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cisplatin + gemcitabine + uracil-tegafur
- Development stage
- Unknown
- Lead developer
- Michigan State University
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Intravenous, Oral
01
Overview
This is a combination chemotherapy regimen consisting of three agents: - **Cisplatin** is a platinum-based chemotherapeutic that forms DNA crosslinks and inhibits DNA synthesis and function. - **Gemcitabine** is a nucleoside analog that inhibits DNA synthesis by incorporation into DNA and inhibition of ribonucleotide reductase. - **Uracil-tegafur (UFT)** is an oral prodrug combination of tegafur (a 5-fluorouracil [5-FU] prodrug) with uracil, which enhances the efficacy of 5-FU by inhibiting its degradation. This regimen has been studied as first-line therapy for advanced non-small-cell lung cancer (NSCLC), showing activity and tolerability. It has also been investigated in other solid tumors such as advanced pancreatic cancer (APC) and biliary tract cancers[1][2][5]. The mechanism involves synergistic cytotoxic effects on rapidly dividing tumor cells through multiple pathways affecting DNA replication.
- Other names
- cisplatin + gemcitabine + UFTcisplatin + gemcitabine + uracil/tegafurCDDP + GEM + UFT
02
Targets
TS (Thymidylate synthase)DNARNR (Ribonucleotide reductase)
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