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tezacitabine + 5-fluorouracil
- Development stage
- Phase 2
- Lead developer
- Sanofi
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
Tezacitabine + 5-fluorouracil is a combination of two **antineoplastic agents** investigated for the treatment of advanced solid tumors. **Tezacitabine** is a novel nucleoside analog that, after intracellular phosphorylation, inhibits ribonucleotide reductase and is incorporated into DNA, leading to DNA chain termination; it thereby disrupts DNA synthesis. **5-fluorouracil (5-FU)** is a pyrimidine analog that primarily inhibits thymidylate synthase, resulting in impaired DNA synthesis and repair, and is also incorporated into RNA and DNA, exerting cytotoxic effects. The combination was studied in solid tumors (including esophageal and gastrointestinal carcinomas), showing tolerability and preliminary antitumor activity in Phase I trials[1][3].
- Other names
- (E)-2'-deoxy-2'-(fluoromethylene) cytidine + 5-fluorouracil
02
Targets
DNARRM1TS (Thymidylate synthase)
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