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

Metabolism and Pharmacokinetics of BI 425809 After Administration of BI 425809 (C-14) as Oral Solution in Healthy Male Volunteers

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

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: BI 425809 mixed with [C-14] BI425809

• Study Type: Interventional
• Enrollment (Actual): 6
• Phase: Phase 1

Contacts and Locations

Study Locations

• Netherlands
  • Groningen, Netherlands, 9728 NZ
    • ICON

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 65 years (Adult, Older Adult)
• Accepts Healthy Volunteers: Yes

Description

Inclusion Criteria:

• 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.

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 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)
• Drug abuse or positive drug screening
• Blood donation of more than 100 mL within 30 days prior to administration of trial medication or intended donation during the trial
• Intention to perform excessive physical activities within 4 days prior to administration of trial medication or during the trial
• Inability to comply with dietary regimen of trial site
• A marked baseline prolongation of QT/QTc interval (such as QTc intervals that are repeatedly greater than 450 ms) or any other relevant ECG finding at screening
• A history of additional risk factors for Torsades de Pointes (such as heart failure, hypokalemia, or family history of Long QT Syndrome)
• Further exclusion criteria apply

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: BI 425809 XX (C-14); 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; 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.; Other Names: Iclepertin

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
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 Outcome Measures

Outcome Measure	Measure Description	Time Frame
Maximum Measured Concentration of the [14C]-Radioactivity and BI 425809 (Cmax)	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)	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). For [14C]-radioactivity the latest tz was 653 h whereas for BI 425809 the latest tz was 336 h.	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.

Collaborators and Investigators

• Sponsor: Boehringer Ingelheim

Publications and helpful links

General Publications

• 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.

Helpful Links

• Related Info

Study record dates

Study Major Dates

• Study Start (Actual): September 11, 2018
• Primary Completion (Actual): November 12, 2018
• Study Completion (Actual): November 12, 2018

Study Registration Dates

• First Submitted: August 29, 2018
• First Submitted That Met QC Criteria: August 29, 2018
• First Posted (Actual): August 31, 2018

Study Record Updates

• Last Update Posted (Actual): March 27, 2026
• Last Update Submitted That Met QC Criteria: March 10, 2026
• Last Verified: February 1, 2026

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Nootropic Agents; Carbon-14
• Other Study ID Numbers: 1346-0016; 2018-001192-21 (EudraCT Number)

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

IPD Plan Description

Clinical studies sponsored by Boehringer Ingelheim, phases I to IV, interventional and non-interventional, are in scope for sharing of the raw clinical study data and clinical study documents. Exceptions might apply, e.g. studies in products where Boehringer Ingelheim is not the license holder; studies regarding pharmaceutical formulations and associated analytical methods, and studies pertinent to pharmacokinetics using human biomaterials; studies conducted in a single center or targeting rare diseases (in case of low number of patients and therefore limitations with anonymization).

For more details refer to: https://www.clinicalstudies.boehringer-ingelheim.com/msw/datasharing

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No