Brain tumours in children and Temozolomide 


Brain tumours in children are the most common of the solid tumours and account for about 16% of all pediatric malignancy, being second only to leukaemia. The treatment of brain tumours embraces a multidisciplinary approach involving surgery, radiotherapy and chemotherapy. To date, we are lacking in drugs being efficacious without severe side effects, therefore more active and less toxic compounds are urgently needed.

Temozolomide belongs to the imidazotetrazine class and it is a DNA-methylating agent. TMZ is a pro-drug, spontaneously converted into its active form at physiological pH, thus not requires enzymatic activation in the liver. It has almost 100% oral bioavailability, with some limited influence of the fasting state, and is able to cross the blood brain barrier, showing a good activity against gliomas in adults. On the basis of the results obtained in adult malignant gliomas, phase I and II clinical trials were performed to evaluate the efficacy and the safety of the use of this novel drug in pediatric cancer too, but pediatric brain gliomas do not appear to be sensitive to this compound, at least alone, and even though, Verschuur et al. observed a mild response in children with oligodendrogliomas, this kind of tumour is very rare in children.

The dose limiting toxicity is a reversible and non-cumulative myelosuppression: neutropenia and, especially, thrombocytopenia are more frequent with the use of the 5-day schedule, occurring about 21 days after the first dose of the cycle and recovering within 7-14 days.  Another significant aspect of TMZ toxicity profile is the lymphocytopenia and low CD4+ cell counts, that occur with all extended schedule of administration both in adults and children.

To date, some aspects of the use of TMZ in children remain unknown, such as the administration with other compounds (i.e. VP16 or Cisplatin) or its use with extended schedule. So, phase II clinical trial are necessary to clarify the real efficacy of TMZ in children.

However, in their multicentric study, Cefalo et al. showed the good antitumour activity of TMZ against refractory or recurrent Medulloblastoma/PNET. Although  this study is still ongoing, these data are very interesting because TMZ may become the first line drug for the treatment of this kind of tumour.

In conclusion, even though TMZ alone did not show the expected efficacy, new phase II clinical trials should be performed to prove its efficacy in combination with other drug or using new schedules, especially against Medulloblastoma /PNET.  

 

Bibliographical reference:

Barone G et al.: "Role of temozolomide in pediatric brain tumors", Childs Nerv Syst. 2006 Mar 25

 

Giuseppe Barone

Division of Pediatric Oncology, Catholic University of Rome, Largo A. Gemelli, 8, Rome, Italy