Article: Temozolomide

Temozolomide
Systematic (IUPAC) name
4-methyl-5-oxo- 2,3,4,6,8-pentazabicyclo [4.3.0] nona-2,7,9-triene- 9-carboxamide
Identifiers
CAS number	85622-93-1
ATC code	L01AX03
PubChem	5394
DrugBank	APRD00557
Chemical data
Formula	C6H6N6O2
Mol. weight	194.151 g/mol
Pharmacokinetic data
Bioavailability	?
Protein binding	15%
Metabolism	spontaneously hydrolized at physiologic pH to the active species, 3-methyl-(triazen-1-yl)imidazole-4-carboxamide (MTIC) and to temozolomide acid metabolite.
Half life	1.8 hours
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status	℞-only(US)
Routes	Oral

Temozolomide (brand name Temodar® Schering-Plough Corporation) is an oral alkylating agent used for the treatment of refractory anaplastic astrocytoma -- a type of cancerous brain tumor. A derivative of imidazotetrazine, temozolomide is the prodrug of MTIC (3-methyl-(triazen-1-yl)imidazole-4-carboxamide). It has been avaialble in the US since August 1999.

Indications

• Glioblastoma multiforme: for the treatment of adult patients with newly diagnosed glioblastoma multiforme concomitantly with radiotherapy.
• Anaplastic astrocytoma: for the treatment of adult patients with refractory anaplastic atrocytoma (ie. patients who have experienced disease progression on a drug regimen containing nitrosourea and procarbazine).
• Unlabeled uses: Metastatic melanoma.

Formulations

Temozolomide is available in the United States in 5mg, 20mg, 100mg, & 250mg capsules.