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methotrexate + 5-fluorouracil
- Development stage
- Unknown
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Intravenous, Intralesional
01
Overview
Methotrexate + 5-fluorouracil is a combination chemotherapy regimen consisting of two antimetabolite agents, methotrexate (MTX) and 5-fluorouracil (5-FU). Both drugs disrupt DNA synthesis but through different mechanisms. Methotrexate inhibits dihydrofolate reductase, blocking folic acid metabolism and thereby preventing the synthesis of purine nucleotides required for DNA replication. 5-Fluorouracil inhibits thymidylate synthase, leading to impaired synthesis of thymidine—a nucleotide essential for DNA production. This combination is used in the treatment of various cancers including head and neck squamous cell carcinoma, colorectal cancer, gastric adenocarcinoma, and keratoacanthoma. The sequence of administration may influence efficacy in certain cancers[1][7][9].
- Brand names
- TrexallRheumatrexAdrucil
- Other names
- MTX + 5-FUmethotrexate and 5-fluorouracil
02
Targets
DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)
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