Temozolomide (Temodar)

General information

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.^[1]^[2]
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.^[1]

Diseases for which it is established

Diseases for which it is used

Patient drug information

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

References

[insert-1] 1.0 ^1.1 ^1.2 Temozolomide (Temodar) package insert

[2] Temozolomide (Temodar) package insert (locally hosted backup)

[3] Temozolomide (Temodar) patient drug information (Chemocare)

[4] Temozolomide (Temodar) patient drug information (UpToDate)

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