Drug intelligence / Profile preview

epirubicin + fluorouracil + methotrexate

Development stage
Unknown
Lead developer
Pfizer
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, Covalent Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

This is a combination chemotherapy regimen consisting of three cytotoxic agents—epirubicin, fluorouracil (5-fluorouracil or 5-FU), and methotrexate. Each drug has a distinct mechanism of action targeting rapidly dividing cancer cells. Epirubicin is an anthracycline antibiotic that inhibits topoisomerase II, leading to DNA strand breaks and inhibition of DNA replication. Fluorouracil is an antimetabolite that interferes with thymidylate synthase, disrupting DNA synthesis and repair. Methotrexate is also an antimetabolite that inhibits dihydrofolate reductase, blocking the synthesis of tetrahydrofolate required for purine and thymidylate production in DNA synthesis. This combination has been studied as sequential or concurrent therapy in various cancers, including advanced extrahepatic biliary system cancers and breast cancer[1][2]. The regimen aims to maximize anti-tumor efficacy by attacking cancer cells through multiple pathways.

02

Targets

TOP2A (DNA topoisomerase II)DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)

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