A Study in Healthy Men to Find Out How BI 425809 is Taken up and Handled by the Body

NCT03654170 | Completed Phase 1 Results

• 2 other identifiers: 1346-00162018-001192-21
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

Brief Summary

This trial intends to investigate the basic pharmacokinetics of BI 425809 and \[14C\]- radioactivity, including mass balance, excretion pathways and metabolism following a single oral dose of 25 mg BI 425809 (C-14) given to healthy male subjects

Conditions

Healthy

Outcome Measures

Primary Outcomes (2)

• Mass Balance Recovery of Total [14C]-Radioactivity in Urine (Feurine, 0-t2)

  feurine, 0-t2, fraction of \[14C\]-radioactivity excreted in urine as percentage of the administered dose over the time interval from 0 to t2, where t2 is the last quantifiable data point across all participants mass balance recovery of total \[14C\]-radioactivity in urine.

  PKurine samples were collected within 2 hours predose and within 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, 485-509 and 653-677 hours after dosing on Day 1.

• Mass Balance Recovery of Total [14C]-Radioactivity in Faeces (Fefaeces, 0-t2)

  fefaeces, 0-t2, fraction of \[14C\]-radioactivity excreted in faeces as percentage of the administered dose over the time interval from 0 to t2, where t2 is the last quantifiable data point across all participants mass balance recovery of total \[14C\]-radioactivity in faeces.

  PKfaeces samples were collected within 2 hours predose and within 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, 485-509 and 653-677 hours after dosing on Day 1.

Secondary Outcomes (2)

• Maximum Measured Concentration of the [14C]-Radioactivity and BI 425809 (Cmax)

  PK samples were collected at 2 hours prior to drug administration and at 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 485, 653 hours after drug administration.

• Area Under the Concentration-time Curve of the [14C]-Radioactivity and BI 425809 Over the Time Interval From 0 to the Last Quantifiable Time Point (AUC0-tz)

  PK samples were collected at 2 hours prior to drug administration and at 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 485, 653 hours after drug administration.

Study Arms (1)

BI 425809 XX (C-14)

EXPERIMENTAL

Participants were administered single oral dose of 25 milligram (mg) mixture of Carbon 14 labelled \[14C\] BI 425809 XX, containing a radioactive dose of 3.7 MegaBecquerel (MBq), and unlabeled BI 425809 XX dissolved in 12.5 milliliter (mL) polyethylene glycol 400 (PEG) as solvent, with 240 mL of water after an overnight fast of at least 10 hours (h).

Drug: BI 425809 mixed with [C-14] BI425809

Interventions

BI 425809 mixed with [C-14] BI425809 DRUG

Single oral dose of 25 milligram (mg) mixture of Carbon 14 labelled \[14C\] BI 425809 XX, containing a radioactive dose of 3.7 MegaBecquerel (MBq), and unlabeled BI 425809 XX dissolved in 12.5 milliliter (mL) polyethylene glycol 400 (PEG) as solvent.

Also known as: Iclepertin

BI 425809 XX (C-14)

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Healthy male subjects according to the investigator's assessment, based on a complete medical history including a physical examination, vital signs (BP, PR), 12-lead ECG, and clinical laboratory tests
• Age of 18 to 65 years (incl.)
• 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 GCP and local legislation
• Subjects who are sexually active must use, with their partner, highly effective contraception from the time of administration of trial medication until 4 months after administration of trial medication.
• Subjects are required to use condoms to prevent unintended exposure of the partner to the study drug via seminal fluid. Alternatively, true abstinence is acceptable when it is in line with the subject's preferred and usual lifestyle. If a subject is usually not sexually active but becomes active, with their partner, they must comply with the contraceptive requirements detailed above.

You may not qualify if:

• 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 139 mmHg, diastolic blood pressure outside the range of 45 to 89 mmHg, or pulse rate outside the range of 40 to 100 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
• Clinically significant gastrointestinal, hepatic, renal, respiratory (including but not limited to interstitial lung disease), cardiovascular, metabolic, immunological or hormonal disorders
• Cholecystectomy and/or surgery of the gastrointestinal tract that could interfere with the pharmacokinetics of the trial medication (except appendectomy and simple hernia repair)
• 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
• History of relevant allergy or hypersensitivity (including allergy to the trial medication or its excipients)
• Use of drugs within 30 days prior to administration of trial medication if that might reasonably influence the results of the trial (incl. QT/QTc interval prolongation). Use of CYP3A4 inhibitors and inducers 1 week prior to administration of trial medication
• Participation in another trial where an investigational drug has been administered within 60 days prior to planned administration of trial medication, or current participation in another trial involving administration of investigational drug
• Smoker (more than 5 cigarettes or 1 cigars or 1 pipes per day)
• Inability to refrain from smoking on trial days
• Average intake of more than 24 units of alcohol per week (1 unit of alcohol equals approximately 250 mL of beer, 100 mL of wine or 35 ml of spirits)

Sponsors & Collaborators

• Boehringer Ingelheim: lead

Study Sites (1)

ICON

Groningen, 9728 NZ, Netherlands

Location

Related Publications (1)

• Burkard U, Desch M, Shatillo Y, Wunderlich G, Mack SR, Schlecker C, Teitelbaum AM, Liu P, Chan TS. The Absolute Bioavailability, Absorption, Distribution, Metabolism, and Excretion of BI 425809 Administered as an Oral Dose or an Oral Dose with an Intravenous Microtracer Dose of [14C]-BI 425809 in Healthy Males. Clin Drug Investig. 2022 Jan;42(1):87-99. doi: 10.1007/s40261-021-01111-9. Epub 2021 Dec 22.

  PMID: 34936055 DERIVED

Related Links

• Related Info

MeSH Terms

Interventions

Carbon-14

Results Point of Contact

• Title: Boehringer Ingelheim, Call Center
• Organization: Boehringer Ingelheim

clintriage.rdg@boehringer-ingelheim.com

1-800-243-0127

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: OTHER
• Restrictive Agreement: Yes

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: August 29, 2018
• First Posted: August 31, 2018
• Study Start: September 11, 2018
• Primary Completion: November 12, 2018
• Study Completion: November 12, 2018
• Last Updated: March 27, 2026
• Results First Posted: March 27, 2026

Record last verified: 2026-02

Data Sharing

• IPD Sharing: Will not share

Locations

NL (1)