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gemcitabine + tegafur-uracil + leucovorin
- Development stage
- Unknown
- Lead developer
- Barbara Ann Karmanos Cancer Institute
- Modality
- Small Molecules
- Administration
- Intravenous, Oral
01
Overview
This is a combination chemotherapy regimen consisting of gemcitabine, UFT (a 4:1 molar ratio of uracil and tegafur), and leucovorin (calcium folinate). Gemcitabine is a nucleoside analog that inhibits DNA synthesis through the inhibition of ribonucleotide reductase and masked chain termination after incorporation into DNA. UFT is an oral fluoropyrimidine where tegafur acts as a prodrug for 5-fluorouracil (5-FU), and uracil competes with 5-FU for the enzyme dihydropyrimidine dehydrogenase (DPD), thereby increasing 5-FU levels. Leucovorin is included to enhance the binding of 5-FU to its target, thymidylate synthase, increasing the cytotoxic effect. This specific combination was investigated in a Phase I dose-escalation study conducted by the Barbara Ann Karmanos Cancer Institute at Wayne State University to treat patients with advanced refractory solid tumors.
- Brand names
- UFT
- Other names
- gemcitabine + UFT + leucovoringemcitabine + UFT + LVgemcitabine + uracil-tegafur + calcium folinate
02
Targets
RNR (Ribonucleotide reductase)TS (Thymidylate synthase)DNADPYD (Dihydropyrimidine dehydrogenase)
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