Safety, Tolerability, and Pharmacokinetics of Multiple Rising Doses of BI 425809 Tablets for 12 Days to Young and Elderly Healthy Male and Female Volunteers and Comparison of Pharmacokinetics of a Single Oral Dose of BI 425809 (Morning Versus Evening)

Safety, Tolerability, and Pharmacokinetics of Multiple Rising Doses of BI 425809 Tablets Given Orally Once Daily for 12 Days to Young and Elderly Healthy Male and Female Volunteers (Randomised, Double-blind, Placebo-controlled Within Dose Groups Phase I Study)(Part 1) and Comparison of Pharmacokinetics of a Single Oral Dose of BI 425809 After Oral Administration in the Morning Versus Oral Administration in the Evening in Young Healthy Male and Female Volunteers (Randomised, Two-sequence, Open, Two Period, Two-way Cross Over) (Part 2)

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT02337283

Enrollment

Registered

2015-01-13

Start date

2015-01-15

Completion date

2015-11-16

Last updated

2026-05-13

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy

Brief summary

The aim of the study is to investigate the safety, tolerability, and pharmacokinetics of multiple rising doses of BI 425809 tablets given orally once daily for 12 days to young and elderly healthy male and female volunteers and to compare single dose pharmacokinetics of BI 425809 given in the morning and in the evening.

Interventions

DRUGBI 425809

Tablets

DRUGPlacebo

Tablets

Study design

Allocation

RANDOMIZED

Intervention model

SINGLE_GROUP

Primary purpose

TREATMENT

Masking

DOUBLE

Eligibility

Sex/Gender

ALL

Age

18 Years to 50 Years

Healthy volunteers

Yes

Inclusion criteria

* Healthy male or female subjects according to the investigator´s assessment, based on a complete medical history including a physical examination, vital signs (blood pressure (BP), pulse rate (PR), 12-lead electrocardiogram (ECG), and clinical laboratory tests * age of 18 to 50 years (incl.) for young healthy volunteers or age of 65 to 80 years (incl.) for elderly healthy volunteers * Body mass index (BMI) of 18.5 to 29.9 kg/m2 (incl.) * Signed and dated written informed consent prior to admission to the study in accordance with good clinical practice (GCP) and local legislation * Female subjects who meet any of the following criteria: 1. Surgically sterilised 2. Postmenopausal, defined as at least 1 year of spontaneous amenorrhea (in questionable cases a blood sample with simultaneous levels of follicle stimulating hormone (FSH) above 40 U/L and estradiol below 30 ng/L is confirmatory)

Exclusion criteria

* Any finding in the medical examination (including BP, PR or ECG) is deviating from normal and judged as clinically relevant by the investigator * Repeated measurement of systolic blood pressure outside the range of 90 to 140 mmHg, diastolic blood pressure outside the range of 50 to 90 mmHg in young subjects, and systolic blood pressure greater than 150 mmHg, diastolic blood pressure greater than 95 mmHg in elderly subjects, or pulse rate outside the range of 50 to 90 bpm * Any laboratory value outside the reference range that the investigator considers to be of clinical relevance * Any evidence of a concomitant disease judged as clinically relevant by the investigator * Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders * Surgery of the gastrointestinal tract that could interfere with kinetics of the trial medication * Diseases of the central nervous system (including but not limited to any kind of seizures or stroke), and other relevant neurological or psychiatric disorders * History of relevant orthostatic hypotension, fainting spells, or blackouts * Chronic or relevant acute infections * Further

Design outcomes

Primary

Measure	Time frame	Description
Percentage of Subjects With Drug Related Adverse Events (AEs) in Part I	From first dose of study medication until 11 days after the last dose of study medication, up to 25 days	Percentage of subjects with drug related adverse events (AEs) in part I is reported
Area Under the Concentration-time Curve of the BI 425809 in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) Part II	PK samples were taken at: 0, 0:30, 1, 2, 3, 3:30, 4, 4:30, 5, 6, 8, 10, 12, 24, 34, 48, 72, 96 hours after drug administration	Area under the concentration-time curve of the BI 425809 in plasma over the time interval from 0 to the last quantifiable data point (AUC0-tz) part II is reported.
Maximum Measured Concentration of the BI 425809 in Plasma (Cmax) Part II	PK samples were taken at: 0, 0:30, 1, 2, 3, 3:30, 4, 4:30, 5, 6, 8, 10, 12, 24, 34, 48, 72, 96 hours after drug administration	Maximum measured concentration of the BI 425809 in plasma (Cmax) part II.

Secondary

Measure	Time frame	Description
Percentage of Subjects With Drug Related Adverse Events (AEs) in Part II	From first dose of study medication until 11 days after the last dose of study medication, up to 12 days	Percentage of subjects with drug related adverse events (AEs) in part II is reported.
Area Under the Concentration-time Curve of the BI 425809 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC 0-infinity) Part II	PK samples were taken at: 0, 0:30, 1, 2, 3, 3:30, 4, 4:30, 5, 6, 8, 10, 12, 24, 34, 48, 72, 96 hours after drug administration	Area under the concentration-time curve of the BI 425809 in plasma over the time interval from 0 extrapolated to infinity (AUC 0-infinity) part II. After single dosing in the morning as well as in the evening.
Area Under the Concentration-time Curve of the BI 425809 in Plasma Over the Time Interval From 0 to 24 Hours (AUC0-24) Part I	PK plasma samples were taken at: 2 hours before drug administration and 0:30, 1, 2, 3, 3:30, 4, 4:30, 5, 6, 8, 10, 12, 24 hours after the drug administration in YH and EH population	Area under the concentration-time curve of the BI 425809 in plasma over the time interval from 0 to 24 hours (AUC0-24) part I. After the first dose.
Area Under the Concentration-time Curve of the BI 425809 in Plasma at Steady State Over a Uniform Dosing Interval τ (AUCτ,ss) Part I	Up to 528 hours. The details are described in description.	The AUC of BI 425809 in plasma at steady state over a dosing interval (AUCτ,ss) in Part I was evaluated for all arms achieving steady state. For the 75 mg twice-daily multiple-dose arm in young healthy subjects (YH), steady state was not achieved due to nonlinear pharmacokinetics; therefore, AUCτ,ss was not determined. Instead, AUCτ after the final dose (AUCτ,22) was calculated, representing AUC over one dosing interval (τ; dosing interval) after the last dose on Day 14 (22nd dose), not at steady state. PK sampling: 75 mg BID YH: 2 h pre-dose and 0:30, 1-6 h (including 30-minute time points), 8, 10, 12, 24-240 h, 264, 288, 312-324 h (including 30-minute time points), 336, 360, 384, 408, 432, 456, 480, 504, 528 h post-dose. Other arms: 0:30, 1-6 h (including 30-minute time points), 8, 10, 12, 24-240 h, 264-272 h (including 30-minute time points), 288, 360, 384, 408, 432, 456, 480, 504, and 528 h post-dose. Time points 264-272 h apply only to 25 mg multiple-dose arms in YH and EH.
Maximum Measured Concentration of the BI 425809 in Plasma (Cmax) Part I	PK plasma samples were taken at: 0:30, 1, 2, 3, 3:30, 4, 4:30, 5, 6, 8, 10, 12, 24, 34, 48 and 58 hours after drug administration.	Maximum measured concentration of the BI 425809 in plasma (Cmax) part I. After the first dose.
Maximum Measured Concentration of the BI 425809 in Plasma at Steady State Over a Uniform Dosing Interval τ (Cmax,ss) Part I	Up to 528 hours. The details are described in description.	Maximum measured plasma concentration of BI 425809 at steady state over a dosing interval (Cmax,ss) in Part I was evaluated for all treatment arms achieving steady state For the 75 mg twice-daily multiple-dose arm in young healthy subjects (YH), steady state was not achieved due to non-linear pharmacokinetics; therefore, Cmax,ss was not determined. Instead, Cmax after the final dose (Cmax,22) was calculated, representing the maximum observed concentration following the last dose on Day 14 (22nd dose), not at steady-state PK sampling: 75 mg BID YH: 2 h pre-dose and 0:30, 1-6 h (including 30-min time points), 8, 10, 12, 24-240 h, 264, 288, 312-324 h (including 30-min time points), 336, 360, 384, 408, 432, 456, 480, 504, 528 h post-dose Other arms: 0:30, 1-6 h (including 30-min time points), 8, 10, 12, 24-240 h, 264-272 h (including 30-min time points); 288, 360, 384, 408, 432, 456, 480, 504, and 528 h post-dose Time points 264-272 h apply only to 25 mg multiple-dose arms in YH and EH

Countries

Germany

Contacts

STUDY_CHAIRBoehringer Ingelheim

Boehringer Ingelheim

Participant flow

Recruitment details

This Phase I trial evaluated safety, tolerability, and pharmacokinetics of BI 425809 in healthy volunteers: Part 1 tested multiple rising doses (randomized, double-blind, placebo-controlled); Part 2 compared single-dose morning vs evening (randomized, crossover).

Pre-assignment details

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.

Baseline characteristics

Characteristic	—
Age, Continuous	48.1 Years STANDARD_DEVIATION 15.2
Ethnicity (NIH/OMB) Hispanic or Latino	0 Participants
Ethnicity (NIH/OMB) Not Hispanic or Latino	6 Participants
Ethnicity (NIH/OMB) Unknown or Not Reported	0 Participants
Race (NIH/OMB) American Indian or Alaska Native	0 Participants
Race (NIH/OMB) Asian	0 Participants
Race (NIH/OMB) Black or African American	1 Participants
Race (NIH/OMB) More than one race	0 Participants
Race (NIH/OMB) Native Hawaiian or Other Pacific Islander	0 Participants
Race (NIH/OMB) Unknown or Not Reported	0 Participants
Race (NIH/OMB) White	94 Participants
Sex: Female, Male Female	29 Participants
Sex: Female, Male Male	11 Participants

Adverse events

Event type	EG000 affected / at risk	EG001 affected / at risk	EG002 affected / at risk	EG003 affected / at risk	EG004 affected / at risk	EG005 affected / at risk	EG006 affected / at risk	EG007 affected / at risk	EG008 affected / at risk	EG009 affected / at risk	EG010 affected / at risk
deaths Total, all-cause mortality	0 / 15	0 / 6	0 / 9	0 / 9	0 / 9	0 / 9	0 / 9	0 / 9	0 / 9	0 / 12	0 / 11
other Total, other adverse events	8 / 15	3 / 6	5 / 9	7 / 9	8 / 9	6 / 9	8 / 9	6 / 9	6 / 9	2 / 12	0 / 11
serious Total, serious adverse events	0 / 15	0 / 6	0 / 9	0 / 9	0 / 9	0 / 9	0 / 9	0 / 9	0 / 9	0 / 12	0 / 11

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: May 14, 2026