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Phase I dose escalation study of telatinib (BAY 57-9352) in patients with advanced solid tumours

D Strumberg1, B Schultheis, I A Adamietz

  • 1Department of Haematology and Medical Oncology, University of Bochum (Marien Hospital, Herne), Herne, Germany. dirk.strumberg@marienhospital-herne.de

British Journal of Cancer
|November 13, 2008
PubMed

Insights

Telatinib, a VEGFR and PDGF inhibitor, is safe and well-tolerated in patients with solid tumors. A continuous daily dose of 900 mg was recommended for Phase II trials based on safety and efficacy.

Area of Science:

  • Oncology
  • Pharmacology
  • Clinical Trials

Background:

  • Telatinib is an oral small-molecule inhibitor targeting VEGFR-2/-3 and PDGF-Rbeta tyrosine kinases.
  • Vascular endothelial growth factor receptors (VEGFR) and platelet-derived growth factor receptors (PDGF) are key targets in cancer therapy.

Purpose of the Study:

  • To evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of telatinib in patients with refractory solid tumors.
  • To determine the recommended Phase II dose for telatinib.

Main Methods:

  • A multicenter Phase I dose escalation study.
  • 71 patients with refractory solid tumors received telatinib BID in noncontinuous or continuous dosing schedules.
  • Pharmacokinetic and pharmacodynamic parameters were assessed, along with adverse events.

Main Results:

  • Telatinib was safe and well-tolerated up to 1500 mg BID continuous dosing; maximum-tolerated dose was not reached.
  • Hypertension and diarrhea were the most frequent grade 3 adverse events.
  • Pharmacokinetics showed rapid absorption, with Cmax and AUC plateauing at 900-1500 mg BID. Tumor blood flow and sVEGFR-2 levels decreased with increasing telatinib exposure.

Conclusions:

  • Telatinib demonstrates a favorable safety profile in patients with refractory solid tumors.
  • A continuous daily dose of 900 mg BID was identified as the recommended dose for Phase II studies based on pharmacokinetic and pharmacodynamic data.

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