A Study in Healthy Men to Test Whether Zongertinib Affects How 3 Other Medicines (Midazolam, Omeprazole, and Repaglinide) Are Taken up and Processed by the Body

NCT06494761 | Completed Phase 1 Results FDA Drug

• 3 other identifiers: 1479-00142023-510263-35-00U1111-1301-9035
• Study Type: interventional
• Target: 16
• Locations: 1 country
• Sites: 1

Brief Summary

The main objective of this trial is to assess the effect of multiple oral doses of zongertinib on the pharmacokinetics of midazolam, omeprazole and repaglinide.

Conditions

Healthy

Outcome Measures

Primary Outcomes (6)

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

  The area under the concentration-time curve of repaglinide in plasma over the time interval from 0 extrapolated to infinity ((AUC0-∞) is reported. Period 1 (Day 1): Up to 3 hours pre-dose and at 15, 30, and 45 minutes, and 1, 1.5, 2, 2.5, 3-, 4-, 6-, and 24-hours post-dose. Period 2 (Day 1): Up to 3 hours pre-dose and at 15, 30, and 45 minutes, and 1, 1.5, 2, 2.5, 3-, 4-, 6-, and 24-hours post-dose. Period 2 (Day 14): ≤15 min pre-dose and at 15, 30, 45 min; 1, 1.5, 2, 2.5, 3-, 4-,6-, and 24-hours post-dose.

  Samples were collected on Day 1 (Period 1), Day 1 (Period 2), and Day 14 (Period 2). See endpoint description for the full sampling schedule

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

  The area under the concentration-time curve of midazolam in plasma over the time interval from 0 extrapolated to infinity ((AUC0-∞) is reported. Period 1 (Day 2): 15 min pre-dose and at 15, 30, 45 min; 1, 1.5, 2, 4, 6, 8, 10, 12 hours post-dose. Period 2 (Day 2): 15 min pre-dose and at 15, 30, 45 min; 1, 1.5, 2, 4, 6, 8, 10, 12 h post-dose. Period 2 (Day 15): 15 min pre-dose, and at 15, 30, 45 min; 1, 1.5, 2, 4, 6, 8, 10, 11, 12 hours post-dose.

  Samples were collected on Day 2 (Period 1), Day 2 (Period 2), and Day 15 (Period 2). See endpoint description for the full sampling schedule

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

  The area under the concentration-time curve of omeprazole in plasma over the time interval from 0 extrapolated to infinity ((AUC0-∞) is reported. Period 1 (Day 2): 15 min pre-dose and at 15, 30, 45 min; 1, 1.5, 2, 4, 6, 8, 10, 12 hours post-dose. Period 2 (Day 2): 15 min pre-dose and at 15, 30, 45 min; 1, 1.5, 2, 4, 6, 8, 10, 12 h post-dose. Period 2 (Day 15): 15 min pre-dose, and at 15, 30, 45 min; 1, 1.5, 2, 4, 6, 8, 10, 11, 12 hours post-dose.

  Samples were collected on Day 2 (Period 1), Day 2 (Period 2), and Day 15 (Period 2). See endpoint description for the full sampling schedule

• Maximum Measured Concentration of Repaglinide in Plasma (Cmax)

  The maximum measured concentration of repaglinide in plasma is reported. Period 1 (Day 1): Up to 3 hours pre-dose and at 15, 30, and 45 minutes, and 1, 1.5, 2, 2.5, 3-, 4-, 6-, and 24-hours post-dose. Period 2 (Day 1): Up to 3 hours pre-dose and at 15, 30, and 45 minutes, and 1, 1.5, 2, 2.5, 3-, 4-, 6-, and 24-hours post-dose. Period 2 (Day 14): ≤15 min pre-dose and at 15, 30, 45 min; 1, 1.5, 2, 2.5, 3-, 4-,6-, and 24-hours post-dose.

  Samples were collected on Day 1 (Period 1), Day 1 (Period 2), and Day 14 (Period 2). See endpoint description for the full sampling schedule

• Maximum Measured Concentration of Midazolam in Plasma (Cmax)

  The maximum measured concentration of midazolam in plasma is reported. Period 1 (Day 2): 15 min pre-dose and at 15, 30, 45 min; 1, 1.5, 2, 4, 6, 8, 10, 12 hours post-dose. Period 2 (Day 2): 15 min pre-dose and at 15, 30, 45 min; 1, 1.5, 2, 4, 6, 8, 10, 12 h post-dose. Period 2 (Day 15): 15 min pre-dose, and at 15, 30, 45 min; 1, 1.5, 2, 4, 6, 8, 10, 11, 12 hours post-dose.

  Samples were collected on Day 2 (Period 1), Day 2 (Period 2), and Day 15 (Period 2). See endpoint description for the full sampling schedule

• Maximum Measured Concentration of Omeprazole in Plasma (Cmax)

  The maximum measured concentration of omeprazole in plasma is reported. Period 1 (Day 2): 15 min pre-dose and at 15, 30, 45 min; 1, 1.5, 2, 4, 6, 8, 10, 12 hours post-dose. Period 2 (Day 2): 15 min pre-dose and at 15, 30, 45 min; 1, 1.5, 2, 4, 6, 8, 10, 12 h post-dose. Period 2 (Day 15): 15 min pre-dose, and at 15, 30, 45 min; 1, 1.5, 2, 4, 6, 8, 10, 11, 12 hours post-dose.

  Samples were collected on Day 2 (Period 1), Day 2 (Period 2), and Day 15 (Period 2). See endpoint description for the full sampling schedule

Secondary Outcomes (3)

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

  Samples were collected on Day 1 (Period 1), Day 1 (Period 2), and Day 14 (Period 2). See endpoint description for the full sampling schedule

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

  Samples were collected on Day 2 (Period 1), Day 2 (Period 2), and Day 15 (Period 2). See endpoint description for the full sampling schedule

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

  Samples were collected on Day 2 (Period 1), Day 2 (Period 2), and Day 15 (Period 2). See endpoint description for the full sampling schedule

Study Arms (1)

Repaglinide+Midazolam+Omeprazole (Reference)/ Zongertinib+Repaglinide+Midazolam+Omeprazole (Test)

EXPERIMENTAL

Reference (Repaglinide + Midazolam + Omeprazole) In the reference treatment period (Period 1), participants received 0.5 mg repaglinide tablet (Day 1, after ≥10 h fast; Reference Treatment 1). On Day 2, they received 1 mg midazolam (0.5 mL oral solution) with 20 mg omeprazole tablet under the same fasting conditions (Reference Treatment 2). Test (Zongertinib + Repaglinide + Midazolam + Omeprazole) In the test treatment period (Period 2), participants received multiple once-daily doses of 120 mg zongertinib from Day 1 to Day 15. A single 0.5 mg repaglinide tablet was co-administered on Day 1 (Test Treatment 1) and Day 14 (Test Treatment 3), and a single dose of the probe drug cocktail containing 1 mg midazolam (0.5 mL oral solution) and 20 mg omeprazole tablet was co-administered on Day 2 (Test Treatment 2) and Day 15 (Test Treatment 4).

Drug: zongertinib; Drug: midazolam; Drug: omeprazole; Drug: repaglinide

Interventions

zongertinib DRUG

Participants received 120 mg Zongertinib daily as two 60 mg tablets.

Also known as: BI 1810631

Repaglinide+Midazolam+Omeprazole (Reference)/ Zongertinib+Repaglinide+Midazolam+Omeprazole (Test)

midazolam DRUG

Participants received 1 mg Midazolam as 0.5 mL oral solution.

Repaglinide+Midazolam+Omeprazole (Reference)/ Zongertinib+Repaglinide+Midazolam+Omeprazole (Test)

omeprazole DRUG

Participants received 20 mg Omeprazole.

Repaglinide+Midazolam+Omeprazole (Reference)/ Zongertinib+Repaglinide+Midazolam+Omeprazole (Test)

repaglinide DRUG

Participants received a 0.5 mg Repaglinide.

Repaglinide+Midazolam+Omeprazole (Reference)/ Zongertinib+Repaglinide+Midazolam+Omeprazole (Test)

Eligibility Criteria

• Age: 18 Years - 55 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 55 years (inclusive)
• Body mass index (BMI) of 18.5 to 29.9 kg/m2 (inclusive)
• Signed and dated written informed consent

You may not qualify if:

• 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 millimetre(s) of mercury (mmHg), diastolic blood pressure outside the range of 50 to 90 mmHg, or pulse rate outside the range of 45 to 90 beats per minute (bpm)
• Any laboratory value outside the reference range that the investigator considers to be of clinical relevance

Sponsors & Collaborators

• Boehringer Ingelheim: lead

Study Sites (1)

Humanpharmakologisches Zentrum Biberach

Biberach, 88397, Germany

Location

Related Links

• Related Info

MeSH Terms

Interventions

Midazolam; Omeprazole; repaglinide

Intervention Hierarchy (Ancestors)

Benzodiazepines; Benzazepines; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring; Heterocyclic Compounds; 2-Pyridinylmethylsulfinylbenzimidazoles; Sulfoxides; Sulfur Compounds; Organic Chemicals; Pyridines; Heterocyclic Compounds, 1-Ring; Benzimidazoles

Results Point of Contact

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

clintriage.rdg@boehringer-ingelheim.com

018002430127

Publication Agreements

• PI is Sponsor Employee: Yes

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: July 3, 2024
• First Posted: July 10, 2024
• Study Start: July 30, 2024
• Primary Completion: October 16, 2024
• Study Completion: October 16, 2024
• Last Updated: December 2, 2025
• Results First Posted: December 2, 2025

Record last verified: 2025-11

Data Sharing

• IPD Sharing: Will not share

Locations

DE (1)