Trial Outcomes & Findings for A Study in Healthy Men to Test How BI 730357 is Processed by the Body (NCT NCT03664011)

Last Updated: 2023-07-12

Results Overview

feurine, fractions of \[14C\]-radioactivity excreted in urine as percentage of the administered dose over the time interval from 0 to tz, where tz is the latest quantifiable data point across all participants.

Recruitment status

COMPLETED

Study phase

PHASE1

Target enrollment

6 participants

Primary outcome timeframe

Within 18 hours (h) predose, 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, 312-336 h after dosing on Day 1, continued in 24 h intervals, every 7 days from Day 21 until Day 50.

Results posted on

2023-07-12

Participant Flow

It was planned to include healthy male participants in this non-randomised, open-label, single-arm, single-dose trial. They were recruited from the volunteer's pool of the study site.

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	BI 730357 All participants were administered an oral single dose of 50 milligram (mg) BI 730357 containing \[C-14\] BI 730357 base (BS) (pure 14C-labelled "hot" drug substance) and BI 730357 BS (unlabelled "cold" drug substance). This mixture corresponds to the warm substance BI 730357 BS (C-14) containing a radioactive dose of approximately 3.7 MegaBecquerel (MBq), (100 microcurie (µCi)), and was administered in a solution of 10 milliliter (mL) volume with 240 mL of water after an overnight fast of at least 10 hours (h).
Overall Study STARTED	6
Overall Study COMPLETED	6
Overall Study NOT COMPLETED	0

Reasons for withdrawal

Withdrawal data not reported

Baseline Characteristics

A Study in Healthy Men to Test How BI 730357 is Processed by the Body

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure	BI 730357 n=6 Participants All participants were administered an oral single dose of 50 milligram (mg) BI 730357 containing \[C-14\] BI 730357 base (BS) (pure 14C-labelled "hot" drug substance) and BI 730357 BS (unlabelled "cold" drug substance). This mixture corresponds to the warm substance BI 730357 BS (C-14) containing a radioactive dose of approximately 3.7 MegaBecquerel (MBq), (100 microcurie (µCi)), and was administered in a solution of 10 milliliter (mL) volume with 240 mL of water after an overnight fast of at least 10 hours (h).
Age, Continuous	44.2 Years STANDARD_DEVIATION 16.6 • 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	5 Participants n=5 Participants
Race (NIH/OMB) More than one race	1 Participants n=5 Participants
Race (NIH/OMB) Unknown or Not Reported	0 Participants n=5 Participants

PRIMARY outcome

Timeframe: Within 18 hours (h) predose, 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, 312-336 h after dosing on Day 1, continued in 24 h intervals, every 7 days from Day 21 until Day 50.

Population: Pharmacokinetic (PK) parameter analysis set (PKS): The PKS included all subjects in the TS who provided at least one value for primary or secondary PK endpoints and were not excluded due to relevant protocol deviations or due to PK non-evaluability.

Outcome measures

Outcome measures
Measure	BI 730357 n=6 Participants All participants were administered an oral single dose of 50 milligram (mg) BI 730357 containing \[C-14\] BI 730357 base (BS) (pure 14C-labelled "hot" drug substance) and BI 730357 BS (unlabelled "cold" drug substance). This mixture corresponds to the warm substance BI 730357 BS (C-14) containing a radioactive dose of approximately 3.7 MegaBecquerel (MBq), (100 microcurie (µCi)), and was administered in a solution of 10 milliliter (mL) volume with 240 mL of water after an overnight fast of at least 10 hours (h).
Mass Balance Recovery of Total [14C]-Radioactivity in Urine (Feurine, 0-tz)	34.3 Percentage of administered dose (%) Geometric Coefficient of Variation 19.2

PRIMARY outcome

Timeframe: Within 48 hours (h) predose, 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 and 312-336 h after dosing on Day 1 and continued in 24 h intervals, every 7 days up to Day 50.

fefaeces, 0-tz, fraction of \[14C\]-radioactivity excreted in faeces as percentage of the administered dose over the time interval from 0 to tz, where tz is the latest quantifiable data point across all participants.

Outcome measures

Outcome measures
Measure	BI 730357 n=6 Participants All participants were administered an oral single dose of 50 milligram (mg) BI 730357 containing \[C-14\] BI 730357 base (BS) (pure 14C-labelled "hot" drug substance) and BI 730357 BS (unlabelled "cold" drug substance). This mixture corresponds to the warm substance BI 730357 BS (C-14) containing a radioactive dose of approximately 3.7 MegaBecquerel (MBq), (100 microcurie (µCi)), and was administered in a solution of 10 milliliter (mL) volume with 240 mL of water after an overnight fast of at least 10 hours (h).
Mass Balance Recovery of Total [14C]-Radioactivity in Faeces (Fefaeces, 0-tz)	65.0 Percentage of administered dose (%) Geometric Coefficient of Variation 8.09

SECONDARY outcome

Timeframe: Within 3:00 Hours: minutes (h:m) pre-dose, 0:30, 1:00, 1:30, 2:00, 4:00, 8:00, 12:00, 24:00, 48:00, 72:00, 120:00, 168:00, 216:00, 264:00, 312:00, 485:00, 653:00 and 821:00 after drug administration.

Cmax, maximum measured concentration of 14C-BI 730357-equivalent (EQ) and BI 730357 in plasma after a single oral dose of 50 mg BI 730357 BS (C-14) is presented. Plasma concentrations of (C-14) BI 730357-radioactivity are expressed as 14C-BI 730357-EQ.

Outcome measures

Outcome measures
Measure	BI 730357 n=6 Participants All participants were administered an oral single dose of 50 milligram (mg) BI 730357 containing \[C-14\] BI 730357 base (BS) (pure 14C-labelled "hot" drug substance) and BI 730357 BS (unlabelled "cold" drug substance). This mixture corresponds to the warm substance BI 730357 BS (C-14) containing a radioactive dose of approximately 3.7 MegaBecquerel (MBq), (100 microcurie (µCi)), and was administered in a solution of 10 milliliter (mL) volume with 240 mL of water after an overnight fast of at least 10 hours (h).
Maximum Measured Concentration of 14C-BI 730357-equivalent (EQ) and BI 730357 (Cmax) 14C-BI 730357-EQ	1020 Nanomole/litre (nmol/L) Geometric Coefficient of Variation 16.5
Maximum Measured Concentration of 14C-BI 730357-equivalent (EQ) and BI 730357 (Cmax) BI 730357	641 Nanomole/litre (nmol/L) Geometric Coefficient of Variation 19.2

SECONDARY outcome

AUC0-tz, area under the concentration-time curve of 14C-BI 730357-equivalent (EQ) and BI 730357 over the time interval from 0 to the last quantifiable time point in plasma after a single oral dose of 50 mg BI 730357 BS (C-14) is presented. Plasma concentrations of (C-14) BI 730357-radioactivity are expressed as 14C-BI 730357-EQ.

Outcome measures

Outcome measures
Measure	BI 730357 n=6 Participants All participants were administered an oral single dose of 50 milligram (mg) BI 730357 containing \[C-14\] BI 730357 base (BS) (pure 14C-labelled "hot" drug substance) and BI 730357 BS (unlabelled "cold" drug substance). This mixture corresponds to the warm substance BI 730357 BS (C-14) containing a radioactive dose of approximately 3.7 MegaBecquerel (MBq), (100 microcurie (µCi)), and was administered in a solution of 10 milliliter (mL) volume with 240 mL of water after an overnight fast of at least 10 hours (h).
Area Under the Concentration-time Curve of 14C-BI 730357-equivalent (EQ) and BI 730357 Over the Time Interval From 0 to the Last Quantifiable Time Point (AUC0-tz) 14C-BI 730357-EQ	24300 NanomoleHours/litre (nmolh/L) Geometric Coefficient of Variation 50.8
Area Under the Concentration-time Curve of 14C-BI 730357-equivalent (EQ) and BI 730357 Over the Time Interval From 0 to the Last Quantifiable Time Point (AUC0-tz) BI 730357	9410 NanomoleHours/litre (nmolh/L) Geometric Coefficient of Variation 79.9

Adverse Events

BI 730357

Serious events: 0 serious events

Other events: 4 other events

Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Other adverse events
Measure	BI 730357 n=6 participants at risk All participants were administered an oral single dose of 50 milligram (mg) BI 730357 containing \[C-14\] BI 730357 base (BS) (pure 14C-labelled "hot" drug substance) and BI 730357 BS (unlabelled "cold" drug substance). This mixture corresponds to the warm substance BI 730357 BS (C-14) containing a radioactive dose of approximately 3.7 MegaBecquerel (MBq), (100 microcurie (µCi)), and was administered in a solution of 10 milliliter (mL) volume with 240 mL of water after an overnight fast of at least 10 hours (h).
General disorders Catheter site haematoma	16.7% 1/6 • From drug administration until End-of-trial (EoT) examination, up to 50 days.
General disorders Catheter site inflammation	16.7% 1/6 • From drug administration until End-of-trial (EoT) examination, up to 50 days.
General disorders Vessel puncture site haematoma	16.7% 1/6 • From drug administration until End-of-trial (EoT) examination, up to 50 days.
Nervous system disorders Headache	33.3% 2/6 • From drug administration until End-of-trial (EoT) examination, up to 50 days.
Nervous system disorders Paraesthesia	16.7% 1/6 • From drug administration until End-of-trial (EoT) examination, up to 50 days.
Musculoskeletal and connective tissue disorders Back pain	16.7% 1/6 • From drug administration until End-of-trial (EoT) examination, up to 50 days.
Musculoskeletal and connective tissue disorders Myalgia	16.7% 1/6 • From drug administration until End-of-trial (EoT) examination, up to 50 days.
Respiratory, thoracic and mediastinal disorders Oropharyngeal pain	16.7% 1/6 • From drug administration until End-of-trial (EoT) examination, up to 50 days.
Skin and subcutaneous tissue disorders Pruritus	16.7% 1/6 • From drug administration until End-of-trial (EoT) examination, up to 50 days.

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.
Publication restrictions are in place

Restriction type: OTHER