Products
Temozolomide is commercially available as capsules and as a powder for the preparation of an infusion solution (Temodal, generics). It has been approved in many countries since 1999.
Structure and properties
Temozolomide (C6H6N6O2, Mr = 194.2 g/mol) is an imidazotetrazine derivative. It is a prodrug that is biotransformed by hydrolysis to the active metabolite MTIC. Temozolomide is structurally related to dacarbazine.
Effects
Temozolomide (ATC L01AX03) has cytostatic, alkylating, and antitumor properties. The effects are due to alkylation of DNA, leading to cell death of cancer cells (methylation of guanine at positions O6 and N7).
Indications
For the treatment of brain tumors:
- Glioblastoma multiforme
- Recurrent malignant glioma
Dosage
According to the SmPC. The drug can be administered perorally (capsules) or as an intravenous infusion.
Contraindications
- Hypersensitivity
- Pregnancy and lactation
- Severe hepatic or renal insufficiency
- Severe myelosuppression
For complete precautions, see the drug label.
Interactions
Drug-drug interactions have been described with valproic acid and myelosuppressive agents.
Adverse effects
The most common possible adverse effects include:
- Hair loss, skin rash
- Fatigue, weakness
- Nausea, vomiting, lack of appetite, constipation, diarrhea.
- Headache, fever, dizziness, incoordination.
- Infectious diseases
- Amnesia, sleep disorders
- Bone marrow toxicity
- Allergic reactions
- Liver toxicity: temozolomide has liver toxic properties and severe liver injury has been reported. Appropriate precautions should be observed.
