Phase 1
N=12
Effect of a Proton Pump Inhibitor on the PK of Tepotinib
Healthy
Bottom Line
View on ClinicalTrials.gov: NCT03531762 ↗Enrolled (actual)
12
Serious AEs
0.0%
Results posted
Jul 2023
Primary outcome: Primary: Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC0-t) of Tepotinib in Treatment A and Treatment C — 21722; 23649 Hour*nanogram per milliliter (h*ng/mL)
Study Design & Population
- Study type
- Interventional
- Phase
- Phase 1
- Interventions
- Tepotinib (Drug); Omeprazole (Drug)
- Age
- Adult · 18+ yrs
- Sex
- All
- Sponsor
- Merck KGaA, Darmstadt, Germany
- Primary completion
- Jul 2018
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC0-t) of Tepotinib in Treatment A and Treatment C |
21722; 23649 | — |
| PRIMARY Area Under the Plasma Concentration-Time Curve From Time Zero to Infinity (AUC0-inf) of Tepotinib in Treatment A and Treatment C |
23081; 25343 | — |
| PRIMARY Maximum Observed Plasma Concentration (Cmax) of Tepotinib in Treatment A and Treatment C |
428; 445 | — |
| SECONDARY Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC0-t) of Tepotinib in Treatment B |
16220 | — |
| SECONDARY Area Under the Plasma Concentration-Time Curve From Time Zero to Infinity (AUC0-inf) of Tepotinib in Treatment B |
17412 | — |
| SECONDARY Maximum Observed Plasma Concentration (Cmax) of Tepotinib in Treatment B |
227 | — |
| SECONDARY Time to Reach Maximum Plasma Concentration (Tmax) of Tepotinib in Treatments A, B and C |
8.0; 12.0; 8.0 | — |
| SECONDARY Apparent Terminal Half-life (t1/2) of Tepotinib in Treatments A, B and C |
32.9; 30.7; 31.7 | — |
| SECONDARY Time Prior to the First Measurable (Non-zero) Concentration (Tlag) of Tepotinib in Treatments A, B and C |
— | — |
| SECONDARY Apparent Total Body Clearance (CL/f) of Tepotinib in Treatments A, B and C |
19.5; 25.8; 17.8 | — |
| SECONDARY Apparent Volume of Distribution During Terminal Phase (Vz/f) of Tepotinib in Treatments A, B and C |
912; 1181; 860 | — |
| SECONDARY Number of Participants With Treatment-emergent Adverse Events (TEAEs) |
1; 3; 1 | — |
| SECONDARY Number of Participants With Clinically Significant Changes in Laboratory Parameters, 12-lead Electrocardiogram (ECG) Findings and Vital Signs |
0; 0; 0; 0; 0; 0 | — |
Summary
This study was investigated in healthy participants (i) the effect of omeprazole (proton pump inhibitor) co-administration on the single dose pharmacokinetics (PK) of tepotinib under fed conditions, and (ii) the effect of food on the single dose PK of tepotinib after co-administration of omeprazole and tepotinib. Furthermore, the study assessed the safety and tolerability of tepotinib alone and upon co-administration of omeprazole.
Eligibility Criteria
Inclusion Criteria
- Healthy participants of non-child bearing potential
- Body mass index (BMI) between 18.5 and 29.9 kilogram per meter square (kg/m^2)
- Body weight between 50 to 100 kilogram (kg)
- Other protocol defined inclusion criteria could apply
Exclusion Criteria
- Participation in a clinical study within 60 days prior to first drug administration
- Whole blood donation or loss of greater than (>) 450 milliliter (mL) within 60 days prior to first drug administration
- Any surgical or medical condition, or any other significant disease that could interfere with the study objectives, conduct, or evaluation
- Other protocol defined exclusion criteria could apply
Data sourced from ClinicalTrials.gov (NCT03531762). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication.