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OpenTrials
Completed

NCT Number: NCT04426851

A Study in Healthy Men to Test How BI 1358894 is Taken up in the Body and How Food Influences the Amount of BI 1358894 in the Blood

The main objective of Part 1 of this trial is to investigate the absolute bioavailability of BI 1358894 with an intravenous microdose formulation containing labelled [C-14] BI 1358894 and an unlabelled oral tablet formulation of BI 1358894 in healthy male subjects.

The main objective of Part 2 of this trial is to investigate the relative bioavailability of BI 1358894 administered as an oral suspension.

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Key information

Conditions

Age range

18 year–55 year

Sex eligibility

Male

Study type

Interventional

Phase

Phase 1

Primary location

ICON

Groningen, 9728 NZ, Netherlands

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

Inclusion criteria

  • Healthy male subjects according to the assessment of the investigator, as 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 55 years (inclusive)
  • BMI of 18.5 to 29.9 kg/m2 (inclusive)
  • Signed and dated written informed consent prior to admission to the study, in accordance with GCP and local legislation
  • Male subjects who meet any of the following criteria from at least 30 days before the first administration of trial medication until 90 days after trial completion:
  • Use of adequate contraception of the female partner, e.g. any of the following methods plus condom: implants, injectables, combined oral or vaginal contraceptives, intrauterine device that started at least 2 months prior to first study drug administration or barrier method (e.g. diaphragm with spermicide) or,
  • Sexually abstinent or
  • A vasectomy performed at least 1 year prior to screening (with medical assessment of the surgical success) or
  • Surgically sterilised female partner (including hysterectomy, bilateral tubal occlusion or bilateral oophorectomy) or
  • Postmenopausal female partner, defined as at least 1 year of spontaneous amenorrhea (in questionable cases a blood sample with FSH (follicle stimulating hormone) above 40 U/L and estradiol below 30 ng/L is confirmatory)

Exclusion criteria

  • Any finding in the medical examination (including BP, PR or ECG) deviating from normal and assessed 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 40 to 100 bpm
  • C-reactive protein (CRP) > upper limit of normal (ULN), liver or kidney parameter above ULN
  • Any laboratory value outside the reference range that the investigator considers to be of clinical relevance
  • Any evidence of a concomitant disease assessed as clinically relevant by the investigator
  • Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
  • Cholecystectomy or other surgery of the gastrointestinal tract that could interfere with the pharmacokinetics of the trial medication (except appendectomy or 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
  • Further exclusion criteria apply

Treatment and study plan

BI 1358894

Drug

Tablet

BI 1358894 (C-14) intravenous solution

Drug

BI 1358894 mixed with [carbon labelled (C-14)] BI 1358894

Primary outcomes

  1. Part 1: Area Under the Concentration-time Curve of BI 1358894 Over the Time Interval From 0 to Infinity After i.v. Administration and After Oral Administration (AUC0-infinity)

    Time frame: Within 2 hours (h) before and at 15 minutes (min), 30 min, 1 h, 1.5, 2, 3, 4, 5, 5.083, 5.16, 5.25, 5.5, 5.75, 6, 6.5, 7,8, 10, 12, 24, 34, 48, 72, 96, 144, 192, 240, 312 h after oral dose of BI 1358894 on Day 1 of Period 1. Continues in description.

    Area under the concentration-time curve of BI 1358894 over the time interval from 0 to infinity after i.v. administration and after oral administration (AUC0-infinity) is reported. The values were calculated using the Analysis of variance (ANOVA) model which included effects accounting for the following sources of variation: 'subjects' and 'formulation'. The effect 'subjects' was considered as random, whereas 'formulation' was considered as fixed.

    Standard error is actually geometric standard error. Time Frame: For "BI 1358894 (C-14) 100 ug i.v" samples were collected at 5h, 5.083, 5.16, 5.25, 5.5, 5.75, 6, 6.5, 7,8, 10, 12, 24, 34, 48, 72, 96, 144, 192, 240, 312 h after oral dose of BI 1358894 on Day 1 of Period 1.

  2. Part 2: Area Under the Concentration-time Curve of BI 1358894 in Plasma Over the Time Interval From 0 to 312 h (AUC 0-312)

    Time frame: Within 2 hours (h) before drug administration and at 15 minutes (min), 30 min, 1 h, 1.5, 2, 3, 4, 5, 6, 7,8, 10, 12, 24, 34, 48, 72, 96, 144, 192, 240, 312 h after administration of BI 1358894.

    Area under the concentration-time curve of BI 1358894 in plasma over the time interval from 0 to 312 h (AUC 0-312) is reported. The values were calculated using the Analysis of variance (ANOVA) model which included effects accounting for the following sources of variation: 'sequence or block', 'subjects within sequences', 'period' and 'treatment'. The effect 'subjects within sequences' was considered as random, whereas the other effects were considered as fixed. Standard error is actually geometric standard error.

Secondary outcomes

  1. Part 1: Maximum Measured Concentration of BI 1358894 in Plasma After i.v. Administration and After Oral Administration (Cmax)

    Time frame: Within 2 hours before and at 15 minutes (min), 30 min, 1 hour (h), 1.5, 2, 3, 4, 5, 5.083, 5.16, 5.25, 5.5, 5.75, 6, 6.5, 7,8, 10, 12, 24, 34, 48, 72, 96, 144, 192, 240, 312 h after oral dose of BI 1358894 on Day 1 of Period 1. Continues in description.

    Maximum measured concentration of BI 1358894 in plasma after i.v. administration and after oral administration(Cmax) is reported.

    Time Frame: For "BI 1358894 (C-14) 100 ug i.v" samples were collected at 5h, 5.083, 5.16, 5.25, 5.5, 5.75, 6, 6.5, 7,8, 10, 12, 24, 34, 48, 72, 96, 144, 192, 240, 312 h after oral dose of BI 1358894 on Day 1 of Period 1.

  2. Part 2: Maximum Measured Concentration of BI 1358894 in Plasma After Administration of the Oral Suspension (Cmax)

    Time frame: Within 2 hours (h) before drug administration and at 15 minutes (min), 30 min, 1 h, 1.5, 2, 3, 4, 5, 6, 7,8, 10, 12, 24, 34, 48, 72, 96, 144, 192, 240, 312 h after administration of BI 1358894.

    Maximum measured concentration of BI 1358894 in plasma after administration of the oral suspension (Cmax) is reported. The Analysis of variance (ANOVA) model included effects accounting for the following sources of variation: 'sequence or block', 'subjects within sequences', 'period' and 'treatment'. The effect 'subjects within sequences' was considered as random, whereas the other effects were considered as fixed. Standard error is actually geometric standard error.

  3. Part 2: Area Under the Concentration-time Curve of BI 1358894 in Plasma Over the Time Interval From 0 Extrapolated to Infinity After Administration of the Oral Suspension (AUC0-infinity)

    Time frame: Within 2 hours (h) before drug administration and at 15 minutes (min), 30 min, 1 h, 1.5, 2, 3, 4, 5, 6, 7,8, 10, 12, 24, 34, 48, 72, 96, 144, 192, 240, 312 h after administration of BI 1358894.

    Area under the concentration-time curve of BI 1358894 in plasma over the time interval from 0 extrapolated to infinity after administration of the oral suspension (AUC0-infinity) is reported. The Analysis of variance (ANOVA) model included effects accounting for the following sources of variation: 'sequence or block', 'subjects within sequences', 'period' and 'treatment'. The effect 'subjects within sequences' was considered as random, whereas the other effects were considered as fixed. Standard error is actually geometric standard error.

Sponsors and collaborators

Lead sponsor

Boehringer Ingelheim

Industry

Registry information

Official study title

Investigation of Pharmacokinetics and Absolute Bioavailability of BI 1358894 Administered Orally as Tablet Co-administered With an Intravenous Microtracer Dose of [C-14]-BI 1358894 in Healthy Male Volunteers Via a Non-randomised, Open-label, Fixed-sequence Trial (Part 1) Followed by a Randomised, Open-label, Single-dose, Two-period, Two-sequence Cross-over Relative Bioavailability Trial in BI 1358894 Oral Suspension (Part 2)

Important dates

Study start
2020
Primary completion
2020
Study completion
2020
First posted
Jun 11, 2020
Registry last updated
Mar 30, 2025

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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