Phase 1
N=66
Bioequivalence of TF3 and TF2 and Effect of Food on the PK of Tepotinib
Healthy
Bottom Line
View on ClinicalTrials.gov: NCT03629223 ↗Enrolled (actual)
66
Serious AEs
0.8%
Results posted
Oct 2023
Primary outcome: Primary: Part A, B and C: Area Under the Plasma Concentration-Time Curve From Time Zero to the Last Quantifiable Concentration (AUC 0-t) of Tepotinib — 16146; 18645; 12609; 23457 nanograms*hour per milliliter (ng*h/mL)
Study Design & Population
- Study type
- Interventional
- Phase
- Phase 1
- Interventions
- Tepotinib TF2 (Drug); Tepotinib TF3 (Drug)
- Age
- Adult · 18+ yrs
- Sex
- All
- Sponsor
- Merck KGaA, Darmstadt, Germany
- Primary completion
- Jan 2019
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Part A, B and C: Area Under the Plasma Concentration-Time Curve From Time Zero to the Last Quantifiable Concentration (AUC 0-t) of Tepotinib |
16146; 18645; 12609; 23457; 17964; 29307 | — |
| PRIMARY Part A, B and C: Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinity (AUC 0-inf) of Tepotinib |
16728; 19316; 13037; 24443; 18447; 30118 | — |
| PRIMARY Part A, B and C: Maximum Observed Plasma Concentration (Cmax) of Tepotinib |
253; 288; 199; 476; 280; 559 | — |
| SECONDARY Part A, B and C: Time to Reach the Maximum Plasma Concentration (Tmax) of Tepotinib |
14.1; 12.0; 24.0; 12.0; 12.0; 8.0 | — |
| SECONDARY Part A, B and C: Terminal Half-Life (t1/2) of Tepotinib |
31.8; 30.9; 30.8; 30.0; 29.2; 29.9 | — |
| SECONDARY Part A, B and C: Apparent Total Body Clearance of Tepotinib From Plasma Following Oral Administration (CL/f) |
26.9; 23.3; 34.5; 18.4; 24.4; 14.9 | — |
| SECONDARY Part A, B and C: Apparent Volume of Distribution of Tepotinib During the Terminal Phase Following Extravascular Administration (Vz/f) |
1232; 1038; 1531; 797; 1027; 644 | — |
| SECONDARY Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious TEAEs |
18; 14; 5; 9; 6; 6 | — |
| SECONDARY Number of Participants With Clinically Significant Abnormalities in Laboratory Values |
0; 0; 0; 0; 0; 0 | — |
| SECONDARY Number of Participants With Clinically Significant Abnormalities in 12-lead Electrocardiogram (ECG) Findings |
0; 0; 0; 0; 0; 0 | — |
| SECONDARY Number of Participants With Clinically Significant Abnormalities in Vital Signs |
0; 0; 0; 0; 0; 0 | — |
Summary
The main purpose of the study was to demonstrate bioequivalence between the new tablet formulation (TF3, test treatment) and the tablet formulation used in clinical studies (TF2, reference treatment) and to investigate effect of food on pharmacokinetics (PK) of tepotinib.
Eligibility Criteria
Inclusion Criteria
- Healthy participants of non-child bearing potential
- Body weight between 50 to 100 kilogram (kg)
- Body mass index (BMI) between 18.5 and 29.9 kilogram per meter square (kg/m^2)
- 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 (NCT03629223). 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.