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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

Completed Phase 1 Results posted Last updated 30 March 2025
What this trial tests

Phase 1 trial testing BI 1358894 in Healthy in 12 participants. Completed in 12 October 2020.

Timeline
13 July 2020
Primary endpoint
12 October 2020
12 October 2020

Quick facts

Lead sponsorBoehringer Ingelheim
PhasePhase 1
StatusCompleted
Study typeINTERVENTIONAL
Allocationrandomized
Designcrossover
Maskingnone
Primary purposetreatment
Enrollment12
Start date13 July 2020
Primary completion12 October 2020
Estimated completion12 October 2020
Sites1 location across Netherlands

Drugs / interventions tested

Conditions studied

Sponsor

Boehringer Ingelheim — full company profile →

Who can join

Adults 18 to 55, male only, with Healthy. Patients with the condition only — healthy volunteers not accepted.

Results — posted to ClinicalTrials.gov

Per-arm endpoint measurements with 95% confidence intervals where reported. Source: trial results section.

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) Primary · 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

GroupValue95% CI
BI 1358894 100 mg Tablet Fasted96± NA
BI 1358894 (C-14) 100 ug i.v209± NA
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) Primary · 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.

GroupValue95% CI
BI 1358894 100 mg Oral Suspension Fasted12217± NA
BI 1358894 100 mg Oral Suspension Fed17271± NA
Part 1: Maximum Measured Concentration of BI 1358894 in Plasma After i.v. Administration and After Oral Administration (Cmax) Secondary · 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.

GroupValue95% CI
BI 1358894 100 mg Tablet Fasted408± 34.1
BI 1358894 (C-14) 100 ug i.v0.847± 28.8
Part 2: Maximum Measured Concentration of BI 1358894 in Plasma After Administration of the Oral Suspension (Cmax) Secondary · 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.

GroupValue95% CI
BI 1358894 100 mg Oral Suspension Fasted810± NA
BI 1358894 100 mg Oral Suspension Fed529± NA
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) Secondary · 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.

GroupValue95% CI
BI 1358894 100 mg Oral Suspension Fasted13510± NA
BI 1358894 100 mg Oral Suspension Fed20052± NA

Adverse events — posted to ClinicalTrials.gov

Time frame: BI tablet = From treatment start until start of C14, up to 1 day. BI fed, BI fasted and BI C14 = day of treatment + 11 days Residual Effect Period (REP), up to 12 days.. Reporting threshold: 5%. Adverse-event reports describe events observed during the trial — not all are caused by the drug.

BI 1358894 100 mg Tablet Fasted
Serious: 0/12 (0%)
Deaths: 0/12
BI 1358894 (C-14) 100 ug i.v
Serious: 0/12 (0%)
Deaths: 0/12
BI 1358894 100 mg Oral Suspension Fasted
Serious: 0/11 (0%)
Deaths: 0/11
BI 1358894 100 mg Oral Suspension Fed
Serious: 0/11 (0%)
Deaths: 0/11
Other adverse events (23 terms — click to expand)

ReactionSystemBI 1358894 100 mg Tablet F…BI 1358894 (C-14) 100 ug i.vBI 1358894 100 mg Oral Sus…BI 1358894 100 mg Oral Sus…
HeadacheNervous system disorders
SomnolenceNervous system disorders
DizzinessNervous system disorders
ErythemaSkin and subcutaneous tissue disorders
Disturbance in attentionNervous system disorders
DysgeusiaNervous system disorders
DiarrhoeaGastrointestinal disorders
ConstipationGastrointestinal disorders
Haemorrhoidal haemorrhageGastrointestinal disorders
NauseaGastrointestinal disorders
FatigueGeneral disorders
Catheter site haematomaGeneral disorders
ThirstGeneral disorders
Skin exfoliationSkin and subcutaneous tissue disorders
PapuleSkin and subcutaneous tissue disorders
ArthralgiaMusculoskeletal and connective tissue disorders
Back painMusculoskeletal and connective tissue disorders
Neck painMusculoskeletal and connective tissue disorders
Vision blurredEye disorders
Visual acuity reducedEye disorders
StressPsychiatric disorders
Oropharyngeal painRespiratory, thoracic and mediastinal disorders
Fungal skin infectionInfections and infestations

Data from ClinicalTrials.gov NCT04426851 adverse events section.

Sponsor's own description

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.

Publications & conference data

No peer-reviewed publications indexed yet for this trial. Completed trials usually publish results within 12-18 months.

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Primary sources · FDA · ClinicalTrials.gov · EMA · SEC EDGAR · ChEMBL · Wikidata · full sourcing