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Temodar (temozolomide)
Temodar works by attaching an alkyl group to the DNA of cancer cells, interfering with their ability to replicate and ultimately leading to cell death.
Temodar (temozolomide) is a small molecule alkylating drug originally developed by Merck Sharp Dohme and currently owned by the same company. It was FDA approved in 1999 for the treatment of various types of brain cancers, including astrocytoma, Ewing's sarcoma, glioblastoma multiforme, glioma, and malignant glioma. Temodar is now off-patent and has multiple generic manufacturers. The drug has a short half-life of 1.5 hours and high bioavailability of 96%. It is used in combination with other treatments to improve patient outcomes.
At a glance
| Generic name | temozolomide |
|---|---|
| Sponsor | Merck & Co. |
| Drug class | Alkylating Drug [EPC] |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 1999 |
Mechanism of action
Temozolomide is not directly active but undergoes rapid nonenzymatic conversion at physiologic pH to the reactive compound 5-(3methyltriazen-1-yl)-imidazole-4-carboxamide (MTIC). The cytotoxicity of MTIC is thought to be primarily due to alkylation of DNA. Alkylation (methylation) occurs mainly at the O6and N7positions of guanine.
Approved indications
- Astrocytoma, anaplastic
- Ewing's sarcoma
- Glioblastoma multiforme of brain
- Glioma, malignant
Common side effects
- Alopecia
- Fatigue
- Nausea
- Vomiting
- Constipation
- Headache
- Convulsions
- Thrombocytopenia
- Decreased lymphocytes
- Decreased platelets
- Decreased neutrophils
- Decreased leukocytes
Key clinical trials
- Vorinostat and Temozolomide in Treating Patients With Malignant Gliomas (PHASE1)
- Hyperpolarized Carbon-13 (13C) Pyruvate Imaging in Patients With Glioblastoma (PHASE1)
- Dinutuximab With Chemotherapy, Surgery and Stem Cell Transplantation for the Treatment of Children With Newly Diagnosed High Risk Neuroblastoma (PHASE3)
- Testing the Addition of an Anti-cancer Drug, Selinexor, to the Usual Chemotherapy Treatment (Temozolomide) for Brain Tumors That Have Returned After Previous Treatment (PHASE1,PHASE2)
- Drug Repurposing in Thyroid Carcinoma: a Feasibility Trial (PHASE1)
- Temozolomide With or Without Veliparib in Treating Patients With Newly Diagnosed Glioblastoma Multiforme (PHASE2,PHASE3)
- Study of Tislelizumab, Pamiparib, and Other Investigational Agents in Participants With Advanced Malignancies (PHASE3)
- Testing the Combination of the Anti-Cancer Drugs Temozolomide and M1774 to Evaluate Their Safety and Effectiveness (PHASE1,PHASE2)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Temodar CI brief — competitive landscape report
- Temodar updates RSS · CI watch RSS
- Merck & Co. portfolio CI