Temozolomide: a novel oral alkylating agent

Expert Rev Anticancer Ther. 2001 Jun;1(1):13-9. doi: 10.1586/14737140.1.1.13.


Temozolomide is an imidazotetrazine with a mechanism of action and efficacy similar to dacarbazine (DTIC). However, it differs from DTIC in that it can be taken orally, degrades spontaneously to an active metabolite and penetrates the blood-brain barrier. It is well tolerated, making it a suitable candidate for combination chemotherapy. Trials to date have focussed on its activity in advanced metastatic melanoma and high-grade malignant glioma. Investigations into other indications, in particular solid tumors with central nervous system metastases, are ongoing. Studies of new drug schedules and of drugs to ameliorate temozolomide resistance offer the prospect of increased efficacy.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Antineoplastic Agents, Alkylating / administration & dosage
  • Antineoplastic Agents, Alkylating / therapeutic use*
  • Brain Neoplasms / drug therapy
  • Dacarbazine / administration & dosage
  • Dacarbazine / analogs & derivatives
  • Dacarbazine / therapeutic use*
  • Drug Administration Schedule
  • Glioma / drug therapy
  • Melanoma / drug therapy
  • Temozolomide


  • Antineoplastic Agents, Alkylating
  • Dacarbazine
  • Temozolomide