Drug intelligence / Profile preview

fluorodeoxyuridine + fluorouracil + leucovorin

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, Intra-arterial, Intrahepatic
01

Overview

This is a combination chemotherapy regimen consisting of three agents: fluorodeoxyuridine (FUDR), fluorouracil (5-FU), and leucovorin. Both FUDR and 5-FU are antimetabolite chemotherapeutic agents that act as pyrimidine analogs, inhibiting DNA synthesis by targeting thymidylate synthase, thereby blocking the production of thymidine required for DNA replication. Leucovorin (folinic acid) is not itself cytotoxic but enhances the binding of FUDR or 5-FU metabolites to thymidylate synthase, increasing their antitumor efficacy. This combination has been studied primarily in metastatic colorectal cancer, particularly for patients with liver metastases or after failure of other regimens. The regimen may involve sequential administration—such as intrahepatic FUDR followed by systemic 5-FU plus leucovorin—to maximize tumor control[1][2][5]. The main toxicities include gastrointestinal side effects like diarrhea and stomatitis; hematologic toxicity is generally less pronounced[1].

Brand names
Adrucil (fluorouracil)FUDR (floxuridine)
Other names
floxuridine + 5-FU + leucovorinFUDR + 5-FU + LV
02

Targets

TS (Thymidylate synthase)DNA

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