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A phase I study of E7080, a multitargeted tyrosine kinase inhibitor, in patients with advanced solid tumours

D S Boss1, H Glen, J H Beijnen

  • 1Division of Medical Oncology, Department of Clinical Pharmacology, The Netherlands Cancer Institute, Plesmanlaan 121, Amsterdam, The Netherlands.

British Journal of Cancer
|April 21, 2012
PubMed
Abstract

Insights

E7080 demonstrated good tolerability up to 25 mg daily in advanced solid tumor patients. Preliminary efficacy was observed in melanoma and renal cell carcinoma, warranting further investigation.

Area of Science:

  • Oncology
  • Pharmacology

Background:

  • Phase I study of E7080 in advanced, refractory solid tumors.
  • Assessed safety, tolerability, maximum tolerated dose (MTD), pharmacokinetics, and anti-tumor efficacy.

Purpose of the Study:

  • Determine the safety and tolerability of E7080.
  • Establish the MTD and pharmacokinetic profile.
  • Explore preliminary anti-tumor efficacy.

Main Methods:

  • Oral administration of E7080 in escalating doses (0.2-32 mg) daily.
  • Pharmacokinetic sampling during cycle 1 and cycle 2.
  • Anti-tumor efficacy assessed every two cycles.

Main Results:

  • MTD established at 25 mg daily; dose-limiting toxicity was grade 3 proteinuria.
  • Common toxicities included hypertension (40%), diarrhea (45%), nausea (37%), stomatitis (32%), and vomiting (23%).
  • Partial response in 9% and stable disease in 46% of patients; dose-linear pharmacokinetics observed.

Conclusions:

  • E7080 is well tolerated up to 25 mg/day.
  • Encouraging anti-tumor activity observed in melanoma and renal cell carcinoma patients.

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