Drug intelligence / Profile preview

capecitabine + floxuridine + gemcitabine

Development stage
Preclinical
Lead developer
Eli Lilly
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intra-arterial, Intravenous
01

Overview

This is a combination chemotherapy regimen consisting of three antimetabolite agents—capecitabine, floxuridine, and gemcitabine. Each drug is a nucleoside analog that interferes with DNA synthesis and function, leading to inhibition of cancer cell proliferation and induction of apoptosis. Capecitabine is an oral prodrug converted to 5-fluorouracil (5-FU) preferentially in tumor tissue; floxuridine is typically administered via hepatic arterial infusion for liver-directed therapy; gemcitabine is an intravenous cytidine analog used in various solid tumors. While combinations such as capecitabine plus gemcitabine or floxuridine plus gemcitabine have been studied for pancreatic cancer and intrahepatic cholangiocarcinoma, there are no widely recognized clinical regimens or brand names specifically for the triple combination of capecitabine + floxuridine + gemcitabine. The rationale for combining these drugs would be to exploit their synergistic effects on DNA synthesis inhibition while targeting different metabolic pathways within tumor cells[1][2][3][4][5].

02

Targets

POLA1 (DNA polymerase alpha)RRM1TS (Thymidylate synthase)

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