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floxuridine + leucovorin
- 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, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Intrahepatic, Intravenous, Intra-arterial
01
Overview
Floxuridine + leucovorin is a combination of two small molecule chemotherapeutic agents used primarily in the treatment of metastatic colorectal cancer and hepatic metastases. Floxuridine (FUDR) is a pyrimidine analog that acts as an antimetabolite by inhibiting thymidylate synthase after conversion to 5-fluorouracil in vivo, thereby disrupting DNA synthesis and cell division. Leucovorin (folinic acid) enhances the cytotoxic effects of fluoropyrimidines like floxuridine by stabilizing the binding of their active metabolites to thymidylate synthase. This combination has been studied for continuous intrahepatic infusion or intravenous administration in patients with liver metastases from colorectal carcinoma and other advanced cancers[1][2]. The regimen aims to increase tumor response rates compared to monotherapy but may also increase toxicity such as sclerosing cholangitis or gastrointestinal side effects[1][2].
- Other names
- 2-deoxy-5-fluorouridine + folinic acidFUDR + LV
02
Targets
TS (Thymidylate synthase)
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