Combination of temozolomide with immunocytokine F16-IL2 for the treatment of glioblastoma

Br J Cancer. 2010 Sep 7;103(6):827-36. doi: 10.1038/sj.bjc.6605832. Epub 2010 Aug 24.

Abstract

Background: Glioblastoma patients are still not cured by the treatments available at the moment. We investigated the therapeutic properties of temozolomide in combination with F16-IL2, a clinical-stage immunocytokine consisting of human interleukin (IL)-2 fused to the human antibody F16, specific to the A1 domain of tenascin-C.

Methods: We conducted three preclinical therapy studies, using subcutaneous and intracranial U87MG glioblastoma tumours xenografted in BALB/c nude mice. The same therapeutic schedule was used, consisting of five total administrations every third day, of 0.525 mg temozolomide, 20 microg F16-IL2, the combination, or the control solution.

Results: Immunohistochemical analysis of U87MG xenografts and of human glioblastoma specimens showed selective tumour staining of F16. A quantitative biodistribution confirmed the preferential tumour accumulation of radiolabelled F16-IL2. In the study with subcutaneous xenografts, the combination of F16-IL2 with temozolomide induced complete remission of the animals, which remained tumour free for over 160 days. The same treatment led to a consistent size reduction of intracranial xenografts and to a longer survival of animals. The immunocytokine promoted the recruitment of leukocytes into tumours of both models.

Conclusion: The combined use of temozolomide with F16-IL2 deserves clinical investigations, which will be facilitated by the excellent safety profile in cynomolgus monkeys, and by the fact that F16-IL2 is in clinical trials in patients with cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / pharmacokinetics
  • Antineoplastic Agents / therapeutic use*
  • Apoptosis
  • Brain Neoplasms / drug therapy*
  • Brain Neoplasms / pathology
  • Cell Proliferation
  • Dacarbazine / administration & dosage
  • Dacarbazine / analogs & derivatives*
  • Dacarbazine / pharmacokinetics
  • Dacarbazine / therapeutic use
  • Glioblastoma / drug therapy*
  • Glioblastoma / pathology
  • Humans
  • Immunohistochemistry
  • Interleukin-2 / administration & dosage
  • Interleukin-2 / pharmacokinetics
  • Interleukin-2 / therapeutic use*
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Neoplasm Transplantation
  • Temozolomide
  • Tissue Distribution

Substances

  • Antineoplastic Agents
  • Interleukin-2
  • Dacarbazine
  • Temozolomide