Temozolomide

Drug

Drug Profile

Temozolomide is marketed as TEMODAR, an alkylating antineoplastic drug used in adults with newly diagnosed glioblastoma (with radiotherapy then maintenance) and anaplastic astrocytoma settings. It is a prodrug that converts nonenzymatically to MTIC, which alkylates DNA and induces tumor cell death. U.S. initial approval was in 1999.

Drug Class
Alkylating antineoplastic agent
Approval Status
FDA approved (Initial U.S. Approval: 1999)
Mechanism of Action
Prodrug rapidly converted at physiologic pH to MTIC, which primarily alkylates DNA at O6 and N7 guanine positions, causing DNA double-strand breaks and programmed cell death.
Brand Names
  • TEMODAR
Indications
  • \Newly diagnosed glioblastoma concomitantly with radiotherapy and then maintenance treatment in adults\
  • \Adjuvant treatment of newly diagnosed anaplastic astrocytoma in adults\
  • \Treatment of refractory anaplastic astrocytoma in adults\

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