A Study in Healthy Men to Test if Taking Different Formulations of BI 1358894 With or Without Food Influences the Amount of BI 1358894 in the Blood

NCT03892616 | Completed Phase 1 Results

• 2 other identifiers: 1402-00102018-003603-19
• Study Type: interventional
• Target: 24
• Locations: 1 country
• Sites: 1

Brief Summary

The main objective of this trial is to investigate the relative bioavailability of a single dose of BI 1358894 administered as tablet formulation 2 (TF2a, TF2b) under fasted conditions compared with the tablet formulation 1 (TF1) of BI 1358894 under fed conditions following oral administration and to investigate the effect of food on the exposure with TF2 (TF2a, TF2b).

Conditions

Healthy

Outcome Measures

Primary Outcomes (2)

• Maximum Measured Concentration of BI 1358894 in Plasma (Cmax)

  Maximum measured concentration of BI 1358894 in plasma (Cmax).

  Within 2 hours (h) before and at 10 minutes (min), 20min, 30min, 1h, 1h30min, 2h, 3h, 4h, 5h, 6h, 7h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, 96h, 144h, 192h, 240h, 312h after drug administration in each treatment period.

• Area Under the Concentration-time Curve of BI 1358894 in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz)

  Area under the concentration-time curve of BI 1358894 in plasma over the time interval from 0 to the last quantifiable data point (AUC0-tz).

  Within 2 hours (h) before and at 10 minutes (min), 20min, 30min, 1h, 1h30min, 2h, 3h, 4h, 5h, 6h, 7h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, 96h, 144h, 192h, 240h, 312h after drug administration in each treatment period.

Secondary Outcomes (2)

• Area Under the Concentration-time Curve of BI 1358894 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞)

  Within 2 hours (h) before and at 10 minutes (min), 20min, 30min, 1h, 1h30min, 2h, 3h, 4h, 5h, 6h, 7h, 8h, 10h, 12h, 24h, 34h, 48h, 72h, 96h, 144h, 192h, 240h, 312h after drug administration in each treatment period.

• Area Under the Concentration-time Curve of BI 1358894 in Plasma Over the Time Interval From 0 to 72 Hours (AUC0-72)

  Within 2 hours (h) before and at 10 minutes (min), 20min, 30min, 1h, 1h30min, 2h, 3h, 4h, 5h, 6h, 7h, 8h, 10h, 12h, 24h, 34h, 48h, 72h after drug administration in each treatment period.

Study Arms (12)

TF1 fed (A)-TF2a fed (B)-TF2a fasted (C)

EXPERIMENTAL

1 tablet of 100 milligram (mg) BI 1358894 was administrated as a single oral dose with 240 milliliter (mL) water 30 minutes (min) after a high-fat, high-calorie breakfast as treatment A (TF1; fed conditions) followed by a washout period of at least 17 days, followed by 2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water 30 min after a high-fat, high-calorie breakfast (TF2a fed conditions) as treatment B followed by at least 17 days of washout, followed by 2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water after an overnight fast of at least 10 hours (h) (TF2a fasted conditions) as treatment C.

Drug: BI 1358894 (B); Drug: BI 1358894 (C); Drug: BI 1358894 (A)

TF2b fed (D)-TF1 fed (A)-TF2a fed (B)

EXPERIMENTAL

2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water 30 min after a high-fat, high-calorie breakfast (TF2b; fed conditions) as treatment D followed by at least 17 days of washout, followed by 1 tablet of 100 mg BI 1358894 was administrated as a single oral dose with 240mL water 30 min after a high-fat, high-calorie breakfast (TF1; fed conditions) as treatment A followed by at least 17 days of washout, followed by 2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water 30 min after a high-fat, high-calorie breakfast (TF2a; fed conditions) as treatment B.

Drug: BI 1358894 (B); Drug: BI 1358894 (D); Drug: BI 1358894 (A)

TF2b fasted (E)-TF2a fed (B)-TF1 fed (A)

EXPERIMENTAL

2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water after an overnight fast of at least 10 h (TF2b; fasted conditions) as treatment E followed by washout period of at least 17 days, followed by 2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water 30 min after a high-fat, high-calorie breakfast (TF2a; fed conditions) as treatment B followed by at least 17 days of washout, followed by 1 tablet of 100 mg BI 1358894 was administrated as a single oral dose with 240mL water 30 min after a high-fat, high-calorie breakfast (TF1; fed conditions) as treatment A.

Drug: BI 1358894 (B); Drug: BI 1358894 (E); Drug: BI 1358894 (A)

TF2a fasted (C)- TF1 fed (A)-TF2b fed (D)

EXPERIMENTAL

2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water after an overnight fast of at least 10 h (TF2a; fasted conditions) as treatment C followed by washout period of at least 17 days, followed by 1 tablet of 100 mg BI 1358894 was administrated as a single oral dose with 240mL water 30 min after a high-fat, high-calorie breakfast (TF1; fed conditions) as treatment A followed by at least 17 days of washout, followed by 2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water 30 min after a high-fat, high-calorie breakfast (TF2b; fed conditions) as treatment D.

Drug: BI 1358894 (C); Drug: BI 1358894 (D); Drug: BI 1358894 (A)

TF1 fed (A)- TF2b fasted (E)- TF2a fasted (C)

EXPERIMENTAL

1 tablet of 100 mg BI 1358894 was administrated as a single oral dose with 240mL water 30 min after a high-fat, high-calorie breakfast (TF1; fed conditions) as treatment A followed by at least 17 days of washout, followed by 2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water after an overnight fast of at least 10 h (TF2b; fasted conditions) as treatment E followed by at least 17 days of washout, followed by 2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water after an overnight fast of at least 10 h (TF2a; fasted conditions) as treatment C.

Drug: BI 1358894 (C); Drug: BI 1358894 (E); Drug: BI 1358894 (A)

TF2b fasted (E)-TF2b fed (D)- TF1 fed (A)

EXPERIMENTAL

2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water after an overnight fast of at least 10 h (TF2b; fasted conditions) as treatment E followed by at least 17 days of washout, followed by 2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water 30 min after a high-fat, high-calorie breakfast (TF2b; fed conditions) as treatment D followed by at least 17 days of washout, followed by 1 tablet of 100 mg BI 1358894 was administrated as a single oral dose with 240mL water 30 min after a high-fat, high-calorie breakfast (TF1; fed conditions) as treatment A.

Drug: BI 1358894 (D); Drug: BI 1358894 (E); Drug: BI 1358894 (A)

TF2a fed (B)- TF2a fasted (C)-TF2b fed (D)

EXPERIMENTAL

2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water 30 min after a high-fat, high-calorie breakfast (TF2a; fed conditions) as treatment B followed by at least 17 days of washout, followed by 2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water after an overnight fast of at least 10 h (TF2a; fasted conditions) as treatment C followed by at least 17 days of washout, followed by 2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water 30 min after a high-fat, high-calorie breakfast (TF2b; fed conditions) as treatment D.

Drug: BI 1358894 (B); Drug: BI 1358894 (C); Drug: BI 1358894 (D)

TF2a fasted(C)-TF2b fasted(E)-TF2a fed(B)

EXPERIMENTAL

2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water after an overnight fast of at least 10 h (TF2a; fasted conditions) as treatment C followed by at least 17 days of washout, followed by 2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water after an overnight fast of at least 10 h (TF2b; fasted conditions) as treatment E followed by at least 17 days of washout, followed by 2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water 30 min after a high-fat, high-calorie breakfast (TF2a; fed conditions) as treatment B.

Drug: BI 1358894 (B); Drug: BI 1358894 (C); Drug: BI 1358894 (E)

TF2a fed(B)-TF2b fed(D)-TF2b fasted(E)

EXPERIMENTAL

2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water 30 min after a high-fat, high-calorie breakfast (TF2a; fed conditions) as treatment B followed by at least 17 days of washout, followed by 2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water 30 min after a high-fat, high-calorie breakfast (TF2b; fed conditions) as treatment D followed by at least 17 days of washout, followed by 2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water after an overnight fast of at least 10 h (TF2b; fasted conditions) as treatment E.

Drug: BI 1358894 (B); Drug: BI 1358894 (D); Drug: BI 1358894 (E)

TF2b fed(D)-TF2a fasted(C)-TF2b fasted(E)

EXPERIMENTAL

2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water 30 min after a high-fat, high-calorie breakfast (TF2b; fed conditions) as treatment D followed by at least 17 days of washout, followed by 2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water after an overnight fast of at least 10 h (TF2a; fasted conditions) as treatment C followed by at least 17 days of washout, followed by 2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water after an overnight fast of at least 10 h (TF2b; fasted conditions) as treatment E.

Drug: BI 1358894 (C); Drug: BI 1358894 (D); Drug: BI 1358894 (E)

TF2a fasted(C)-TF2a fed(B)-TF1 fed(A)

EXPERIMENTAL

2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water after an overnight fast of at least 10 h (TF2a; fasted conditions) as treatment C followed by at least 17 days of washout, followed by 2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water 30 min after a high-fat, high-calorie breakfast (TF2a; fed conditions) as treatment B followed by at least 17 days of washout, followed by 1 tablet of 100 mg BI 1358894 was administrated as a single oral dose with 240mL water 30 min after a high-fat, high-calorie breakfast (TF1; fed conditions) as treatment A.

Drug: BI 1358894 (B); Drug: BI 1358894 (C); Drug: BI 1358894 (A)

TF1 fed (A)- TF2b fasted (E)-TF2b fed (D)

EXPERIMENTAL

1 tablet of 100 mg BI 1358894 was administrated as a single oral dose with 240mL water 30 min after a high-fat, high-calorie breakfast (TF1; fed conditions) as treatment A followed by at least 17 days of washout, followed by 2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water after an overnight fast of at least 10 h (TF2b; fasted conditions) as treatment E followed by at least 17 days of washout, followed by 2 tablets of 50mg BI 1358894 (total: 100mg) administrated as a single oral dose with 240 mL water 30 min after a high-fat, high-calorie breakfast (TF2b; fed conditions) as treatment D.

Drug: BI 1358894 (D); Drug: BI 1358894 (E); Drug: BI 1358894 (A)

Interventions

BI 1358894 (B) DRUG

Tablet formulation 2 (TF2a), fed

TF1 fed (A)-TF2a fed (B)-TF2a fasted (C); TF2a fasted(C)-TF2a fed(B)-TF1 fed(A); TF2a fasted(C)-TF2b fasted(E)-TF2a fed(B); TF2a fed (B)- TF2a fasted (C)-TF2b fed (D); TF2a fed(B)-TF2b fed(D)-TF2b fasted(E); TF2b fasted (E)-TF2a fed (B)-TF1 fed (A); TF2b fed (D)-TF1 fed (A)-TF2a fed (B)

BI 1358894 (C) DRUG

Tablet formulation 2 (TF2a), fasted

TF1 fed (A)- TF2b fasted (E)- TF2a fasted (C); TF1 fed (A)-TF2a fed (B)-TF2a fasted (C); TF2a fasted (C)- TF1 fed (A)-TF2b fed (D); TF2a fasted(C)-TF2a fed(B)-TF1 fed(A); TF2a fasted(C)-TF2b fasted(E)-TF2a fed(B); TF2a fed (B)- TF2a fasted (C)-TF2b fed (D); TF2b fed(D)-TF2a fasted(C)-TF2b fasted(E)

BI 1358894 (D) DRUG

Tablet formulation 2 (TF2b), fed

TF1 fed (A)- TF2b fasted (E)-TF2b fed (D); TF2a fasted (C)- TF1 fed (A)-TF2b fed (D); TF2a fed (B)- TF2a fasted (C)-TF2b fed (D); TF2a fed(B)-TF2b fed(D)-TF2b fasted(E); TF2b fasted (E)-TF2b fed (D)- TF1 fed (A); TF2b fed (D)-TF1 fed (A)-TF2a fed (B); TF2b fed(D)-TF2a fasted(C)-TF2b fasted(E)

BI 1358894 (E) DRUG

Tablet formulation 2 (TF2b), fasted

TF1 fed (A)- TF2b fasted (E)- TF2a fasted (C); TF1 fed (A)- TF2b fasted (E)-TF2b fed (D); TF2a fasted(C)-TF2b fasted(E)-TF2a fed(B); TF2a fed(B)-TF2b fed(D)-TF2b fasted(E); TF2b fasted (E)-TF2a fed (B)-TF1 fed (A); TF2b fasted (E)-TF2b fed (D)- TF1 fed (A); TF2b fed(D)-TF2a fasted(C)-TF2b fasted(E)

BI 1358894 (A) DRUG

Tablet formulation 1 (TF1), fed

TF1 fed (A)- TF2b fasted (E)- TF2a fasted (C); TF1 fed (A)- TF2b fasted (E)-TF2b fed (D); TF1 fed (A)-TF2a fed (B)-TF2a fasted (C); TF2a fasted (C)- TF1 fed (A)-TF2b fed (D); TF2a fasted(C)-TF2a fed(B)-TF1 fed(A); TF2b fasted (E)-TF2a fed (B)-TF1 fed (A); TF2b fasted (E)-TF2b fed (D)- TF1 fed (A); TF2b fed (D)-TF1 fed (A)-TF2a fed (B)

Eligibility Criteria

• Age: 18 Years - 50 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy male subjects according to the assessment of the investigator, as 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 (inclusive)
• Body mass index (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 Good Clinical Practice (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 30 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 (IUD) that started at least 2 months prior to first study drug administration, or barrier method (e.g. diaphragm with spermicide)
• Sexually abstinent
• A vasectomy performed at least 1 year prior to screening (with medical assessment of the surgical success)
• Surgically sterilised female partner (including hysterectomy, bilateral tubal occlusion or bilateral oophorectomy)

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 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 50 to 90 bpm
• C-Reactive Protein (CRP) \> upper limit of normal (ULN), erythrocyte sedimentation rate (ESR) ≥15 millimeters/h, liver or kidney parameter above ULN, or any other 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 and 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
• History of relevant orthostatic hypotension, fainting spells, or blackouts
• Chronic or relevant acute infections
• History of relevant allergy or hypersensitivity (including allergy to the trial medication or its excipients)
• Use of drugs within 30 days of planned administration of trial medication that might reasonably influence the results of the trial (including drugs that cause QT/QTc interval prolongation)
• Intake of an investigational drug in another clinical trial within 60 days of planned administration of investigational drug in the current trial, or concurrent participation in another clinical trial in which investigational drug is administered
• Smoker (more than 10 cigarettes or 3 cigars or 3 pipes per day)
• Inability to refrain from smoking on specified trial days
• Alcohol abuse (consumption of more than 30 g per day)

Sponsors & Collaborators

• Boehringer Ingelheim: lead

Study Sites (1)

CRS Clinical Research Services Mannheim GmbH

Mannheim, 68167, Germany

Location

Related Links

• Related Info

MeSH Terms

Interventions

TRPC inhibitor BI 1358894; Fumigant 93

Results Point of Contact

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

clintriage.rdg@boehringer-ingelheim.com

1-800-243-0127

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
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: March 26, 2019
• First Posted: March 27, 2019
• Study Start: April 8, 2019
• Primary Completion: July 3, 2019
• Study Completion: July 3, 2019
• Last Updated: February 28, 2025
• Results First Posted: February 28, 2025

Record last verified: 2025-02

Data Sharing

• IPD Sharing: Will not share

Locations

DE (1)