Temozolomide

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Temozolomide (Temodar in the US, Temodal in Europe) is an oral alkylating used for the treatment of anaplastic astrocytoma and GBM. A derivative of imidazotetrazine, temozolomide is the prodrug of MTIC (3-methyl-(triazen-1-yl)imidazole-4-carboxamide).

Mechanism of action

Temozolomide is an imidazotetrazine derivative of the alkylating agent dacarbazine. It undergoes rapid chemical conversion in the systemic circulation at physiological pH to the active compound, MTIC (monomethyl triazeno-imidazole carboxamide). Temozolomide exhibits schedule-dependent antineoplastic activity by interfering with DNA replication.

Indications

Temozolomide is considered standard of care chemotherapy for patients with anaplastic oligodendroglioma, anaplastic astrocytoma and GBM. Its use in the care of patients with low-grade glioma, oligodendroglioma and intracranial metastatic disease is under investigation.

Side Effects

The most common non-hematological adverse effects associated with temozolomide were nausea and vomiting and were either self-limiting or readily controlled with standard antiemetic therapy. These effects were usually mild to moderate (grade 1 to 2). Temozolomide may also cause myelosuppression.

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