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Tepotinib TF2

Phase 1

Healthy | Small molecule | Other |Merck KGaA|Last Updated: Oct 10, 2023

Success Probability

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Market & Valuation

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Trial Design

RandomizedCONTROLLED
Total Trials1
Total Enrollment66

FDA Designations

No designations recorded

Clinical trial landscape

Tepotinib TF2 · 1 trial · 1 indication

Phase 1 1
NCT03629223Bioequivalence of TF3 and TF2 and Effect of Food on the PK of TepotinibHealthy
COMPLETED66 Analytics
PHASE1COMPLETED
Bioequivalence of TF3 and TF2 and Effect of Food on the PK of Tepotinib
HealthyUnlock trial analytics

Study Endpoints

Primary Endpoints

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
Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 60, 72, 96, 120, 144 and 168 hours post-dose on Day 1 of each treatment period

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.

Part A, B and C: Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinity (AUC 0-inf) of Tepotinib
Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 60, 72, 96, 120, 144 and 168 hours post-dose on Day 1 of each treatment period

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.

Part A, B and C: Maximum Observed Plasma Concentration (Cmax) of Tepotinib
Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 60, 72, 96, 120, 144 and 168 hours post-dose on Day 1 of each treatment period

Cmax was obtained directly from the concentration versus time curve.

Secondary Endpoints

Part A, B and C: Time to Reach the Maximum Plasma Concentration (Tmax) of Tepotinib
Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 60, 72, 96, 120, 144 and 168 hours post-dose on Day 1 of each treatment period
Part A, B and C: Terminal Half-Life (t1/2) of Tepotinib
Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 60, 72, 96, 120, 144 and 168 hours post-dose on Day 1 of each treatment period
Part A, B and C: Apparent Total Body Clearance of Tepotinib From Plasma Following Oral Administration (CL/f)
Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 60, 72, 96, 120, 144 and 168 hours post-dose on Day 1 of each treatment period
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelCROSSOVER
PurposeOTHER

Treatment Arms

ArmTypeDescription
Part A: First Tepotinib TF2 then TF3EXPERIMENTALParticipants 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 TF2EXPERIMENTALParticipants 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 FedEXPERIMENTALParticipants 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 FastedEXPERIMENTALParticipants 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 FedEXPERIMENTALParticipants 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 FastedEXPERIMENTALParticipants 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.

Interventions

NameTypeDescription
Tepotinib TF2DRUGParticipants received a single oral dose of 500 mg Tepotinib TF2 under fasting or fed conditions in treatment period 1 or 2.
Tepotinib TF3DRUGParticipants received single oral dose of 500 mg (2 x 250 mg)Tepotinib TF3 under fasting or fed conditions in treatment period 1 or 2.
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Eligibility Criteria

Age Range18 Years to 55 Years
SexALL
Healthy VolunteersYes
Study Sites1

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 ...

Countries:Germany
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Frequently asked questions about Tepotinib TF2

What is Tepotinib TF2 used for?

Tepotinib TF2 is an investigational small molecule being studied in healthy volunteers. It is being evaluated in a Phase 1 clinical trial to assess bioequivalence and the effect of food on its pharmacokinetics. The drug is not approved for any indication and is still in clinical development.

Who makes Tepotinib TF2?

Tepotinib TF2 is being developed by Merck KGaA, a company traded under the ticker MKGAF. The company is conducting clinical research on this investigational small molecule in healthy volunteers.

What phase is Tepotinib TF2 in?

Tepotinib TF2 is in Phase 1 clinical development. It is an investigational drug, meaning it has not been approved by regulatory authorities. The only trial for this drug has been completed, and it involved healthy volunteers.

What clinical trials is Tepotinib TF2 in?

Tepotinib TF2 is associated with one clinical trial, NCT03629223, titled 'Bioequivalence of TF3 and TF2 and Effect of Food on the PK of Tepotinib.' This Phase 1 study enrolled 66 healthy participants in Germany and has been completed.

Is Tepotinib TF2 the same as TF3?

Tepotinib TF2 and TF3 are distinct formulations being compared in the clinical trial NCT03629223. The study evaluates the bioequivalence of TF3 and TF2, meaning they are separate versions of the drug being tested for similarity in how the body processes them.