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gemcitabine + fluorouracil + leucovorin
- Development stage
- Unknown
- Lead developer
- Eli Lilly
- Modality
- Small Molecules
- Administration
- Intravenous, Oral
01
Overview
This combination therapy consists of gemcitabine, 5-fluorouracil (5-FU), and leucovorin, investigated by the National Institutes of Health Clinical Center (CC) for the treatment of advanced solid tumors and lymphomas. Gemcitabine is a pyrimidine antimetabolite that inhibits DNA synthesis through the inhibition of ribonucleotide reductase and incorporation into DNA. Fluorouracil is a thymidylate synthase inhibitor that interferes with pyrimidine synthesis, while leucovorin (folinic acid) is administered to potentiate the cytotoxic effects of 5-FU by stabilizing its binding to the target enzyme. This specific regimen was evaluated in a Phase I dose-escalation study to determine the safety and efficacy in patients with refractory, recurrent, or metastatic malignancies.
- Brand names
- GemzarAdrucilWellcovorin
- Other names
- Gemcitabine/5-FU/LVGFL regimen
02
Targets
TS (Thymidylate synthase)RNR (Ribonucleotide reductase)DNA polymerase family
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