Bioequivalence of 2 Formulations of TKI258 in Patients With Advanced Solid Tumors


This is a multi-center, open-label, two way crossover study designed to test the bioequivalence of 2 different oral forms of TKI258, FMI capsule and FMI tablet in patients with advanced solid tumors, excluding breast cancer. The aim of this test is to demonstrate that those 2 formulations are considered to be the same for all intents and purposes by making sure they are acting on the body with the same strength and are absorbed in similar amounts by the body. During the bioequivalence phase, patients will take orally at a daily dose of 500 mg one formulation of TKI258 during the first 3 weeks of treatment on a 5 days on/2days off dosing schedule, after which time, patients will switch to the alternate formulation for one additional week. After the bioequivalence phase, all patients may continue to take orally at a daily dose of 500 mg only TKI258 FMI capsule formulation until disease progression (assessed by RECIST 1.1), unacceptable toxicity, death or discontinuation from the study treatment for any other reason.

Full Title of Study: “A Phase I, Open-label, Multi-center, Randomized, Crossover Study to Assess the Bioequivalence of 2 Formulations of TKI258, FMI Capsule and FMI Tablet, in Patients With Advanced Solid Tumors”

Study Type

  • Study Type: Interventional
  • Study Design
    • Allocation: Randomized
    • Intervention Model: Crossover Assignment
    • Primary Purpose: Treatment
    • Masking: None (Open Label)
  • Study Primary Completion Date: July 2014


  • Drug: TKI258

Arms, Groups and Cohorts

  • Experimental: 500 mg FMI capsule + 250 mg FMI tablet
    • BE phase sequence 1= 3 weeks on FMI capsule then 1 week on FMI tablet
  • Experimental: 500 mg TKI258 FMI capsule +250 mg FMI tablet
    • BE phase sequence 2= 3 weeks on FMI tablet then 1 week on FMI capsule

Clinical Trial Outcome Measures

Primary Measures

  • Composite of Pharmacokinetics of TKI258, FMI capsule (supplied in 100 mg strength) and FMI tablet (supplied in 250 mg strength), in patients with advanced solid tumors, excluding breast cancer based on PK parameters AUClast and Cmax
    • Time Frame: 9 days

Secondary Measures

  • Frequency of Adverse Events in patients treated with TKI258 on a 5 days on/2 days off dosing schedule in patients with advanced solid tumors, excluding breast cancer
    • Time Frame: up to 30 days after the last dose of study drug
  • Preliminary evidence of anti-tumor activity based on RECIST criteria of TKI258 in patients with advanced solid tumors, excluding breast cancer
    • Time Frame: Every 8 weeks until progression of disease

Participating in This Clinical Trial

Inclusion Criteria

1. Patients with a histopathologically or cytopathologically confirmed diagnosis of an advanced solid tumor, excluding breast cancer, who have progressed despite standard therapy, or for which no standard therapy exists

2. ECOG performance status (PS) 0, 1 or 2

3. Patients must meet protocol-specified laboratory values

Exclusion Criteria

1. Patients with brain metastases

2. Patients who have concurrent severe and/or uncontrolled medical conditions which could compromise participation in the study

3. Patients who have not recovered from previous anti-cancer therapies

4. Patients who are expected to receive any prohibited medications during the bioequivalence phase of the study

5. Female patients who are pregnant, breast feeding

6. Fertile male or women of child-bearing potential not willing to use two highly effective methods of contraception

Other protocol-defined inclusion/exclusion criteria may apply

Gender Eligibility: All

Minimum Age: 18 Years

Maximum Age: N/A

Are Healthy Volunteers Accepted: No

Investigator Details

  • Lead Sponsor
    • Novartis Pharmaceuticals
  • Provider of Information About this Clinical Study
    • Sponsor
  • Overall Official(s)
    • Novartis Pharmaceuticals, Study Director, Novartis Pharmaceuticals
    • Novartitis Pharmaceuticals, Study Director, Novartitis Pharmaceuticals

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