Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Tepotinib TF2 · 1 trial · 1 indication
Area under the plasma concentration versus time curve from time zero to the last sampling time t at which the concentration was at or above the lower limit of quantification (LLOQ). AUC0-t was to be calculated according to the mixed log-linear trapezoidal rule.
AUC0-inf was calculated by combining AUC0-t and AUCextra. AUC extra represents an extrapolated value obtained by Clast/ lambda z, where Clast is the calculated plasma concentration at the last sampling time point at which the measured plasma concentration is at or above the Lower Limit of quantification (LLOQ) and lambda z is the apparent terminal rate constant determined by log-linear regression analysis of the measured plasma concentrations of the terminal log-linear phase.
Cmax was obtained directly from the concentration versus time curve.
| Arm | Type | Description |
|---|---|---|
| Part A: First Tepotinib TF2 then TF3 | EXPERIMENTAL | Participants received a single oral dose of 500 milligrams (mg) Tepotinib tablet formulation 2 (TF2, reference treatment) on Day 1 of treatment period 1 followed by a single oral dose of 500 mg (2 x 250 mg) Tepotinib tablet formulation 3 (TF3, test treatment) on Day 1 of treatment period 2 under fasting conditions. The washout period was 21 days between Day 1 of each period. |
| Part A: First Tepotinib TF3 then TF2 | EXPERIMENTAL | Participants received a single oral dose of 500 mg (2 x 250 mg) Tepotinib TF3 (test treatment) on Day 1 of treatment period 1 followed by a single oral dose of 500 mg Tepotinib TF2 (reference treatment) on Day 1 of treatment period 2 under fasting conditions. The washout period was 21 days between Day 1 of each period. |
| Part B: First Tepotinib TF2 Fasted then TF2 Fed | EXPERIMENTAL | Participants received a single oral dose of 500 mg Tepotinib TF2 (reference treatment) on Day 1 of treatment period 1 under fasting conditions followed by a single oral dose of 500 mg Tepotinib TF2 (reference treatment) on Day 1 of treatment period 2 under fed conditions. The washout period was 21 days between Day 1 of each period. |
| Part B: First Tepotinib TF2 Fed then TF2 Fasted | EXPERIMENTAL | Participants received a single oral dose of 500 mg Tepotinib TF2 (reference treatment) on Day 1 of treatment period 1 under fed conditions followed by a single oral dose of 500 mg Tepotinib TF2 (reference treatment) on Day 1 of treatment period 2 under fasting conditions. The washout period was 21 days between Day 1 of each period. |
| Part C: First Tepotinib TF3 Fasted then TF3 Fed | EXPERIMENTAL | Participants received a single oral dose of 500 mg (2 x 250 mg) Tepotinib TF3 (test treatment) on Day 1 of treatment period 1 under fasting conditions followed by a single oral dose of 500 mg (2 x 250 mg) Tepotinib TF3 (test treatment) on Day 1 of treatment period 2 under fed conditions. The washout period was 21 days between Day 1 of each period. |
| Part C: First Tepotinib TF3 Fed then TF3 Fasted | EXPERIMENTAL | Participants received a single oral dose of 500 mg (2 x 250 mg) Tepotinib TF3 (test treatment) on Day 1 of treatment period 1 under fed conditions followed by a single oral dose of 500 mg (2 x 250 mg) Tepotinib TF3 (test treatment) on Day 1 of treatment period 2 under fasting conditions. The washout period was 21 days between Day 1 of each period. |
| Name | Type | Description |
|---|---|---|
| Tepotinib TF2 | DRUG | Participants received a single oral dose of 500 mg Tepotinib TF2 under fasting or fed conditions in treatment period 1 or 2. |
| Tepotinib TF3 | DRUG | Participants received single oral dose of 500 mg (2 x 250 mg)Tepotinib TF3 under fasting or fed conditions in treatment period 1 or 2. |
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 ...
Tepotinib TF2 is an investigational small molecule developed by Merck KGaA. It is a MET inhibitor that has been studied in a Phase 1 clinical trial in healthy volunteers. The trial evaluated the bioequivalence of TF3 and TF2 and the effect of food on the pharmacokinetics of tepotinib.
Tepotinib TF2 targets MET, a receptor tyrosine kinase. It acts as an inhibitor of MET. By inhibiting MET, tepotinib TF2 may interfere with signaling pathways involved in cell growth and survival. The drug is a small molecule designed for oral administration.
Tepotinib TF2 is being developed by Merck KGaA, a German pharmaceutical company. Merck KGaA trades on the OTC market under the ticker MKGAF. The company is responsible for the clinical development of tepotinib TF2.
Tepotinib TF2 is in Phase 1 clinical development. It has completed one Phase 1 trial. The drug is investigational and has not been approved by the FDA for any indication.
Tepotinib TF2 has been studied in one completed Phase 1 trial, NCT03629223, titled "Bioequivalence of TF3 and TF2 and Effect of Food on the PK of Tepotinib." The trial enrolled 66 healthy volunteers in Germany and was a controlled, randomized study.