Trial Outcomes & Findings for A Study in Healthy Men to Measure the Amount of BI 425809 in the Blood When Taken as a Tablet (NCT NCT03783000)

NCT ID: NCT03783000

Last Updated: 2026-03-27

Results Overview

The dose-normalised area under the concentration-time curve of the analyte (\[14C\]-BI 425809 after iv administration as well as for BI 425809 after oral administration) over the time interval from 0 to infinity (AUC0-∞, norm) is presented. Geometric least square mean (adjusted geometric mean) and adjusted geometric standard error were calculated using an analysis of variance (ANOVA) model performed on the logarithmic scale, including 'formulation' as a fixed effect and 'subject' as a random effect. For treatment T, pharmacokinetic samples were collected within 2 h prior to the drug administration and at 1, 2, 3, 4.083, 6, 8, 12, 24, 72, 120 and at 168 h after single oral administration of unlabelled BI 425809. For treatment R, samples were collected at 3, 4.083, 4.167, 4.25, 4.5, 5, 6, 7, 8, 12, 16, 24, 72, 120 and 168 h after single oral administration of unlabelled BI 425809.

Recruitment status

COMPLETED

Study phase

PHASE1

Target enrollment

6 participants

Primary outcome timeframe

Pharmacokinetic samples were collected within 2 h before and up to 168 h after single oral administration of unlabelled BI 425809. Further details are in description.

Results posted on

2026-03-27

Participant Flow

It was an open-label, non-randomized, single period, single arm Phase I trial in healthy participants. All participants received a single dose of 25 milligram (mg) unlabelled BI 425809 tablet plus a single intravenous (iv) micro-tracer infusion of 30 microgram (μg) BI 425809 (C-14), containing 27 μg BI 425809 mixed with 3 μg \[C-14\]-BI 425809.

All participants were screened for eligibility to participate in the trial. Participants attended specialist site which would then ensured that all participants met all inclusion/exclusion criteria. Participants were not to be administered to trial treatment if any one of the specific entry criteria were not met.

Participant milestones

Participant milestones
Measure
BI 425809 (T) BI 425809 Mixed With [C-14]-BI 425809 (R)
All healthy participants received one unlabelled oral dose of 25 milligram (mg) BI 425809 in the film coated tablet (Test treatment, T) and in addition an intravenous (iv) micro-tracer infusion of 30 microgram (μg) BI 425809 (14-C) (Reference treatment, R), consisting of 27 μg unlabelled BI 425809 mixed with 3 μg labelled \[C-14\]-BI 425809 in 10 milliliter (mL) iv solution at a concentration of 3 μg BI 425809 (C-14)/ mL. Both treatments were given in the fasted state on the same study day. The reference treatment started 4 hour (h) after administration of the test treatment.
Overall Study
STARTED
6
Overall Study
COMPLETED
5
Overall Study
NOT COMPLETED
1

Reasons for withdrawal

Reasons for withdrawal
Measure
BI 425809 (T) BI 425809 Mixed With [C-14]-BI 425809 (R)
All healthy participants received one unlabelled oral dose of 25 milligram (mg) BI 425809 in the film coated tablet (Test treatment, T) and in addition an intravenous (iv) micro-tracer infusion of 30 microgram (μg) BI 425809 (14-C) (Reference treatment, R), consisting of 27 μg unlabelled BI 425809 mixed with 3 μg labelled \[C-14\]-BI 425809 in 10 milliliter (mL) iv solution at a concentration of 3 μg BI 425809 (C-14)/ mL. Both treatments were given in the fasted state on the same study day. The reference treatment started 4 hour (h) after administration of the test treatment.
Overall Study
Lost to Follow-up
1

Baseline Characteristics

A Study in Healthy Men to Measure the Amount of BI 425809 in the Blood When Taken as a Tablet

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure
BI 425809 (T) BI 425809 Mixed With [C-14]-BI 425809 (R)
n=6 Participants
All healthy participants received one unlabelled oral dose of 25 milligram (mg) BI 425809 in the film coated tablet (Test treatment, T) and in addition an intravenous (iv) micro-tracer infusion of 30 microgram (μg) BI 425809 (14-C) (Reference treatment, R), consisting of 27 μg unlabelled BI 425809 mixed with 3 μg labelled \[C-14\]-BI 425809 in 10 milliliter (mL) iv solution at a concentration of 3 μg BI 425809 (C-14)/ mL. Both treatments were given in the fasted state on the same study day. The reference treatment started 4 hour (h) after administration of the test treatment.
Age, Continuous
35.0 Years
STANDARD_DEVIATION 14.5 • n=56 Participants
Sex: Female, Male
Female
0 Participants
n=56 Participants
Sex: Female, Male
Male
6 Participants
n=56 Participants
Ethnicity (NIH/OMB)
Hispanic or Latino
0 Participants
n=56 Participants
Ethnicity (NIH/OMB)
Not Hispanic or Latino
6 Participants
n=56 Participants
Ethnicity (NIH/OMB)
Unknown or Not Reported
0 Participants
n=56 Participants
Race (NIH/OMB)
American Indian or Alaska Native
0 Participants
n=56 Participants
Race (NIH/OMB)
Asian
0 Participants
n=56 Participants
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
0 Participants
n=56 Participants
Race (NIH/OMB)
Black or African American
0 Participants
n=56 Participants
Race (NIH/OMB)
White
5 Participants
n=56 Participants
Race (NIH/OMB)
More than one race
1 Participants
n=56 Participants
Race (NIH/OMB)
Unknown or Not Reported
0 Participants
n=56 Participants

PRIMARY outcome

Timeframe: Pharmacokinetic samples were collected within 2 h before and up to 168 h after single oral administration of unlabelled BI 425809. Further details are in description.

Population: Pharmacokinetic (PK) set (PKS): All participants in the treated set (TS) who provided at least one primary or secondary PK endpoint not excluded due to a protocol violation relevant to the evaluation of PK or due to PK non-evaluability.

The dose-normalised area under the concentration-time curve of the analyte (\[14C\]-BI 425809 after iv administration as well as for BI 425809 after oral administration) over the time interval from 0 to infinity (AUC0-∞, norm) is presented. Geometric least square mean (adjusted geometric mean) and adjusted geometric standard error were calculated using an analysis of variance (ANOVA) model performed on the logarithmic scale, including 'formulation' as a fixed effect and 'subject' as a random effect. For treatment T, pharmacokinetic samples were collected within 2 h prior to the drug administration and at 1, 2, 3, 4.083, 6, 8, 12, 24, 72, 120 and at 168 h after single oral administration of unlabelled BI 425809. For treatment R, samples were collected at 3, 4.083, 4.167, 4.25, 4.5, 5, 6, 7, 8, 12, 16, 24, 72, 120 and 168 h after single oral administration of unlabelled BI 425809.

Outcome measures

Outcome measures
Measure
BI 425809 (T)
n=6 Participants
All healthy participants received a single dose of 25 mg unlabelled BI 425809 tablet with 240 mL of water after an overnight fast of at least 10 h.
[C14]-BI 425809 (R)
n=6 Participants
All healthy participants received a single 15 minute iv infusion of 30 μg \[C14\]-BI 425809 (containing 27 μg BI 425809 mixed with 3 μg \[C-14\]-BI 42580) after an overnight fast of at least 10 h and at about 4 h after intake of oral dose of unlabelled BI 425809 tablet (T).
Area Under the Concentration-time Curve of the Analyte ([14C]-BI 425809 After iv Administration as Well as for BI 425809 After Oral Administration) Over the Time Interval From 0 to Infinity (AUC0-∞, Norm)
306.17 Nanomole*hour/Liter/mg (nmol*h/L/mg)
Standard Error 1.15
427.36 Nanomole*hour/Liter/mg (nmol*h/L/mg)
Standard Error 1.15

SECONDARY outcome

Timeframe: Pharmacokinetic samples were collected within 2:00 h:m prior to the drug administration and at 1:00, 2:00, 3:00, 4:05, 6:00, 8:00, 12:00, 24:00, 72:00, 120:00 and at 168:00 h:m after drug administration.

Population: PKS

Cmax, maximum measured concentration of the BI 425809 in plasma after a single oral dose is presented.

Outcome measures

Outcome measures
Measure
BI 425809 (T)
n=6 Participants
All healthy participants received a single dose of 25 mg unlabelled BI 425809 tablet with 240 mL of water after an overnight fast of at least 10 h.
[C14]-BI 425809 (R)
All healthy participants received a single 15 minute iv infusion of 30 μg \[C14\]-BI 425809 (containing 27 μg BI 425809 mixed with 3 μg \[C-14\]-BI 42580) after an overnight fast of at least 10 h and at about 4 h after intake of oral dose of unlabelled BI 425809 tablet (T).
Maximum Measured Concentration of the BI 425809 in Plasma After a Single Oral Dose (Cmax)
225 Nanomole/Liter (nmol/L)
Geometric Coefficient of Variation 34.4

Adverse Events

BI 425809 (T) BI 425809 Mixed With [C-14]-BI 425809 (R)

Serious events: 0 serious events
Other events: 3 other events
Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Other adverse events
Measure
BI 425809 (T) BI 425809 Mixed With [C-14]-BI 425809 (R)
n=6 participants at risk
All healthy participants received one unlabelled oral dose of 25 milligram (mg) BI 425809 in the film coated tablet (Test treatment, T) and in addition an intravenous (iv) micro-tracer infusion of 30 microgram (μg) BI 425809 (14-C) (Reference treatment, R), consisting of 27 μg unlabelled BI 425809 mixed with 3 μg labelled \[C-14\]-BI 425809 in 10 milliliter (mL) iv solution at a concentration of 3 μg BI 425809 (C-14)/ mL. Both treatments were given in the fasted state on the same study day. The reference treatment started 4 hour (h) after administration of the test treatment.
Gastrointestinal disorders
Abdominal pain
16.7%
1/6 • Adverse events: from first drug administration until 11 days after the last administration of BI 425809, up to 12 days. All-cause mortality: from first drug administration until end of trial, up to 15 days.
Treated set (TS): All participants who were randomized and received at least one dose of the trial medication.
Gastrointestinal disorders
Diarrhoea
16.7%
1/6 • Adverse events: from first drug administration until 11 days after the last administration of BI 425809, up to 12 days. All-cause mortality: from first drug administration until end of trial, up to 15 days.
Treated set (TS): All participants who were randomized and received at least one dose of the trial medication.
Eye disorders
Visual brightness
16.7%
1/6 • Adverse events: from first drug administration until 11 days after the last administration of BI 425809, up to 12 days. All-cause mortality: from first drug administration until end of trial, up to 15 days.
Treated set (TS): All participants who were randomized and received at least one dose of the trial medication.
Nervous system disorders
Somnolence
16.7%
1/6 • Adverse events: from first drug administration until 11 days after the last administration of BI 425809, up to 12 days. All-cause mortality: from first drug administration until end of trial, up to 15 days.
Treated set (TS): All participants who were randomized and received at least one dose of the trial medication.

Additional Information

Boehringer Ingelheim, Call Centre

Boehringer Ingelheim

Phone: 1-800-243-0127

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