawal data not reported
Baseline Characteristics
A Study in Healthy Men to Test How BI 1265162 is Taken up and Processed by the Body
Baseline characteristics by cohort
| Measure |
BI 1265162 - Intravenous
n=7 Participants
Participants received a single intravenous infusion (i.v.) of 50 microgram (μg) of BI 1265162, consisting of 45 μg unlabeled BI 1265162 mixed with 5 μg Carbon 14 labelled BI 1265162 (\[14C\]BI 1265162) (radocarbon as 10 milliliter (mL) in i.v. solution (5 μg BI 1265162 (C-14)/mL) over 1 hour (h) was administered after an overnight fast of at least 10 h.
The radioactive dose per infusion was calculated to not exceed 0.018 megabecquerel (MBq).
Participants received 240 mL of fluid 1 h and 4 h after administration. Participants also received lunch 4 h after administration.
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Age, Continuous
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51.3 Years
STANDARD_DEVIATION 9.5 • n=99 Participants
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Sex/Gender, Customized
Male
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7 Participants
n=99 Participants
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Sex/Gender, Customized
Female
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0 Participants
n=99 Participants
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Ethnicity (NIH/OMB)
Hispanic or Latino
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0 Participants
n=99 Participants
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Ethnicity (NIH/OMB)
Not Hispanic or Latino
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7 Participants
n=99 Participants
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Ethnicity (NIH/OMB)
Unknown or Not Reported
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0 Participants
n=99 Participants
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Race (NIH/OMB)
American Indian or Alaska Native
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0 Participants
n=99 Participants
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Race (NIH/OMB)
Asian
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0 Participants
n=99 Participants
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Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
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0 Participants
n=99 Participants
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Race (NIH/OMB)
Black or African American
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1 Participants
n=99 Participants
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Race (NIH/OMB)
White
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6 Participants
n=99 Participants
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Race (NIH/OMB)
More than one race
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0 Participants
n=99 Participants
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Race (NIH/OMB)
Unknown or Not Reported
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0 Participants
n=99 Participants
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PRIMARY outcome
Timeframe: On Day -1 or Day 1 pre-dose (blank) sample, on Day 1 prior to start of urine collection voiding of the bladder, 0-4 , 4-8, 8-12, 12-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, and 168-192 hours after administration of BI 1265162 (C-14).Population: Pharmacokinetic parameter analysis set (PKS): This set includes all participants from the treated set (TS) who provide at least one pharmacokinetic endpoint that was defined as primary or secondary and was not excluded due to a protocol deviation relevant to the evaluation of pharmacokinetics or due to pharmacokinetic non-evaluability (as specified in the following subsection 'Pharmacokinetics'). Descriptive analyses of pharmacokinetic parameters will be based on the PKS.
Mass balance recovery assessed as amount of (C-14) BI 1265162-radioactivity excreted as a percentage of the single intravenous administered dose of BI 1265162 (C-14) over the time interval from 0 to 192 hours. The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis.
Outcome measures
| Measure |
BI 1265162 - Intravenous
n=7 Participants
Participants received a single intravenous infusion (i.v.) of 50 microgram (μg) of BI 1265162, consisting of 45 μg unlabeled BI 1265162 mixed with 5 μg Carbon 14 labelled BI 1265162 (\[14C\]BI 1265162) (radocarbon as 10 milliliter (mL) in i.v. solution (5 μg BI 1265162 (C-14)/mL) over 1 hour (h) was administered after an overnight fast of at least 10 h.
The radioactive dose per infusion was calculated to not exceed 0.018 megabecquerel (MBq).
Participants received 240 mL of fluid 1 h and 4 h after administration. Participants also received lunch 4 h after administration.
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Part 1: Mass Balance Recovery of Total (C-14) BI 1265162-radioactivity in Urine
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27.3 Percentage of the administered dose
Geometric Coefficient of Variation 16.1
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PRIMARY outcome
Timeframe: On Day -2, Day -1 or Day 1 pre-dose (blank) sample, and on Day 1 0-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, and 168-192 hours after administration of BI 1265162 (C-14).Population: Pharmacokinetic parameter analysis set (PKS): This set includes all participants from the treated set (TS) who provide at least one pharmacokinetic endpoint that was defined as primary or secondary and was not excluded due to a protocol deviation relevant to the evaluation of pharmacokinetics or due to pharmacokinetic non-evaluability (as specified in the following subsection 'Pharmacokinetics'). Descriptive analyses of pharmacokinetic parameters will be based on the PKS.
Mass balance recovery assessed as amount of (C-14) BI 1265162-radioactivity excreted as a percentage of the single intravenous administered dose of BI 1265162 (C-14) over the time interval from 0 to 192 hours. The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis.
Outcome measures
| Measure |
BI 1265162 - Intravenous
n=7 Participants
Participants received a single intravenous infusion (i.v.) of 50 microgram (μg) of BI 1265162, consisting of 45 μg unlabeled BI 1265162 mixed with 5 μg Carbon 14 labelled BI 1265162 (\[14C\]BI 1265162) (radocarbon as 10 milliliter (mL) in i.v. solution (5 μg BI 1265162 (C-14)/mL) over 1 hour (h) was administered after an overnight fast of at least 10 h.
The radioactive dose per infusion was calculated to not exceed 0.018 megabecquerel (MBq).
Participants received 240 mL of fluid 1 h and 4 h after administration. Participants also received lunch 4 h after administration.
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Part 1: Mass Balance Recovery of Total (C-14) BI 1265162-radioactivity in Faeces.
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65.3 Percentage of the administered dose
Geometric Coefficient of Variation 8.17
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SECONDARY outcome
Timeframe: At 02:00 hours:minutes pre-dose and at 0:05, 00:30, 00:59 01:05, 01:10, 01:40, 02:00, 03:00, 04:00, 05:00, 07:00, 08:00, 09:00, 11:00, 12:00, 24:00, 48:00, 72:00, 96:00, 120:00, 144:00, 168:00, 192:00 after single dose of BI 1265162 (C-14).Population: Pharmacokinetic parameter analysis set (PKS): This set includes all participants from the treated set (TS) who provide at least one pharmacokinetic endpoint that was defined as primary or secondary and was not excluded due to a protocol deviation relevant to the evaluation of pharmacokinetics or due to pharmacokinetic non-evaluability (as specified in the following subsection 'Pharmacokinetics'). Descriptive analyses of pharmacokinetic parameters will be based on the PKS.
Area under the concentration-time curve of total \[14C\]BI 1265162-EQ in plasma over the time interval from 0 to 192 hours (the last quantifiable data point (AUC0-tz)) was analyzed after the single intravenous dose administration of BI 1265162 (C-14). Plasma concentrations of (C-14) BI 1265162-radioactivity are expressed as \[14C\]BI 1265162-EQ. The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis.
Outcome measures
| Measure |
BI 1265162 - Intravenous
n=7 Participants
Participants received a single intravenous infusion (i.v.) of 50 microgram (μg) of BI 1265162, consisting of 45 μg unlabeled BI 1265162 mixed with 5 μg Carbon 14 labelled BI 1265162 (\[14C\]BI 1265162) (radocarbon as 10 milliliter (mL) in i.v. solution (5 μg BI 1265162 (C-14)/mL) over 1 hour (h) was administered after an overnight fast of at least 10 h.
The radioactive dose per infusion was calculated to not exceed 0.018 megabecquerel (MBq).
Participants received 240 mL of fluid 1 h and 4 h after administration. Participants also received lunch 4 h after administration.
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Part 1: Area Under the Concentration-time Curve of Total [14C]BI 1265162-equivalent (EQ) in Plasma Over the Time Interval From 0 to 192 Hours (the Last Quantifiable Data Point (AUC0-tz))
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5290 Hour times picomole per litre
Geometric Coefficient of Variation 27
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SECONDARY outcome
Timeframe: At 02:00 hours:minutes pre-dose and at 0:05, 00:30, 00:59 01:05, 01:10, 01:40, 02:00, 03:00, 04:00, 05:00, 07:00, 08:00, 09:00, 11:00, 12:00, 24:00, 48:00, 72:00, 96:00, 120:00, 144:00, 168:00, 192:00 after single dose of BI 1265162 (C-14).Population: Pharmacokinetic parameter analysis set (PKS): This set includes all participants from the treated set (TS) who provide at least one pharmacokinetic endpoint that was defined as primary or secondary and was not excluded due to a protocol deviation relevant to the evaluation of pharmacokinetics or due to pharmacokinetic non-evaluability (as specified in the following subsection 'Pharmacokinetics'). Descriptive analyses of pharmacokinetic parameters will be based on the PKS.
Area under the concentration-time curve of total BI 1265162 in plasma over the time interval from 0 to 192 hours (the last quantifiable data point (AUC0-tz)) was analyzed after the single intravenous dose administration. The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis.
Outcome measures
| Measure |
BI 1265162 - Intravenous
n=7 Participants
Participants received a single intravenous infusion (i.v.) of 50 microgram (μg) of BI 1265162, consisting of 45 μg unlabeled BI 1265162 mixed with 5 μg Carbon 14 labelled BI 1265162 (\[14C\]BI 1265162) (radocarbon as 10 milliliter (mL) in i.v. solution (5 μg BI 1265162 (C-14)/mL) over 1 hour (h) was administered after an overnight fast of at least 10 h.
The radioactive dose per infusion was calculated to not exceed 0.018 megabecquerel (MBq).
Participants received 240 mL of fluid 1 h and 4 h after administration. Participants also received lunch 4 h after administration.
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Part 1: Area Under the Concentration-time Curve of Total BI 1265162 in Plasma Over the Time Interval From 0 to 192 Hours (the Last Quantifiable Data Point (AUC0-tz))
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1890 Hour times picomole per litre
Geometric Coefficient of Variation 12.3
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SECONDARY outcome
Timeframe: At 02:00 hours:minutes pre-dose and at 0:05, 00:30, 00:59 01:05, 01:10, 01:40, 02:00, 03:00, 04:00, 05:00, 07:00, 08:00, 09:00, 11:00, 12:00, 24:00, 48:00, 72:00, 96:00, 120:00, 144:00, 168:00, 192:00 after single dose of BI 1265162 (C-14).Population: Pharmacokinetic parameter analysis set (PKS): This set includes all participants from the treated set (TS) who provide at least one pharmacokinetic endpoint that was defined as primary or secondary and was not excluded due to a protocol deviation relevant to the evaluation of pharmacokinetics or due to pharmacokinetic non-evaluability (as specified in the following subsection 'Pharmacokinetics'). Descriptive analyses of pharmacokinetic parameters will be based on the PKS.
Area under the concentration-time curve of total BI 1265162 metabolite M582 in plasma over the time interval from 0 to 192 hours (the last quantifiable data point (AUC0-tz)) was analyzed after the single intravenous dose administration. The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis.
Outcome measures
| Measure |
BI 1265162 - Intravenous
n=7 Participants
Participants received a single intravenous infusion (i.v.) of 50 microgram (μg) of BI 1265162, consisting of 45 μg unlabeled BI 1265162 mixed with 5 μg Carbon 14 labelled BI 1265162 (\[14C\]BI 1265162) (radocarbon as 10 milliliter (mL) in i.v. solution (5 μg BI 1265162 (C-14)/mL) over 1 hour (h) was administered after an overnight fast of at least 10 h.
The radioactive dose per infusion was calculated to not exceed 0.018 megabecquerel (MBq).
Participants received 240 mL of fluid 1 h and 4 h after administration. Participants also received lunch 4 h after administration.
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Part 1: Area Under the Concentration-time Curve of Total BI 1265162 Metabolite M582 in Plasma Over the Time Interval From 0 to 192 Hours (the Last Quantifiable Data Point (AUC0-tz))
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3400 Hour times picomole per litre
Geometric Coefficient of Variation 37.8
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SECONDARY outcome
Timeframe: At 02:00 hours:minutes pre-dose and at 0:05, 00:30, 00:59 01:05, 01:10, 01:40, 02:00, 03:00, 04:00, 05:00, 07:00, 08:00, 09:00, 11:00, 12:00, 24:00, 48:00, 72:00, 96:00, 120:00, 144:00, 168:00, 192:00 after single dose of BI 1265162 (C-14).Population: Pharmacokinetic parameter analysis set (PKS): This set includes all participants from the treated set (TS) who provide at least one pharmacokinetic endpoint that was defined as primary or secondary and was not excluded due to a protocol deviation relevant to the evaluation of pharmacokinetics or due to pharmacokinetic non-evaluability (as specified in the following subsection 'Pharmacokinetics'). Descriptive analyses of pharmacokinetic parameters will be based on the PKS.
Maximum measured concentration (Cmax) of total \[14C\]BI 1265162-EQ in plasma was analyzed after the single intravenous dose administration. Plasma concentrations of (C-14) BI 1265162-radioactivity are expressed as \[14C\]BI 1265162-EQ (EQ: equivalent). The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis.
Outcome measures
| Measure |
BI 1265162 - Intravenous
n=7 Participants
Participants received a single intravenous infusion (i.v.) of 50 microgram (μg) of BI 1265162, consisting of 45 μg unlabeled BI 1265162 mixed with 5 μg Carbon 14 labelled BI 1265162 (\[14C\]BI 1265162) (radocarbon as 10 milliliter (mL) in i.v. solution (5 μg BI 1265162 (C-14)/mL) over 1 hour (h) was administered after an overnight fast of at least 10 h.
The radioactive dose per infusion was calculated to not exceed 0.018 megabecquerel (MBq).
Participants received 240 mL of fluid 1 h and 4 h after administration. Participants also received lunch 4 h after administration.
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Part 1: Maximum Measured Concentration (Cmax) of Total [14C]BI 1265162-equivalent (EQ) in Plasma
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2270 Picomole per litre
Geometric Coefficient of Variation 14.7
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SECONDARY outcome
Timeframe: At 02:00 hours:minutes pre-dose and at 0:05, 00:30, 00:59 01:05, 01:10, 01:40, 02:00, 03:00, 04:00, 05:00, 07:00, 08:00, 09:00, 11:00, 12:00, 24:00, 48:00, 72:00, 96:00, 120:00, 144:00, 168:00, 192:00 after single dose of BI 1265162 (C-14).Population: Pharmacokinetic parameter analysis set (PKS): This set includes all participants from the treated set (TS) who provide at least one pharmacokinetic endpoint that was defined as primary or secondary and was not excluded due to a protocol deviation relevant to the evaluation of pharmacokinetics or due to pharmacokinetic non-evaluability (as specified in the following subsection 'Pharmacokinetics'). Descriptive analyses of pharmacokinetic parameters will be based on the PKS.
Maximum measured concentration (Cmax) of total BI 1265162 in plasma was analyzed after the single intravenous dose administration. The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis.
Outcome measures
| Measure |
BI 1265162 - Intravenous
n=7 Participants
Participants received a single intravenous infusion (i.v.) of 50 microgram (μg) of BI 1265162, consisting of 45 μg unlabeled BI 1265162 mixed with 5 μg Carbon 14 labelled BI 1265162 (\[14C\]BI 1265162) (radocarbon as 10 milliliter (mL) in i.v. solution (5 μg BI 1265162 (C-14)/mL) over 1 hour (h) was administered after an overnight fast of at least 10 h.
The radioactive dose per infusion was calculated to not exceed 0.018 megabecquerel (MBq).
Participants received 240 mL of fluid 1 h and 4 h after administration. Participants also received lunch 4 h after administration.
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Part 1: Maximum Measured Concentration (Cmax) of Total BI 1265162 in Plasma
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1880 Picomole per litre
Geometric Coefficient of Variation 15.7
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SECONDARY outcome
Timeframe: At 02:00 hours:minutes pre-dose and at 0:05, 00:30, 00:59 01:05, 01:10, 01:40, 02:00, 03:00, 04:00, 05:00, 07:00, 08:00, 09:00, 11:00, 12:00, 24:00, 48:00, 72:00, 96:00, 120:00, 144:00, 168:00, 192:00 after single dose of BI 1265162 (C-14).Population: Pharmacokinetic parameter analysis set (PKS): This set includes all participants from the treated set (TS) who provide at least one pharmacokinetic endpoint that was defined as primary or secondary and was not excluded due to a protocol deviation relevant to the evaluation of pharmacokinetics or due to pharmacokinetic non-evaluability (as specified in the following subsection 'Pharmacokinetics'). Descriptive analyses of pharmacokinetic parameters will be based on the PKS.
Maximum measured concentration (Cmax) of total metabolite M582 in plasma was analyzed after single dose administration. The geometric mean and geometric coefficient of variation were calculated by noncompartmental analysis.
Outcome measures
| Measure |
BI 1265162 - Intravenous
n=7 Participants
Participants received a single intravenous infusion (i.v.) of 50 microgram (μg) of BI 1265162, consisting of 45 μg unlabeled BI 1265162 mixed with 5 μg Carbon 14 labelled BI 1265162 (\[14C\]BI 1265162) (radocarbon as 10 milliliter (mL) in i.v. solution (5 μg BI 1265162 (C-14)/mL) over 1 hour (h) was administered after an overnight fast of at least 10 h.
The radioactive dose per infusion was calculated to not exceed 0.018 megabecquerel (MBq).
Participants received 240 mL of fluid 1 h and 4 h after administration. Participants also received lunch 4 h after administration.
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Part 1: Maximum Measured Concentration (Cmax) of Total BI 1265162 Metabolite M582 in Plasma
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650 Picomole per litre
Geometric Coefficient of Variation 33.9
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SECONDARY outcome
Timeframe: From drug administration up to 22 days.Population: Treated set (TS): The treated set includes all participants who were entered and treated with one dose of trial drug. The treated set will be used for safety analyses.
Percentage of participants with drug related adverse events (AEs) including clinically relevant findings from the physical examination. Percentages are calculated using total number of participants per treatment as the denominator.
Outcome measures
| Measure |
BI 1265162 - Intravenous
n=7 Participants
Participants received a single intravenous infusion (i.v.) of 50 microgram (μg) of BI 1265162, consisting of 45 μg unlabeled BI 1265162 mixed with 5 μg Carbon 14 labelled BI 1265162 (\[14C\]BI 1265162) (radocarbon as 10 milliliter (mL) in i.v. solution (5 μg BI 1265162 (C-14)/mL) over 1 hour (h) was administered after an overnight fast of at least 10 h.
The radioactive dose per infusion was calculated to not exceed 0.018 megabecquerel (MBq).
Participants received 240 mL of fluid 1 h and 4 h after administration. Participants also received lunch 4 h after administration.
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Part 1: Percentage of Participants With Drug Related Adverse Events (AEs) Including Clinically Relevant Findings From the Physical Examination
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14.3 Percentage of participants
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Adverse Events
BI 1265162 - Intravenous
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
BI 1265162 - Intravenous
n=7 participants at risk
Participants received a single intravenous infusion (i.v.) of 50 microgram (μg) of BI 1265162, consisting of 45 μg unlabeled BI 1265162 mixed with 5 μg Carbon 14 labelled BI 1265162 (\[14C\]BI 1265162) (radocarbon as 10 milliliter (mL) in i.v. solution (5 μg BI 1265162 (C-14)/mL) over 1 hour (h) was administered after an overnight fast of at least 10 h.
The radioactive dose per infusion was calculated to not exceed 0.018 megabecquerel (MBq).
Participants received 240 mL of fluid 1 h and 4 h after administration. Participants also received lunch 4 h after administration.
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Gastrointestinal disorders
Toothache
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14.3%
1/7 • From drug administration up to 22 days.
Treated set (TS): The treated set includes all participants who were entered and treated with one dose of trial drug. The treated set will be used for safety analyses.
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Nervous system disorders
Dysgeusia
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14.3%
1/7 • From drug administration up to 22 days.
Treated set (TS): The treated set includes all participants who were entered and treated with one dose of trial drug. The treated set will be used for safety analyses.
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Nervous system disorders
Headache
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42.9%
3/7 • From drug administration up to 22 days.
Treated set (TS): The treated set includes all participants who were entered and treated with one dose of trial drug. The treated set will be used for safety analyses.
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Respiratory, thoracic and mediastinal disorders
Dyspnoea
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14.3%
1/7 • From drug administration up to 22 days.
Treated set (TS): The treated set includes all participants who were entered and treated with one dose of trial drug. The treated set will be used for safety analyses.
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Additional Information
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.
- Publication restrictions are in place
Restriction type: OTHER