Safety, Tolerability, and Pharmacokinetics of Single Doses BI 425809

Safety, Tolerability, and Pharmacokinetics of Single Rising Oral Doses of BI 425809 in Healthy Male Subjects (Partially Randomised, Single-blind, Placebo-controlled) and Investigation of Relative Bioavailability and Food Effect of BI 425809 (Open-label, Randomised, Three-way Crossover)

To investigate safety, tolerability, and pharmacokinetics of BI 425809 following single rising doses of BI 425809 in healthy male volunteers; To explore dose proportionality of BI 425809 as oral drinking solution; To investigate relative bioavailability of BI 425809 oral drinking solution fasted compared to BI 425809 tablet fasted and tablet fed

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Placebo PfOS; Drug: BI 425809 PfOS; Drug: BI 425809 tablet

• Study Type: Interventional
• Enrollment (Actual): 83
• Phase: Phase 1

Contacts and Locations

Study Locations

• Germany
  • Ingelheim, Germany
    • 1346.1.1 Boehringer Ingelheim Investigational Site

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 45 years (Adult)
• Accepts Healthy Volunteers: Yes

Description

Inclusion criteria:

• Healthy male subjects
• Age 18 to 45 years (incl.)
• Body mass index (BMI) 18.5 to 29.9 kg/m2 (incl.)
• Subject must be able to understand and comply with study requirements

Exclusion criteria:

• Any finding in the medical examination (including blood pressure (BP), pulse rate (PR) or electrocardiogram (ECG)) deviating from normal and judged clinically relevant by the investigator
• Repeated measurement of systolic blood pressure <90 or >140 mmHg, or diastolic blood pressure <50 or >90 mmHg, or pulse rate <50 or >90
• Any laboratory value outside the reference range that the investigator considers to be of clinical relevance
• Any evidence of a concomitant disease judged 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 study drug(s)
• Diseases of the central nervous system (such as epilepsy), other neurological disorders or psychiatric disorders

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

16

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Placebo Comparator: SRD Part: Placebo; Participants received a single dose of oral solution of placebo matching BI 425809. SRD = Single Rising Dose.	Drug: Placebo PfOS; Placebo as a powder for an oral solution (PfOS)
Experimental: SRD Part: 0.5 mg BI 425809; Participants received a single dose of oral solution containing 0.5 milligrams (mg) of BI 425809. SRD = Single Rising Dose.	Drug: BI 425809 PfOS; BI 425809 as a powder for an oral solution (PfOS); Other Names: Iclepertin
Experimental: SRD Part: 1 mg BI 425809; Participants received a single dose of oral solution containing 1 milligram (mg) of BI 425809. SRD = Single Rising Dose.	Drug: BI 425809 PfOS; BI 425809 as a powder for an oral solution (PfOS); Other Names: Iclepertin
Experimental: SRD Part: 2 mg BI 425809; Participants received a single dose of oral solution containing 2 milligrams (mg) of BI 425809. SRD = Single Rising Dose.	Drug: BI 425809 PfOS; BI 425809 as a powder for an oral solution (PfOS); Other Names: Iclepertin
Experimental: SRD Part: 5 mg BI 425809; Participants received a single dose of oral solution containing 5 milligrams (mg) of BI 425809. SRD = Single Rising Dose.	Drug: BI 425809 PfOS; BI 425809 as a powder for an oral solution (PfOS); Other Names: Iclepertin
Experimental: SRD Part: 10 mg BI425809; Participants received a single dose of oral solution containing 10 milligrams (mg) of BI 425809. SRD = Single Rising Dose.	Drug: BI 425809 PfOS; BI 425809 as a powder for an oral solution (PfOS); Other Names: Iclepertin
Experimental: SRD Part: 25 mg BI 425809; Participants received a single dose of oral solution containing 25 milligrams (mg) of BI 425809. SRD = Single Rising Dose.	Drug: BI 425809 PfOS; BI 425809 as a powder for an oral solution (PfOS); Other Names: Iclepertin
Experimental: SRD Part: 50 mg BI 425809; Participants received a single dose of oral solution containing 50 milligrams (mg) of BI 425809. SRD = Single Rising Dose.	Drug: BI 425809 PfOS; BI 425809 as a powder for an oral solution (PfOS); Other Names: Iclepertin
Experimental: SRD Part: 100 mg BI 425809; Participants received a single dose of oral solution containing 100 milligrams (mg) of BI 425809. SRD = Single Rising Dose.	Drug: BI 425809 PfOS; BI 425809 as a powder for an oral solution (PfOS); Other Names: Iclepertin
Experimental: SRD Part: 150 mg BI 425809; Participants received a single dose of oral solution containing 150 milligrams (mg) of BI 425809. SRD = Single Rising Dose.	Drug: BI 425809 PfOS; BI 425809 as a powder for an oral solution (PfOS); Other Names: Iclepertin
Experimental: BA/FE Part: 25 mg BI 425809, R/T1/T2; Participants were administered 25 mg of BI 425809 as a tablet without food (reference treatment R), 25 mg of BI 425809 as a tablet after a standardized high-fat, high-calorie meal (test treatment T1), and 25 mg of BI 425809 as a powder in an oral solution without food (test treatment T2). The 3 treatments were separated by a washout period of at least 14 days. BA = Bioavailability, FE = Food Effect.	Drug: BI 425809 PfOS; BI 425809 as a powder for an oral solution (PfOS); Other Names: Iclepertin; Drug: BI 425809 tablet; BI 425809 as a tablet; Other Names: Iclepertin
Experimental: BA/FE Part: 25 mg BI 425809, R/T2/T1; Participants were administered 25 mg of BI 425809 as a tablet without food (reference treatment R), 25 mg of BI 425809 as a powder in an oral solution without food (test treatment T2), and 25 mg of BI 425809 as a tablet after a standardized high-fat, high-calorie meal (test treatment T1). The 3 treatments were separated by a washout period of at least 14 days. BA = Bioavailability, FE = Food Effect.	Drug: BI 425809 PfOS; BI 425809 as a powder for an oral solution (PfOS); Other Names: Iclepertin; Drug: BI 425809 tablet; BI 425809 as a tablet; Other Names: Iclepertin
Experimental: BA/FE Part: 25 mg BI 425809, T1/T2/R; Participants were administered 25 mg of BI 425809 as a tablet after a standardized high-fat, high-calorie meal (test treatment T1), 25 mg of BI 425809 as a powder in an oral solution without food (test treatment T2), and 25 mg of BI 425809 as a tablet without food (reference treatment R). The 3 treatments were separated by a washout period of at least 14 days. BA = Bioavailability, FE = Food Effect.	Drug: BI 425809 PfOS; BI 425809 as a powder for an oral solution (PfOS); Other Names: Iclepertin; Drug: BI 425809 tablet; BI 425809 as a tablet; Other Names: Iclepertin
Experimental: BA/FE Part: 25 mg BI 425809, T1/R/T2; Participants were administered 25 mg of BI 425809 as a tablet after a standardized high-fat, high-calorie meal (test treatment T1), 25 mg of BI 425809 as a tablet without food (reference treatment R), and 25 mg of BI 425809 as a powder in an oral solution without food (test treatment T2). The 3 treatments were separated by a washout period of at least 14 days. BA = Bioavailability, FE = Food Effect.	Drug: BI 425809 PfOS; BI 425809 as a powder for an oral solution (PfOS); Other Names: Iclepertin; Drug: BI 425809 tablet; BI 425809 as a tablet; Other Names: Iclepertin
Experimental: BA/FE Part: 25 mg BI 425809, T2/T1/R; Participants were administered 25 mg of BI 425809 as a powder in an oral solution without food (test treatment T2), 25 mg of BI 425809 as a tablet after a standardized high-fat, high-calorie meal (test treatment T1), and 25 mg of BI 425809 as a tablet without food (reference treatment R). The 3 treatments were separated by a washout period of at least 14 days. BA = Bioavailability, FE = Food Effect.	Drug: BI 425809 PfOS; BI 425809 as a powder for an oral solution (PfOS); Other Names: Iclepertin; Drug: BI 425809 tablet; BI 425809 as a tablet; Other Names: Iclepertin
Experimental: BA/FE Part: 25 mg BI 425809, T2/R/T1; Participants were administered 25 mg of BI 425809 as a powder in an oral solution without food (test treatment T2), 25 mg of BI 425809 as a tablet without food (reference treatment R), and 25 mg of BI 425809 as a tablet after a standardized high-fat, high-calorie meal (test treatment T1). The 3 treatments were separated by a washout period of at least 14 days. BA = Bioavailability, FE = Food Effect.	Drug: BI 425809 PfOS; BI 425809 as a powder for an oral solution (PfOS); Other Names: Iclepertin; Drug: BI 425809 tablet; BI 425809 as a tablet; Other Names: Iclepertin

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Number of Participants With Drug-related Adverse Events (AE)	Number of participants with drug-related Adverse Events (AE). Drug-relatedness was assessed by the investigator.	SRD Part: From the time of first drug administration until the end of study, up to 18 days for each intervention. BA/FE Part: From the time of first drug administration until the end of study, up to 18 days for each intervention.

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
SRD Part: Maximum Concentration of BI 425809 in Plasma (Cmax)	Maximum measured concentration of BI 425809 in plasma (Cmax) in the Single Rising Dose (SRD) part of the trial is reported.	2 hours (h) before drug administration and 15 minutes (m), 30m, 45m, 1h, 1h30m, 2h, 3h, 4h, 5h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, 96h, 120h, 144h, 168h, 192h after drug administration.
BA/FE Part: Maximum Concentration of BI 425809 in Plasma (Cmax)	Maximum measured concentration of BI 425809 in plasma (Cmax) in the bioavailability/food effect (BA/FE) part of the trial is reported.	2 hours (h) before drug administration and 15 minutes (m), 30m, 45m, 1h, 1h30m, 2h, 3h, 4h, 5h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, 96h, 120h, 144h, 168h, 192h after drug administration.
SRD Part: Area Under the Concentration-time Curve of BI 425809 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC(0-∞))	Area under the concentration-time curve of BI 425809 in plasma over the time interval from 0 extrapolated to infinity (AUC(0-∞)) in the Single Rising Dose (SRD) part of the trial is reported.	2 hours (h) before drug administration and 15 minutes (m), 30m, 45m, 1h, 1h30m, 2h, 3h, 4h, 5h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, 96h, 120h, 144h, 168h, 192h after drug administration.
BA/FE Part: Area Under the Concentration-time Curve of BI 425809 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC(0-∞))	Area under the concentration-time curve of BI 425809 in plasma over the time interval from 0 extrapolated to infinity (AUC(0-∞)) in the Bioavailability/Food Effect (BA/FE) part of the trial is reported.	2 hours (h) before drug administration and 15 minutes (m), 30m, 45m, 1h, 1h30m, 2h, 3h, 4h, 5h, 6h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, 96h, 120h, 144h, 168h, 192h after drug administration.

Collaborators and Investigators

• Sponsor: Boehringer Ingelheim
• Investigators: Study Chair: Boehringer Ingelheim, Boehringer Ingelheim

Publications and helpful links

General Publications

• Moschetti V, Desch M, Goetz S, Liesenfeld KH, Rosenbrock H, Kammerer KP, Wunderlich G, Wind S. Safety, Tolerability and Pharmacokinetics of Oral BI 425809, a Glycine Transporter 1 Inhibitor, in Healthy Male Volunteers: A Partially Randomised, Single-Blind, Placebo-Controlled, First-in-Human Study. Eur J Drug Metab Pharmacokinet. 2018 Apr;43(2):239-249. doi: 10.1007/s13318-017-0440-z.

Helpful Links

• Related Info

Study record dates

Study Major Dates

• Study Start (Actual): March 20, 2014
• Primary Completion (Actual): September 10, 2014
• Study Completion (Actual): September 10, 2014

Study Registration Dates

• First Submitted: February 20, 2014
• First Submitted That Met QC Criteria: February 20, 2014
• First Posted (Estimated): February 21, 2014

Study Record Updates

• Last Update Posted (Actual): May 5, 2026
• Last Update Submitted That Met QC Criteria: April 15, 2026
• Last Verified: April 1, 2026

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Nootropic Agents; BI 425809
• Other Study ID Numbers: 1346.1; 2013-004937-34 (EudraCT Number: EudraCT)

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