Drug intelligence / Profile preview

5-fluorouracil + floxuridine

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, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous, Hepatic Arterial Infusion
01

Overview

This is a combination chemotherapy regimen consisting of 5-fluorouracil (5-FU) and floxuridine (FUdR), both of which are antimetabolite agents classified as pyrimidine analogs. The combination is typically administered via continuous infusion, either intravenously or regionally (such as hepatic arterial infusion), for the treatment of advanced cancers—most notably gastrointestinal adenocarcinoma metastatic to the liver and colorectal cancer with liver metastases[1][2][4]. Both drugs interfere with DNA synthesis by inhibiting thymidylate synthase, thereby blocking the methylation of deoxyuridylic acid to thymidylic acid during DNA synthesis. Floxuridine is rapidly converted in vivo to 5-fluorouracil, so their mechanisms overlap but may provide additive or synergistic effects when used together[3]. This regimen has been studied in phase I/II trials for its safety and efficacy profile; dose-limiting toxicities include gastrointestinal side effects such as enteritis and stomatitis[1][2].

Brand names
FUDR (for floxuridine)Adrucil (for fluorouracil)
Other names
5-FU + FUdRfluorouracil + floxuridine
02

Targets

TS (Thymidylate synthase)

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