Safety, Tolerability, and Pharmacokinetics of Single Doses BI 425809

NCT02068690 | Completed Phase 1 Results

• 2 other identifiers: 1346.12013-004937-34
• Study Type: interventional
• Target: 83
• Locations: 1 country
• Sites: 1

Brief Summary

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

Conditions

Healthy

Outcome Measures

Primary Outcomes (1)

• 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 Outcomes (4)

• SRD Part: Maximum Concentration of BI 425809 in Plasma (Cmax)

  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)

  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-∞))

  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-∞))

  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.

Study Arms (16)

SRD Part: Placebo

PLACEBO COMPARATOR

Participants received a single dose of oral solution of placebo matching BI 425809. SRD = Single Rising Dose.

Drug: Placebo PfOS

SRD Part: 0.5 mg BI 425809

EXPERIMENTAL

Participants received a single dose of oral solution containing 0.5 milligrams (mg) of BI 425809. SRD = Single Rising Dose.

Drug: BI 425809 PfOS

SRD Part: 1 mg BI 425809

EXPERIMENTAL

Participants received a single dose of oral solution containing 1 milligram (mg) of BI 425809. SRD = Single Rising Dose.

Drug: BI 425809 PfOS

SRD Part: 2 mg BI 425809

EXPERIMENTAL

Participants received a single dose of oral solution containing 2 milligrams (mg) of BI 425809. SRD = Single Rising Dose.

Drug: BI 425809 PfOS

SRD Part: 5 mg BI 425809

EXPERIMENTAL

Participants received a single dose of oral solution containing 5 milligrams (mg) of BI 425809. SRD = Single Rising Dose.

Drug: BI 425809 PfOS

SRD Part: 10 mg BI425809

EXPERIMENTAL

Participants received a single dose of oral solution containing 10 milligrams (mg) of BI 425809. SRD = Single Rising Dose.

Drug: BI 425809 PfOS

SRD Part: 25 mg BI 425809

EXPERIMENTAL

Participants received a single dose of oral solution containing 25 milligrams (mg) of BI 425809. SRD = Single Rising Dose.

Drug: BI 425809 PfOS

SRD Part: 50 mg BI 425809

EXPERIMENTAL

Participants received a single dose of oral solution containing 50 milligrams (mg) of BI 425809. SRD = Single Rising Dose.

Drug: BI 425809 PfOS

SRD Part: 100 mg BI 425809

EXPERIMENTAL

Participants received a single dose of oral solution containing 100 milligrams (mg) of BI 425809. SRD = Single Rising Dose.

Drug: BI 425809 PfOS

SRD Part: 150 mg BI 425809

EXPERIMENTAL

Participants received a single dose of oral solution containing 150 milligrams (mg) of BI 425809. SRD = Single Rising Dose.

Drug: BI 425809 PfOS

BA/FE Part: 25 mg BI 425809, R/T1/T2

EXPERIMENTAL

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; Drug: BI 425809 tablet

BA/FE Part: 25 mg BI 425809, R/T2/T1

EXPERIMENTAL

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; Drug: BI 425809 tablet

BA/FE Part: 25 mg BI 425809, T1/T2/R

EXPERIMENTAL

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; Drug: BI 425809 tablet

BA/FE Part: 25 mg BI 425809, T1/R/T2

EXPERIMENTAL

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; Drug: BI 425809 tablet

BA/FE Part: 25 mg BI 425809, T2/T1/R

EXPERIMENTAL

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; Drug: BI 425809 tablet

BA/FE Part: 25 mg BI 425809, T2/R/T1

EXPERIMENTAL

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; Drug: BI 425809 tablet

Interventions

BI 425809 PfOS DRUG

BI 425809 as a powder for an oral solution (PfOS)

Also known as: Iclepertin

BA/FE Part: 25 mg BI 425809, R/T1/T2; BA/FE Part: 25 mg BI 425809, R/T2/T1; BA/FE Part: 25 mg BI 425809, T1/R/T2; BA/FE Part: 25 mg BI 425809, T1/T2/R; BA/FE Part: 25 mg BI 425809, T2/R/T1; BA/FE Part: 25 mg BI 425809, T2/T1/R; SRD Part: 0.5 mg BI 425809; SRD Part: 1 mg BI 425809; SRD Part: 10 mg BI425809; SRD Part: 100 mg BI 425809; SRD Part: 150 mg BI 425809; SRD Part: 2 mg BI 425809; SRD Part: 25 mg BI 425809; SRD Part: 5 mg BI 425809; SRD Part: 50 mg BI 425809

BI 425809 tablet DRUG

BI 425809 as a tablet

Also known as: Iclepertin

BA/FE Part: 25 mg BI 425809, R/T1/T2; BA/FE Part: 25 mg BI 425809, R/T2/T1; BA/FE Part: 25 mg BI 425809, T1/R/T2; BA/FE Part: 25 mg BI 425809, T1/T2/R; BA/FE Part: 25 mg BI 425809, T2/R/T1; BA/FE Part: 25 mg BI 425809, T2/T1/R

Placebo PfOS DRUG

Placebo as a powder for an oral solution (PfOS)

SRD Part: Placebo

Eligibility Criteria

• Age: 18 Years - 45 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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

You may not qualify if:

• 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

Sponsors & Collaborators

• Boehringer Ingelheim: lead

Study Sites (1)

1346.1.1 Boehringer Ingelheim Investigational Site

Ingelheim, Germany

Location

Related Publications (1)

• 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.

  PMID: 29076028 DERIVED

Related Links

• Related Info

MeSH Terms

Interventions

BI 425809

Results Point of Contact

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

clintriage.rdg@boehringer-ingelheim.com

800-243-0127

Study Officials

• Boehringer Ingelheim

  Boehringer Ingelheim

  STUDY CHAIR

Publication Agreements

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

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Masking Details: In Part 1 of this study, single-blind conditions regarding the subjects' treatment were maintained within each dose group, but the current dose level was known to subjects and investigators. Part 2 of this study did not have masking and treatments were open-label.
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Model Details: Part 1 of this study was conducted as a sequential assignment, while Part 2 of this study was conducted as a crossover assignment.

Study Record Dates

• First Submitted: February 20, 2014
• First Posted: February 21, 2014
• Study Start: March 20, 2014
• Primary Completion: September 10, 2014
• Study Completion: September 10, 2014
• Last Updated: May 5, 2026
• Results First Posted: May 5, 2026

Record last verified: 2026-04

Data Sharing

• IPD Sharing: Will not share

Locations

DE (1)