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 established
Diseases for which it is used
- Acute myeloid leukemia
- 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
- 1999-08-11: Initial accelerated 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. (Based on MK-7365-006)
- 2005-03-15: Regular approval for newly diagnosed glioblastoma multiforme (GBM) concomitantly with radiotherapy and then as maintenance treatment. (Based on EORTC 22981/26981; NCIC-CTG CE.3)
- 2005-03-15: Regular approval for refractory anaplastic astrocytoma patients who have experienced disease progression on a drug regimen containing nitrosourea and procarbazine. (Based on MK-7365-006)
- 2023-09-14: Project Renewal revised indication for adjuvant treatment of adults with newly diagnosed anaplastic astrocytoma. (Based on CATNON)
- 2023-09-14: Project Renewal revised indication for treatment of adults with refractory anaplastic astrocytoma. (Based on MK-7365-006)
History of changes in EMA indication
- 1999-01-26: Initial marketing authorization as Temodal.
History of changes in PMDA indication
- 2006-07-26: Initial approval for treatment of malignant glioma.
- 2019-02-21: New additional indication and a new dosage for the treatment of relapsed or refractory Ewing's sarcoma.
Also known as
- Generic name: TMZ
- Brand names: Gliotem, Temcad, Temizole, Temodal, Temodar, Temomedac, Temonat, Temoside, Temoz, Temzol