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tegafur + temozolomide
- Development stage
- Unknown
- Lead developer
- Taiho Pharmaceutical
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Tegafur + temozolomide is a combination chemotherapy regimen primarily investigated for the treatment of advanced neuroendocrine tumors (NETs), including pancreatic and extrapancreatic variants. Tegafur is a small molecule prodrug of 5-fluorouracil (5-FU) that acts as a thymidylate synthase inhibitor, disrupting DNA synthesis. Temozolomide is an oral alkylating agent that induces DNA damage by methylating guanine residues. In clinical practice, tegafur is frequently administered as part of the S-1 formulation (Teysuno), which includes gimeracil and oteracil to optimize 5-FU levels and reduce gastrointestinal toxicity. The combination of these two agents aims to achieve synergistic anti-tumor effects through complementary mechanisms of DNA disruption and is currently being evaluated in Phase II clinical trials in China.
- Other names
- S-1 + temozolomideS-1 plus temozolomideS1 plus temozolomideS 1 plus temozolomideS-1/TMZ
02
Targets
N7-G (DNA guanine-N7 adduct)TS (Thymidylate synthase)
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