Class/mechanism: Alkylator. Temozolomide is converted in vivo to the reactive compound 5-(3-methyltriazen-
1-yl)-imidazole-4-carboxamide (MTIC). MTIC causes alkylation of DNA at the O6 and N7 positions of guanine, leading to cell damage and cell death.
Route: PO, IV
Extravasation: no information
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.
Diseases for which it is used
- Acute myeloid leukemia
- Anaplastic glioma
- CNS lymphoma
- Ewing sarcoma
- Low-grade glioma
- Myelodysplastic syndrome
- Neuroendocrine tumor
- Pancreatic NET
- Soft tissue sarcoma
- Small cell lung cancer
- Uveal melanoma
Patient drug information
- Temozolomide (Temodar) package insert
- Temozolomide (Temodar) patient drug information (Chemocare)
- Temozolomide (Temodar) patient drug information (UpToDate)
History of changes in FDA indication
- 8/11/1999: Initial FDA approval for treatment of adult patients with refractory anaplastic astrocytoma, i.e., patients at first relapse who have experienced disease progression on a drug regimen containing a nitrosourea and procarbazine
- Indicated for newly diagnosed glioblastoma multiforme (GBM) concomitantly with radiotherapy and then as maintenance treatment.
- Indicated for refractory anaplastic astrocytoma patients who have experienced disease progression on a drug regimen containing nitrosourea and procarbazine.
Also known as
- Generic name: TMZ
- Brand names: Gliotem, Temcad, Temizole, Temodal, Temodar, Temonat, Temoside, Temoz, Temzol