Temozolomide (Temodar)
Other Medications · Approved since 1999
Description
Temozolomide is an oral alkylating chemotherapy agent used off-label in colorectal cancer, particularly in tumors with MGMT methylation or mismatch repair deficiency. This DNA-damaging agent is primarily FDA-approved for brain tumors but has shown activity in CRC patients whose tumors have specific molecular characteristics that make them more susceptible to alkylating damage. In colorectal cancer, temozolomide is often combined with other agents like capecitabine or radiation therapy, especially in locally advanced rectal cancer with MGMT silencing.
Mechanism of Action
Temozolomide spontaneously converts to its active metabolite MTIC (methyl-triazeno-imidazole-carboxamide), which methylates DNA at the O6 position of guanine residues, leading to DNA strand breaks and cell death. Tumors with methylated MGMT (O6-methylguanine-DNA methyltransferase) promoter are particularly sensitive because they cannot efficiently repair this DNA damage.
Molecular Targets
Side Effects
Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.
Clinical Trials
Quick Info
| Brand Name | Temodar |
| Category | Other Medications |
 Status | Off-label |
 EMA Status | EMA Approved |
 Spain Access | Funded by SNS off-label in CRC |
| Administration | Oral |
| Year Approved | 1999 |
| Clinical Trials | 15 |
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Medical Disclaimer
This information is for educational purposes only and should not replace professional medical advice. Always consult your healthcare team before making treatment decisions.