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temozolomide + radiation therapy
- Development stage
- Unknown
- Lead developer
- Eastern Cooperative Oncology Group
- Modality
- Implantable Devices → Device-based Delivery → Drug Delivery Systems, Small Molecules
- Administration
- Oral, Radiation
01
Overview
This therapeutic regimen consists of the oral alkylating agent temozolomide administered concurrently with and following whole-brain radiation therapy (WBRT). Temozolomide is a lipophilic prodrug that crosses the blood-brain barrier and undergoes spontaneous hydrolysis at physiological pH to its active metabolite, MTIC. MTIC exerts its cytotoxic effect by methylating DNA at the O6 and N7 positions of guanine, which triggers DNA mismatch repair-mediated apoptosis. When administered concurrently with radiation, temozolomide acts as a radiosensitizer, potentially overcoming tumor resistance and enhancing the therapeutic index of radiotherapy in the treatment of brain metastases from non-small cell lung cancer (NSCLC). The Eastern Cooperative Oncology Group (ECOG) conducted Phase II trials, such as E3501, to evaluate this combination's safety and efficacy in improving local control and survival for NSCLC patients with brain involvement.
- Brand names
- TemodarTemodal
- Other names
- TMZ + WBRTTemozolomide + Whole-Brain Radiation TherapyTemozolomide + Radiation
02
Targets
DNA
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