Trial Outcomes & Findings for A Study in Healthy Men to Test How BI 1291583 is Processed in the Body (NCT NCT05833035)

Results Overview

Fraction of \[14C\]-radioactivity excreted in urine expressed as percentage of the administered dose over the time interval from 0 to the last quantifiable time point (feurine, 0-tz) is reported. Timeframe: After 336h, 24h interval urine sample collection was planned every 7 days starting on Day 21 until Day 43.

Recruitment status

COMPLETED

Study phase

PHASE1

Target enrollment

8 participants

Primary outcome timeframe

Urine sampling intervals: Within 14 hours (h) prior and 0-4 , 4-8, 8-12, 12-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, 168-192, 192-216, 216-240, 240-264, 264-288, 288-312, 312-336h after intake of BI 1291583 (C14). Continues in description.

Results posted on

2026-01-21

Participant Flow

The trial was performed as an open-label, single-arm, single-dose trial in healthy male subjects to investigate the basic PK of BI 1291583, its metabolites (BI 1373234, CD 18507, CD 17849, CD 16785, and BI 1321869 (CD 16426)) and \[14C\]-radioactivity, including mass balance, excretion pathways and metabolism following a single oral dose of 5 mg BI 1291583 (C-14).

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

Participant milestones

Participant milestones
Measure	BI 1291583 (C-14) Participants received a single dose of 20 milliliter (mL) of BI 1291583 (C-14) radioactive solution for oral administration concentrated at 0.25 milligram/mL. The radioactive solution contained a radioactive dose of approximately 0.36 Megabecquerel (MBq). The oral solution contained a mixture of pure radioactive carbon \[14C\]-labelled "hot" drug substance, and BI 1291583, i.e. unlabelled "cold" drug substance. The BI 1291583 (C-14) oral solution was administered with 240 mL of water after an overnight fast of at least 10 hours (h).
Overall Study STARTED	8
Overall Study COMPLETED	8
Overall Study NOT COMPLETED	0

Reasons for withdrawal

Withdrawal data not reported

Baseline Characteristics

A Study in Healthy Men to Test How BI 1291583 is Processed in the Body

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure	BI 1291583 (C-14) n=8 Participants Participants received a single dose of 20 milliliter (mL) of BI 1291583 (C-14) radioactive solution for oral administration concentrated at 0.25 milligram/mL. The radioactive solution contained a radioactive dose of approximately 0.36 Megabecquerel (MBq). The oral solution contained a mixture of pure radioactive carbon \[14C\]-labelled "hot" drug substance, and BI 1291583, i.e. unlabelled "cold" drug substance. The BI 1291583 (C-14) oral solution was administered with 240 mL of water after an overnight fast of at least 10 hours (h).
Age, Continuous	35.4 years STANDARD_DEVIATION 8.7 • n=37 Participants
Sex: Female, Male Female	0 Participants n=37 Participants
Sex: Female, Male Male	8 Participants n=37 Participants
Ethnicity (NIH/OMB) Hispanic or Latino	0 Participants n=37 Participants
Ethnicity (NIH/OMB) Not Hispanic or Latino	8 Participants n=37 Participants
Ethnicity (NIH/OMB) Unknown or Not Reported	0 Participants n=37 Participants
Race (NIH/OMB) American Indian or Alaska Native	0 Participants n=37 Participants
Race (NIH/OMB) Asian	0 Participants n=37 Participants
Race (NIH/OMB) Native Hawaiian or Other Pacific Islander	0 Participants n=37 Participants
Race (NIH/OMB) Black or African American	0 Participants n=37 Participants
Race (NIH/OMB) White	8 Participants n=37 Participants
Race (NIH/OMB) More than one race	0 Participants n=37 Participants
Race (NIH/OMB) Unknown or Not Reported	0 Participants n=37 Participants

PRIMARY outcome

Timeframe: Urine sampling intervals: Within 14 hours (h) prior and 0-4 , 4-8, 8-12, 12-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, 168-192, 192-216, 216-240, 240-264, 264-288, 288-312, 312-336h after intake of BI 1291583 (C14). Continues in description.

Population: Pharmacokinetic set (PKS): This set included all subjects in the treated (TS) who provided at least one pharmacokinetic (PK) endpoint that was defined as primary or secondary and was not excluded due to a protocol deviation relevant to the evaluation of PK or due to PK non-evaluability. Thus, a subject was included in the PKS, even if he/she contributed only one PK parameter value for one period to the statistical assessment.

Fraction of \[14C\]-radioactivity excreted in urine expressed as percentage of the administered dose over the time interval from 0 to the last quantifiable time point (feurine, 0-tz) is reported. Timeframe: After 336h, 24h interval urine sample collection was planned every 7 days starting on Day 21 until Day 43.

Outcome measures

Outcome measures
Measure	BI 1291583 (C-14) n=8 Participants Participants received a single dose of 20 milliliter (mL) of BI 1291583 (C-14) radioactive solution for oral administration concentrated at 0.25 milligram/mL. The radioactive solution contained a radioactive dose of approximately 0.36 Megabecquerel (MBq). The oral solution contained a mixture of pure radioactive carbon \[14C\]-labelled "hot" drug substance, and BI 1291583, i.e. unlabelled "cold" drug substance. The BI 1291583 (C-14) oral solution was administered with 240 mL of water after an overnight fast of at least 10 hours (h).
Mass Balance and Total Recovery of [14C]-Radioactivity in Urine: Fraction of [14C]-Radioactivity Excreted in Urine Expressed as Percentage of the Administered Dose Over the Time Interval From 0 to the Last Quantifiable Time Point (Feurine, 0-tz)	26.0 percentage of administered dose Geometric Coefficient of Variation 12.9

PRIMARY outcome

Timeframe: All stools were collected prior and up to 336 hours (h) (sampling intervals 0-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, 168-192, 192-216, 216 -240, 240-264, 264-288, 288-312, 312-336 h) after intake of BI 1291583 (C14). Continues in description.

Population: Pharmacokinetic set (PKS): This set included all subjects in the treated (TS) who provided at least one pharmacokinetic (PK) endpoint that was defined as primary or secondary and was not excluded due to a protocol deviation relevant to the evaluation of PK or due to PK non-evaluability. Thus, a subject was included in the PKS, even if he/she contributed only one PK parameter value for one period to the statistical assessment.

Fraction of \[14C\]-radioactivity excreted in faeces expressed as percentage of the administered dose over the time interval from 0 to the last quantifiable time point (fefaeces, 0-tz) is reported. Timeframe: After 336h, 24h interval stools sample collection was planned every 7 days starting on Day 21 until Day 43.

Outcome measures

Outcome measures
Measure	BI 1291583 (C-14) n=8 Participants Participants received a single dose of 20 milliliter (mL) of BI 1291583 (C-14) radioactive solution for oral administration concentrated at 0.25 milligram/mL. The radioactive solution contained a radioactive dose of approximately 0.36 Megabecquerel (MBq). The oral solution contained a mixture of pure radioactive carbon \[14C\]-labelled "hot" drug substance, and BI 1291583, i.e. unlabelled "cold" drug substance. The BI 1291583 (C-14) oral solution was administered with 240 mL of water after an overnight fast of at least 10 hours (h).
Mass Balance and Total Recovery of [14C]-Radioactivity in Faeces: Fraction of [14C]-Radioactivity Excreted in Faeces Expressed as Percentage of the Administered Dose Over the Time Interval From 0 to the Last Quantifiable Time Point (Fefaeces, 0-tz)	61.4 percentage of administered dose Geometric Coefficient of Variation 13.2

SECONDARY outcome

Timeframe: Within 4 hours prior and 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, 24, 48, 72, 120, 168, 216, 264, 336, 485, 653, 821, 989 hours after administration of BI 1291583 (C14).

Population: Pharmacokinetic set (PKS): This set included all subjects in the treated (TS) who provided at least one pharmacokinetic (PK) endpoint that was defined as primary or secondary and was not excluded due to a protocol deviation relevant to the evaluation of PK or due to PK non-evaluability. Thus, a subject was included in the PKS, even if he/she contributed only one PK parameter value for one period to the statistical assessment.

Area under the concentration-time curve of \[14C\]-radioactivity (\[14C\]-BI 1291583-EQ) in plasma over the time interval from 0 to the last quantifiable time point (AUC0-tz, \[14C\]-BI 1291583-EQ) is reported.

Outcome measures

Outcome measures
Measure	BI 1291583 (C-14) n=8 Participants Participants received a single dose of 20 milliliter (mL) of BI 1291583 (C-14) radioactive solution for oral administration concentrated at 0.25 milligram/mL. The radioactive solution contained a radioactive dose of approximately 0.36 Megabecquerel (MBq). The oral solution contained a mixture of pure radioactive carbon \[14C\]-labelled "hot" drug substance, and BI 1291583, i.e. unlabelled "cold" drug substance. The BI 1291583 (C-14) oral solution was administered with 240 mL of water after an overnight fast of at least 10 hours (h).
Area Under the Concentration-time Curve of [14C]-Radioactivity ([14C]-BI 1291583-Equivalents (EQ)) in Plasma Over the Time Interval From 0 to the Last Quantifiable Time Point (AUC0-tz, [14C]-BI 1291583-EQ)	1730 hour * nanomole/Liter (h*nmol/L) Geometric Coefficient of Variation 16.1

SECONDARY outcome

Timeframe: Within 4 hours (h) prior and 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, 24, 48, 72, 120, 168, 216, 264, 336, 485, 653, 821, 989 h after administration of BI 1291583 (C14).

Population: Pharmacokinetic set (PKS): This set included all subjects in the treated (TS) who provided at least one pharmacokinetic (PK) endpoint that was defined as primary or secondary and was not excluded due to a protocol deviation relevant to the evaluation of PK or due to PK non-evaluability. Thus, a subject was included in the PKS, even if he/she contributed only one PK parameter value for one period to the statistical assessment.

Area under the concentration-time curve of BI 1291583 in plasma over the time interval from 0 to the last quantifiable time point (AUC0-tz, BI 1291583) is reported.

Outcome measures

Outcome measures
Measure	BI 1291583 (C-14) n=8 Participants Participants received a single dose of 20 milliliter (mL) of BI 1291583 (C-14) radioactive solution for oral administration concentrated at 0.25 milligram/mL. The radioactive solution contained a radioactive dose of approximately 0.36 Megabecquerel (MBq). The oral solution contained a mixture of pure radioactive carbon \[14C\]-labelled "hot" drug substance, and BI 1291583, i.e. unlabelled "cold" drug substance. The BI 1291583 (C-14) oral solution was administered with 240 mL of water after an overnight fast of at least 10 hours (h).
Area Under the Concentration-time Curve of BI 1291583 in Plasma Over the Time Interval From 0 to the Last Quantifiable Time Point (AUC0-tz, BI 1291583)	139 hour * nanomole/Liter (h*nmol/L) Geometric Coefficient of Variation 19.7

SECONDARY outcome

Timeframe: Within 4 hours prior and 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, 24, 48, 72, 120, 168, 216, 264, 336, 485, 653, 821, 989 hours after administration of BI 1291583 (C14).

Population: Pharmacokinetic set (PKS): This set included all subjects in the treated (TS) who provided at least one pharmacokinetic (PK) endpoint that was defined as primary or secondary and was not excluded due to a protocol deviation relevant to the evaluation of PK or due to PK non-evaluability. Thus, a subject was included in the PKS, even if he/she contributed only one PK parameter value for one period to the statistical assessment.

Maximum measured concentration of \[14C\]-radioactivity (\[14C\]-BI 1291583-EQ) in plasma (Cmax, \[14C\]-BI 1291583-EQ) is reported.

Outcome measures

Outcome measures
Measure	BI 1291583 (C-14) n=8 Participants Participants received a single dose of 20 milliliter (mL) of BI 1291583 (C-14) radioactive solution for oral administration concentrated at 0.25 milligram/mL. The radioactive solution contained a radioactive dose of approximately 0.36 Megabecquerel (MBq). The oral solution contained a mixture of pure radioactive carbon \[14C\]-labelled "hot" drug substance, and BI 1291583, i.e. unlabelled "cold" drug substance. The BI 1291583 (C-14) oral solution was administered with 240 mL of water after an overnight fast of at least 10 hours (h).
Maximum Measured Concentration of [14C]-Radioactivity ([14C]-BI 1291583-Equivalents (EQ)) in Plasma (Cmax, [14C]-BI 1291583-EQ)	6.58 nanomole/Liter (nmol/L) Geometric Coefficient of Variation 14.4

SECONDARY outcome

Timeframe: Within 4 hours prior and 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, 24, 48, 72, 120, 168, 216, 264, 336, 485, 653, 821, 989 hours after administration of BI 1291583 (C14).

Population: Pharmacokinetic set (PKS): This set included all subjects in the treated (TS) who provided at least one pharmacokinetic (PK) endpoint that was defined as primary or secondary and was not excluded due to a protocol deviation relevant to the evaluation of PK or due to PK non-evaluability. Thus, a subject was included in the PKS, even if he/she contributed only one PK parameter value for one period to the statistical assessment.

Maximum measured concentration of BI 1291583 in plasma (Cmax, BI 1291583) is reported.

Outcome measures

Outcome measures
Measure	BI 1291583 (C-14) n=8 Participants Participants received a single dose of 20 milliliter (mL) of BI 1291583 (C-14) radioactive solution for oral administration concentrated at 0.25 milligram/mL. The radioactive solution contained a radioactive dose of approximately 0.36 Megabecquerel (MBq). The oral solution contained a mixture of pure radioactive carbon \[14C\]-labelled "hot" drug substance, and BI 1291583, i.e. unlabelled "cold" drug substance. The BI 1291583 (C-14) oral solution was administered with 240 mL of water after an overnight fast of at least 10 hours (h).
Maximum Measured Concentration of BI 1291583 in Plasma (Cmax, BI 1291583)	1.90 nanomole/Liter (nmol/L) Geometric Coefficient of Variation 23.8

SECONDARY outcome

Timeframe: Within 4 hours (h) prior and 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, 24, 48, 72, 120, 168, 216, 264, 336, 485, 653, 821, 989 h after administration of BI 1291583 (C14).

Population: Pharmacokinetic set (PKS): This set included all subjects in the treated (TS) who provided at least one pharmacokinetic (PK) endpoint that was defined as primary or secondary and was not excluded due to a protocol deviation relevant to the evaluation of PK or due to PK non-evaluability. Thus, a subject was included in the PKS, even if he/she contributed only one PK parameter value for one period to the statistical assessment.

Area under the concentration-time curve of BI 1291583 metabolites in plasma over the time interval from 0 to the last quantifiable time point (AUC0-tz, BI 1291583 metabolites). AUC0-tz of the following BI 1291583 metabolites is reported: BI 1373234; CD 18507; CD 17849; CD 16785; BI 1321869.

Outcome measures

Outcome measures
Measure	BI 1291583 (C-14) n=8 Participants Participants received a single dose of 20 milliliter (mL) of BI 1291583 (C-14) radioactive solution for oral administration concentrated at 0.25 milligram/mL. The radioactive solution contained a radioactive dose of approximately 0.36 Megabecquerel (MBq). The oral solution contained a mixture of pure radioactive carbon \[14C\]-labelled "hot" drug substance, and BI 1291583, i.e. unlabelled "cold" drug substance. The BI 1291583 (C-14) oral solution was administered with 240 mL of water after an overnight fast of at least 10 hours (h).
Area Under the Concentration-time Curve of BI 1291583 Metabolites in Plasma Over the Time Interval From 0 to the Last Quantifiable Time Point (AUC0-tz, BI 1291583 Metabolites) CD 17849	157 hour nanomole/Liter (hnmol/L) Geometric Coefficient of Variation 47.8
Area Under the Concentration-time Curve of BI 1291583 Metabolites in Plasma Over the Time Interval From 0 to the Last Quantifiable Time Point (AUC0-tz, BI 1291583 Metabolites) CD 18507	159 hour nanomole/Liter (hnmol/L) Geometric Coefficient of Variation 37.3
Area Under the Concentration-time Curve of BI 1291583 Metabolites in Plasma Over the Time Interval From 0 to the Last Quantifiable Time Point (AUC0-tz, BI 1291583 Metabolites) CD 16785	167 hour nanomole/Liter (hnmol/L) Geometric Coefficient of Variation 47.6
Area Under the Concentration-time Curve of BI 1291583 Metabolites in Plasma Over the Time Interval From 0 to the Last Quantifiable Time Point (AUC0-tz, BI 1291583 Metabolites) BI 1373234	48.3 hour nanomole/Liter (hnmol/L) Geometric Coefficient of Variation 33.2
Area Under the Concentration-time Curve of BI 1291583 Metabolites in Plasma Over the Time Interval From 0 to the Last Quantifiable Time Point (AUC0-tz, BI 1291583 Metabolites) BI 1321869	5280 hour nanomole/Liter (hnmol/L) Geometric Coefficient of Variation 79.4

SECONDARY outcome

Timeframe: Within 4 hours (h) prior and 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 14, 24, 48, 72, 120, 168, 216, 264, 336, 485, 653, 821, 989 h after administration of BI 1291583 (C14).

Population: Pharmacokinetic set (PKS): This set included all subjects in the treated (TS) who provided at least one pharmacokinetic (PK) endpoint that was defined as primary or secondary and was not excluded due to a protocol deviation relevant to the evaluation of PK or due to PK non-evaluability. Thus, a subject was included in the PKS, even if he/she contributed only one PK parameter value for one period to the statistical assessment.

Maximum measured concentration of BI 1291583 metabolites in plasma (Cmax, BI 1291583 metabolites). Cmax of the following metabolites is reported: BI 1373234; CD 18507; CD 17849; CD 16785; BI 1321869.

Outcome measures

Outcome measures
Measure	BI 1291583 (C-14) n=8 Participants Participants received a single dose of 20 milliliter (mL) of BI 1291583 (C-14) radioactive solution for oral administration concentrated at 0.25 milligram/mL. The radioactive solution contained a radioactive dose of approximately 0.36 Megabecquerel (MBq). The oral solution contained a mixture of pure radioactive carbon \[14C\]-labelled "hot" drug substance, and BI 1291583, i.e. unlabelled "cold" drug substance. The BI 1291583 (C-14) oral solution was administered with 240 mL of water after an overnight fast of at least 10 hours (h).
Maximum Measured Concentration of BI 1291583 Metabolites in Plasma (Cmax, BI 1291583 Metabolites) CD 17849	1.48 nanomole/Liter (nmol/L) Geometric Coefficient of Variation 44.9
Maximum Measured Concentration of BI 1291583 Metabolites in Plasma (Cmax, BI 1291583 Metabolites) CD 18507	0.944 nanomole/Liter (nmol/L) Geometric Coefficient of Variation 28.3
Maximum Measured Concentration of BI 1291583 Metabolites in Plasma (Cmax, BI 1291583 Metabolites) CD 16785	0.330 nanomole/Liter (nmol/L) Geometric Coefficient of Variation 43.6
Maximum Measured Concentration of BI 1291583 Metabolites in Plasma (Cmax, BI 1291583 Metabolites) BI 1373234	0.391 nanomole/Liter (nmol/L) Geometric Coefficient of Variation 26.3
Maximum Measured Concentration of BI 1291583 Metabolites in Plasma (Cmax, BI 1291583 Metabolites) BI 1321869	12.2 nanomole/Liter (nmol/L) Geometric Coefficient of Variation 26.2

Adverse Events

BI 1291583 (C-14)

Serious events: 0 serious events

Other events: 5 other events

Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Other adverse events
Measure	BI 1291583 (C-14) n=8 participants at risk Participants received a single dose of 20 milliliter (mL) of BI 1291583 (C-14) radioactive solution for oral administration concentrated at 0.25 milligram/mL. The radioactive solution contained a radioactive dose of approximately 0.36 Megabecquerel (MBq). The oral solution contained a mixture of pure radioactive carbon \[14C\]-labelled "hot" drug substance, and BI 1291583, i.e. unlabelled "cold" drug substance. The BI 1291583 (C-14) oral solution was administered with 240 mL of water after an overnight fast of at least 10 hours (h).
Nervous system disorders Syncope	12.5% 1/8 • From first administration of BI 1291583 (C14) until the end of the residual effect period, up to 28 days. Treated set (TS): included all subjects who were treated with at least one dose of trial drug.
Nervous system disorders Dizziness	12.5% 1/8 • From first administration of BI 1291583 (C14) until the end of the residual effect period, up to 28 days. Treated set (TS): included all subjects who were treated with at least one dose of trial drug.
Nervous system disorders Headache	12.5% 1/8 • From first administration of BI 1291583 (C14) until the end of the residual effect period, up to 28 days. Treated set (TS): included all subjects who were treated with at least one dose of trial drug.
Nervous system disorders Presyncope	12.5% 1/8 • From first administration of BI 1291583 (C14) until the end of the residual effect period, up to 28 days. Treated set (TS): included all subjects who were treated with at least one dose of trial drug.
Gastrointestinal disorders Abdominal distension	12.5% 1/8 • From first administration of BI 1291583 (C14) until the end of the residual effect period, up to 28 days. Treated set (TS): included all subjects who were treated with at least one dose of trial drug.
Gastrointestinal disorders Abdominal pain	12.5% 1/8 • From first administration of BI 1291583 (C14) until the end of the residual effect period, up to 28 days. Treated set (TS): included all subjects who were treated with at least one dose of trial drug.
Renal and urinary disorders Micturition urgency	12.5% 1/8 • From first administration of BI 1291583 (C14) until the end of the residual effect period, up to 28 days. Treated set (TS): included all subjects who were treated with at least one dose of trial drug.

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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