Active ingredient: Temozolomide - Basic Profile / Key Facts

Basic Profile / Key Facts

Drug Category

• Antineoplastic Agents

Dosage Forms

• Capsule

Indications

For the treatment of adult patients diagnosed with anaplastic astrocytoma who have relapsed following chemotherapy

Pharmacology

Temozolomide is an antineoplastic agent. It causes death of of rapidly replicating cells, especially malignant cells, leading to regression or slowed tumor growth.

Mechanism of Action

Temozolomide is not active until it is converted at physiologic pH to the active form, 5-(3-methyltriazen-1-yl)imidazole-4-carboxamide (MTIC). The cytotoxicity of MTIC is due to alkylation of DNA at the O6 and N7 positions of guanine.

Absorption

Rapid and complete absorption in the gastrointestinal tract

Toxicity

Not Available

Biotrnasformation / Drug Metabolism

Not Available

Contraindications

TEMODAR (temozolomide) Capsules are contraindicated in patients who have a history of hypersensitivity reaction to any of its components. TEMODAR is also contraindicated in patients who have a history of hypersensitivity to DTIC, since both drugs are metabolized to MTIC.

Drug Interactions

Administration of valproic acid decreases oral clearance of temozolomide by about 5%. The clinical implication of this effect is not known.

Patients with Severe Hepatic or Renal Impairment

Caution should be exercised when TEMODAR Capsules are administered to patients with severe hepatic or renal impairment.