Abstract

Temozolomide, an oral alkylating agent, is a commonly used medicine in the treatment of anaplastic astrocytoma and glioblastoma multiforme. This paper will present the mechanism of action as well as the clinical role for this chemotherapeutic drug.

Highlights

  • Temozolomide (Temodar) is an oral alkylating agent approved by the FDA for use in the first-line treatment of glioblastoma multiforme as well as for recurrent anaplastic astrocytoma.[1]

  • The proposed mechanism of action is based on the ability of its metabolites to deposit methyl groups on DNA guanine bases

  • MTIC methylates a number of nucleobases, most important, the guanine base

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Summary

Introduction

Temozolomide (Temodar) is an oral alkylating agent approved by the FDA for use in the first-line treatment of glioblastoma multiforme as well as for recurrent anaplastic astrocytoma.[1]. Proposed Mechanism of Action Temozolomide is an oral alkylating agent, first developed in the early 1980s at Aston University in Great Britain.[3] The proposed mechanism of action is based on the ability of its metabolites to deposit methyl groups on DNA guanine bases. The prodrug temozolomide is readily absorbed in the small intestine, with good penetration of the blood-brain barrier due to its small size (194 Da).

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