Drug intelligence / Profile preview

5-fluorouracil + methotrexate + mitomycin

Development stage
Unknown
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Intravesical
01

Overview

This is a combination chemotherapy regimen consisting of three antineoplastic agents—5-fluorouracil, methotrexate, and mitomycin. The regimen is used primarily for the treatment of advanced cancers, including colorectal cancer and non-small-cell lung cancer. Each component has a distinct mechanism of action: - **5-fluorouracil** is a pyrimidine analog that inhibits thymidylate synthase, disrupting DNA synthesis in rapidly dividing cells. - **Methotrexate** is an antifolate that inhibits dihydrofolate reductase, blocking DNA synthesis and cell replication. - **Mitomycin** (commonly as mitomycin C) acts as an alkylating agent causing cross-linking of DNA strands. The combination exploits schedule-specific biochemical modulation to enhance efficacy while maintaining tolerability. In clinical studies, this regimen has demonstrated significant activity with manageable toxicity in advanced colorectal cancer and has also been evaluated in other solid tumors[1][2][6].

02

Targets

DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)DNA

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