A Study in Healthy Men to Test Whether Rifampicin Influences the Amount of BI 425809 in the Blood

Effects of Rifampicin on the Pharmacokinetics of BI 425809 Following Oral Administration in Healthy Male Subjects (an Open-label, Two-period, Fixed-sequence Trial)

The primary objective of this trial is to investigate the relative bioavailability of a single dose of BI 425809 when given alone (Reference, B) compared with co-administration (Test, A) on the 7th day of a 10-day treatment with rifampicin following oral administration in healthy male volunteers.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Rifampicin; Drug: BI 425809

• Study Type: Interventional
• Enrollment (Actual): 16
• Phase: Phase 1

Contacts and Locations

Study Locations

• Germany
  • Biberach, Germany, 88397
    • Humanpharmakologisches Zentrum Biberach

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes

Description

Inclusion Criteria:

• Healthy male subjects according to the assessment of the investigator, 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 55 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 Good Clinical Practice (GCP) and local legislation

Exclusion Criteria:

• Any finding in the medical examination (including Blood Pressure (BP), Pulse Rate (PR) or Electrocardiogram (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, 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
• 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)
• 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 10 cigarettes or 3 cigars or 3 pipes per day)
• Inability to refrain from smoking on specified trial days
• Alcohol abuse (consumption of more than 20 g per day)
• 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 one week prior to administration of trial medication or during the trial
• Inability to comply with dietary regimen of trial site
• Subject is assessed as unsuitable for inclusion by the investigator, for instance, because considered not able to understand and comply with study requirements, or has a condition that would not allow safe participation in the study

In addition, the following trial-specific exclusion criteria apply:

• History of relevant liver diseases such as disturbance of liver function, jaundice, drug induced liver injury, Dubin-Johnson syndrome, Rotor syndrome, or liver tumours
• Thrombocytes below lower limit of normal or liver enzymes (Alanine transaminase (ALT), Aspartate transaminase (AST), Gamma-Glutamyl transpeptidase (GGT), Alkaline phosphatase (AP)) above upper limit of normal at the screening examination

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 alone (reference, Treatment B) then BI 425809 + Rifampicin (test, Treatment A); BI 425809 alone (reference, Treatment B): Subjects were administered with a single dose of 25 mg BI 425809 orally in the morning after an overnight fast for a single day. BI 425809 + Rifampicin (test, Treatment A): Subjects were administered with multiple doses of 1 film coated tablet of Rifampicin (Eremfat®) 600 mg orally in the evening for 10 days and a single dose of 25 mg BI 425809 was administered on the seventh day of rifampicin (Eremfat®) treatment. The administrations of the single dose of BI 425809 in the first period and in the following combined treatment period were separated by a washout period of at least 49 days.

Drug: Rifampicin; once daily; Drug: BI 425809; once daily; Other Names: Iclepertin

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Area Under the Plasma Concentration-time Curve From 0 to 168 Hours Time Point of BI 425809 (AUC0-168).	This endpoint calculates area under the concentration-time curve of BI 425809 in plasma over the time interval from 0 to 168 hour time point. Geometric least square mean (adjusted geometric mean) and adjusted geometric standard error were calculated using an analysis of variance (ANOVA) model on the logarithmic scale including subject as random effect and treatment as fixed effect.	Pharmacokinetic samples were collected at 2:00 hour Pre-dose and at 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 3:30, 4:00, 4:30, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 34:00, 48:00, 72:00, 96:00 and 168:00 hours post dose.
Maximum Concentration of BI 425809 in Plasma (Cmax).	This outcome is maximum measured concentration of the BI 425809 in plasma.	Pharmacokinetic samples were collected at 2:00 hour Pre-dose and at 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 3:30, 4:00, 4:30, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 34:00, 48:00, 72:00, 96:00 and 168:00 hours post dose.

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Area Under the Concentration-time Curve of BI 425809 in Plasma With and Without Co-administration of Rifampicin Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞).	This endpoint calculates area under the concentration-time curve of BI 425809 in plasma with and without adminstration of Rifampicin over the time interval from 0 extrapolated to infinity.	Pharmacokinetic samples were collected at 2:00 hour Pre-dose and at 0:30, 1:00, 1:30, 2:00, 2:30, 3:00, 3:30, 4:00, 4:30, 5:00, 6:00, 8:00, 10:00, 12:00, 24:00, 34:00, 48:00, 72:00, 96:00 and 168:00 hours post dose.
Terminal Half-life of the Metabolite BI 761036 in Plasma (t1/2)	Half life is the period of time required for the concentration or amount of drug in the body to be reduced to exactly one-half of a given concentration or amount.	Pharmacokinetic samples were collected at 2:00 hour Pre-dose and at 3:00, 6:00, 12:00, 24:00, 34:00, 48:00, 72:00, 96:00, 168:00, 216:00, 264:00, 336:00, 408:00, 504:00, 576:00, 672:00, 744:00, 840:00 and 1008:00 hours post dose.

Collaborators and Investigators

• Sponsor: Boehringer Ingelheim

Publications and helpful links

General Publications

• Desch M, Wunderlich G, Goettel M, Goetz S, Liesenfeld KH, Chan TS, Rosenbrock H, Sennewald R, Link J, Keller S, Wind S. Effects of Cytochrome P450 3A4 Induction and Inhibition on the Pharmacokinetics of BI 425809, a Novel Glycine Transporter 1 Inhibitor. Eur J Drug Metab Pharmacokinet. 2022 Jan;47(1):91-103. doi: 10.1007/s13318-021-00723-y. Epub 2021 Oct 29.

Helpful Links

• Related Info

Study record dates

Study Major Dates

• Study Start (Actual): March 28, 2017
• Primary Completion (Actual): June 20, 2017
• Study Completion (Actual): June 20, 2017

Study Registration Dates

• First Submitted: March 10, 2017
• First Submitted That Met QC Criteria: March 13, 2017
• First Posted (Actual): March 17, 2017

Study Record Updates

• Last Update Posted (Actual): March 30, 2026
• Last Update Submitted That Met QC Criteria: March 10, 2026
• Last Verified: March 1, 2026

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Heterocyclic Compounds; Heterocyclic Compounds, Fused-Ring; Polycyclic Compounds; Heterocyclic Compounds, 4 or More Rings; Rifamycins; Lactams, Macrocyclic; Macrocyclic Compounds; BI 425809; Rifampin
• Other Study ID Numbers: 1346-0018; 2016-004862-24 (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