Safety, Tolerability, and Pharmacokinetics of Multiple Rising Doses of BI 425809 Tablets for 12 Days to Young and Elderly Healthy Male and Female Volunteers and Comparison of Pharmacokinetics of a Single Oral Dose of BI 425809 (Morning Versus Evening)

NCT02337283 | Completed Phase 1

• 2 other identifiers: 1346.22014-004390-16
• Study Type: interventional
• Target: 96
• Locations: 1 country
• Sites: 1

Brief Summary

The aim of the study is to investigate the safety, tolerability, and pharmacokinetics of multiple rising doses of BI 425809 tablets given orally once daily for 12 days to young and elderly healthy male and female volunteers and to compare single dose pharmacokinetics of BI 425809 given in the morning and in the evening.

Conditions

Healthy

Outcome Measures

Primary Outcomes (3)

• frequency [N(%)] of subjects with drug related adverse events (AEs)

  up to 25 days after first drug administration

• AUC0-tz (area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the last quantifiable data point) only part II

  up to 96 hours

• Cmax (maximum measured concentration of the analyte in plasma) only part II

  up to 96 hours

Secondary Outcomes (5)

• Cmax (maximum measured concentration of the analyte in plasma)

  up to 72 hours after first dose

• AUCt,ss (area under the concentration-time curve of the analyte in plasma at steady state over a uniform dosing interval t)

  up to 216 hours after last dose

• Cmax,ss (maximum measured concentration of the analyte in plasma at steady state over a uniform dosing interval t)

  up to 216 hours after last dose

• AUC0-infinity (area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity) only part II

  up to 96 hours

• AUCt 0-24(area under the concentration-time curve of the analyte in plasma over a uniform dosing interval t after administration of the first dose)

  up to 72 hours after first dose

Study Arms (7)

BI 425809 very low dose - part I

EXPERIMENTAL

Part I only - very low dose tablet, oral administration with 240 ml water, over 14 days

Drug: BI 425809

Placebo - part I

PLACEBO COMPARATOR

Part I only - placebo tablet, oral administration with 240ml water, over 14 days

Drug: Placebo

BI 425809 low dose - part I

EXPERIMENTAL

Part I - low dose tablet, oral administration with 240 ml water, over 14 days

Drug: BI 425809

BI 425809 medium dose - part I

EXPERIMENTAL

Part I only - medium dose tablet, oral administration with 240 ml water, over 14 days

Drug: BI 425809

BI 425809 high dose -part I

EXPERIMENTAL

Part I only - high dose tablet, oral administration with 240 ml water, over 14 days

Drug: BI 425809

BI 425809 low dose - part II

EXPERIMENTAL

Part II - one low dose tablet on day 1 of visit 2 and 2a

Drug: BI 425809

BI 425809 very high dose -part I

EXPERIMENTAL

Part I only - very high dose tablet, oral administration with 240 ml water, over 14 days

Drug: BI 425809

Interventions

BI 425809 DRUG

Tablets

Also known as: Iclepertin

BI 425809 high dose -part I; BI 425809 low dose - part I; BI 425809 low dose - part II; BI 425809 medium dose - part I; BI 425809 very high dose -part I; BI 425809 very low dose - part I

Placebo DRUG

Tablets

Placebo - part I

Eligibility Criteria

• Age: 18 Years - 85 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Healthy male or female subjects according to the investigator´s assessment, 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 50 years (incl.) for young healthy volunteers or age of 65 to 80 years (incl.) for elderly healthy volunteers
• Body mass index (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
• Female subjects who meet any of the following criteria:
• Surgically sterilised
• Postmenopausal, defined as at least 1 year of spontaneous amenorrhea (in questionable cases a blood sample with simultaneous levels of follicle stimulating hormone (FSH) above 40 U/L and estradiol below 30 ng/L is confirmatory)

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 140 mmHg, diastolic blood pressure outside the range of 50 to 90 mmHg in young subjects, and systolic blood pressure greater than 150 mmHg, diastolic blood pressure greater than 95 mmHg in elderly subjects, 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
• Surgery of the gastrointestinal tract that could interfere with kinetics of the trial medication
• 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

Sponsors & Collaborators

• Boehringer Ingelheim: lead

Study Sites (1)

1346.2.1 Boehringer Ingelheim Investigational Site

Mannheim, Germany

Location

Related Publications (1)

• Moschetti V, Schlecker C, Wind S, Goetz S, Schmitt H, Schultz A, Liesenfeld KH, Wunderlich G, Desch M. Multiple Rising Doses of Oral BI 425809, a GlyT1 Inhibitor, in Young and Elderly Healthy Volunteers: A Randomised, Double-Blind, Phase I Study Investigating Safety and Pharmacokinetics. Clin Drug Investig. 2018 Aug;38(8):737-750. doi: 10.1007/s40261-018-0660-2.

  PMID: 29846887 DERIVED

MeSH Terms

Interventions

BI 425809

Study Officials

• Boehringer Ingelheim

  Boehringer Ingelheim

  STUDY CHAIR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: DOUBLE
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: January 9, 2015
• First Posted: January 13, 2015
• Study Start: January 1, 2015
• Primary Completion: November 1, 2015
• Study Completion: November 1, 2015
• Last Updated: September 20, 2024

Record last verified: 2024-09

Locations

DE (1)