Name: | temozolomide |
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PubChem Compound ID: | 10012882 |
Molecular formula: | C6H6N6O2 |
Molecular weight: | 195.144 g/mol |
Name: | temozolomide |
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Name (isomeric): | DB00853 |
Drug Type: | small molecule |
Synonyms: |
Methazolastone; Temozolamide; Temozolomidum [Latin]; Temozolodida [Spanish]
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Brand: | Temodar, Temodal |
Category: | Antineoplastic Agents, Antineoplastic Agents, Alkylating |
CAS number: | 85622-93-1 |
Indication: | For the treatment of adult patients diagnosed with anaplastic astrocytoma whose disease has progressed after therapy with nitrosourea and procarbazine, as well as concomitantly with radiation therapy for treatment of newly diagnosed glioblastoma multiforme. Also used as maintenance therapy for glioblastoma multiforme. |
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Pharmacology: |
Temozolomide is an imidazotetrazine deritave and an antineoplastic agent. It is a prodrug that has little to no pharmacological activity until it is hydrolyzed in vivo to 5-(3-methyltriazen-1-yl)imidazole-4-carboxamide (MTIC). After administration, temozolomide undergoes rapid, nonenzymatic hydrolysis at physiological pH to MTIC, which is the activ...
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Mechanism of Action: |
Temozolomide is not active until it is converted at physiologic pH to MTIC. It is suggested that MTIC then alkylates DNA at the N7 position of guanine, O3 position of adenosine, and O6 position of guanosine, with the most common site being the N7 position. This methylation of guanine residues lead to single and double-strand DNA breaks and subseque...
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Absorption: | Rapid and complete absorption in the gastrointestinal tract |
Protein binding: | 15% |
Route of elimination: | About 38% of the administered temozolomide total radioactive dose is recovered over 7 days: 37.7% in urine and 0.8% in feces. |
Half Life: | Approximately 1.8 hours. |
Clearance: | 5.5 L/hr/m2 |
Affected organisms: | Humans and other mammals |
Drug interaction: |
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