Bioequivalence of TF3 and TF2 and Effect of Food on the PK of Tepotinib

Sponsor
Merck KGaA, Darmstadt, Germany
Study ID
NCT03629223
Phase
PHASE1
Status
Completed

Conditions

  • Healthy

Eligibility Criteria

Sex
ALL
Age
18 Years - 55 Years
Healthy Volunteers
Accepted

Interventions

  • 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.

Study Details

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.

Key Dates

Start date
Aug 23, 2018
Status verified
Oct 2023
Primary completion
Jan 25, 2019
Completion
Jan 25, 2019

Study Design

Enrollment
66 participants (actual)
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
OTHER

Arms

  • Experimental: Part A: First Tepotinib TF2 then TF3
    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.
  • Experimental: Part A: First Tepotinib TF3 then TF2
    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.
  • Experimental: Part B: First Tepotinib TF2 Fasted then TF2 Fed
    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.
  • Experimental: Part B: First Tepotinib TF2 Fed then TF2 Fasted
    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.
  • Experimental: Part C: First Tepotinib TF3 Fasted then TF3 Fed
    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.
  • Experimental: Part C: First Tepotinib TF3 Fed then TF3 Fasted
    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.

Primary Outcome Measure

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 [ Time Frame: 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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