Temodar

Glioblastoma multiforme — newly diagnosed, concomitantly with radiotherapy and then as maintenance; Refractory anaplastic astrocytoma — patients who have experienced disease progression on a drug regimen containing nitrosourea and procarbazine

Newly diagnosed GBM (with radiation): 75 mg/m² daily for 42 days concomitant with focal radiotherapy, followed by maintenance: 150 mg/m² Days 1-5 of 28-day Cycle 1, then 200 mg/m² Days 1-5 if tolerated
Refractory anaplastic astrocytoma: 150 mg/m² once daily Days 1-5 per 28-day cycle; may increase to 200 mg/m² if ANC ≥1.5 and platelets ≥100K at Cycle 1 nadir
Take on empty stomach to reduce nausea
Antiemetic therapy: May be administered before or after

Capsules: 5 mg, 20 mg, 100 mg, 140 mg, 180 mg, 250 mg; For injection: 100 mg lyophilized powder

Hypersensitivity to temozolomide, dacarbazine, or any component.

• Myelosuppression: Prolonged pancytopenia may occur, resulting in aplastic anemia (fatal cases reported). Nadir usually Days 21-28, recovery within 14 days. Monitor CBC on Day 22 (21 days after first dose) or within 48 hours, and weekly until ANC >1.5 × 10⁹/L and platelets >100 × 10⁹/L.
• Myelodysplastic Syndrome/Secondary Malignancies: MDS and secondary malignancies including myeloid leukemia reported.
• Pneumocystis Pneumonia (PCP): Higher risk during 42-day concomitant treatment. PCP prophylaxis required for all patients receiving concomitant radiotherapy regimen.
• Hepatotoxicity: Including fatal hepatic failure. Monitor LFTs at baseline, midway through first cycle, prior to each subsequent cycle.
• Embryo-Fetal Toxicity

Concomitant phase: Alopecia (69%), nausea (49%), fatigue (38%), constipation (33%), vomiting (29%), headache (23%), thrombocytopenia (14%), anorexia (19%)
Maintenance phase: Fatigue (34%), nausea (29%), constipation (22%), vomiting (17%), headache (15%), thrombocytopenia (19%), lymphopenia (12%)

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.

Consult the full prescribing information for pregnancy-related considerations.

Refer to prescribing information for lactation guidance.

Pediatric safety and efficacy information is detailed in the full label.

Dose modifications for organ impairment are specified in the complete prescribing information.

Temozolomide is a prodrug that undergoes rapid nonenzymatic conversion at physiologic pH to the reactive compound MTIC (5-(3-methyltriazen-1-yl)-imidazole-4-carboxamide). MTIC methylates DNA at the O⁶ and N⁷ positions of guanine. This methylation triggers the mismatch repair system, leading to DNA strand breaks and apoptosis. The cytotoxicity is enhanced in cells with deficient O⁶-methylguanine-DNA methyltransferase (MGMT) activity.

Tmax: 1 hour (oral). Bioavailability: approximately 100%. Half-life: 1.8 hours. Protein binding: 15%. Crosses blood-brain barrier (CNS concentrations approximately 30% of plasma). Excreted primarily in urine (38% as unchanged MTIC, 6% as unchanged temozolomide).

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• EORTC/NCIC — Temozolomide + radiotherapy vs. radiotherapy alone in newly diagnosed glioblastoma. Phase III, n=573.
  🔬 NCT00006353 ↗ 📄 Primary Publication ↗

Temodar has FDA-approved indications across the following cancer types covered on PipelineEvidence: