Temozón

Temozolomide

Temozolomide (brand names Temodar and Temodal | Schering-Plough) is an oral chemotherapy drug. It is an alkylating agent used for the treatment of Grade IV astrocytoma — an aggressive brain tumor, also known as glioblastoma multiforme.

Mechanism of Action

Temozolomide is a prodrug, meaning it is metabolized into its active form in the body. It undergoes rapid chemical conversion in the systemic circulation at physiological pH to the active compound, MTIC (5-(3-methyltriazen-1-yl)-imidazole-4-carboxamide).

The cytotoxicity of temozolomide is thought to be caused primarily by alkylation of DNA. This damage is recognized and repaired by the enzyme O6-methylguanine-DNA methyltransferase (MGMT), but the repair process leads to the introduction of DNA strand breaks. If the damage is not successfully repaired, the cells undergo apoptosis, or programmed cell death.

Clinical Use

Temozolomide is used in the treatment of certain types of brain tumors such as glioblastoma multiforme and anaplastic astrocytoma. It is usually given after other cancer medicines have been tried without success.

Side Effects

Like all chemotherapy, temozolomide can cause side effects, the nature of which can vary from person to person. Some people might experience very few side effects while others may experience more. The most common side effects are fatigue, nausea, and vomiting. Other side effects can include loss of appetite, constipation, headaches, and hair loss.

See Also

• Chemotherapy
• Glioblastoma multiforme
• Anaplastic astrocytoma

References

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