Drug intelligence / Profile preview

fluorouracil + oxaliplatin + raltitrexed

Development stage
Unknown
Lead developer
Roche
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
01

Overview

This is a combination chemotherapy regimen consisting of three cytotoxic agents—fluorouracil (5-FU), oxaliplatin, and raltitrexed. Each drug has a distinct mechanism of action targeting DNA synthesis or function, leading to inhibition of cancer cell proliferation. Fluorouracil is a pyrimidine analog that inhibits thymidylate synthase, disrupting DNA synthesis. Oxaliplatin is a platinum-based compound that forms DNA crosslinks and induces apoptosis in rapidly dividing cells. Raltitrexed is a folate analog that also inhibits thymidylate synthase but via direct competition with the natural substrate, further impairing DNA replication and repair. This combination has been studied primarily for the treatment of advanced or metastatic colorectal cancer, especially in patients who are intolerant to standard 5-FU/leucovorin regimens or have specific clinical needs such as dihydropyrimidine dehydrogenase (DPD) deficiency[1][2]. The regimen may be considered in other gastrointestinal cancers based on clinical context.

Other names
5-fluorouracil + oxaliplatin + raltitrexed
02

Targets

TS (Thymidylate synthase)DNA

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