Drug reference

Temozolomide

Alkylating Agent · Antineoplastic agent

Alkylating AgentAntineoplastic agentATC null

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Avoid (teratogenic and embryotoxic in animals).

FDA category + note

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Mechanism

Temozolomide is an alkylating agent, specifically a triazene derivative, that exerts its cytotoxic effects by modifying DNA. It is classified as a cell cycle-nonspecific (CCNS) agent, meaning it can damage tumor cells whether they are actively dividing or in the resting phase (G0). This DNA damage ultimately leads to cell death.

Indications

Malignant gliomasNewly diagnosed high-grade gliomaRhabdomyosarcoma (investigational)high-grade malignant gliomas (standard agent, in combination with radiation therapy, for initial treatment)GliomaMalignant brain tumoursMelanoma

Dosing

Adult: l INDICATIONS AND DOSE Some lymphomas and chronic leukaemias (used either alone or in combination therapy) ▶ BY MOUTH ▶ Adult: (consult local protocol) IMPORTANT SAFETY INFORMATION RISKS OF INCORRECT DOSING OF ORAL ANTI-CANCER MEDICINES See Cytotoxic drugs p. 938. Children with nephrotic syndrome (increased seizure risk) .…

Pharmacokinetics

Onset

not specified

Peak effect

not specified

Bioavailability

approaching 100% (oral)

Protein binding

not specified

Metabolism

spontaneous, nonenzymatic activation to MTIC; primary urinary metabolite is inactive imidazole carboxamide

Contraindications

Pregnancy (teratogenic and embryotoxic in animals)
Conception during treatment (effective contraception advised for men and women)

Side effects

Common

hematological toxicities (mirror those of dacarbazine)NauseaVomitingFlu-like symptomsNeuropathyMyelosuppression

Serious

Pulmonary toxicity (lung infiltration, pulmonary fibrosis, pneumonitis, interstitial lung disease, potentially fatal)
Hepatotoxicity (with high intravenous doses, usually reversible, may be delayed)
Cerebral infarction (with implant use, uncommon)
Intracranial haemorrhage (with implant use, uncommon)
Gynaecomastia (with intravenous use, rare or very rare)
Nephrotoxicity (cumulative, with intravenous use, rare or very rare)
Peripheral vascular disease (with high intravenous doses, rare or very rare)