Drug intelligence / Profile preview

floxuridine + fluorouracil + leucovorin + oxaliplatin

Development stage
Phase 3
Lead developer
Roche
Modality
DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous, Intra-arterial
01

Overview

This is a combination chemotherapy regimen consisting of four agents: - **Floxuridine** and **fluorouracil** are antimetabolite chemotherapeutic agents that inhibit thymidylate synthase, disrupting DNA synthesis and repair. - **Leucovorin** (folinic acid) enhances the binding of fluorouracil to thymidylate synthase, increasing its cytotoxicity. - **Oxaliplatin** is a platinum-based chemotherapeutic that forms DNA crosslinks, inhibiting DNA replication and transcription. This combination targets rapidly dividing cancer cells through multiple mechanisms affecting nucleotide synthesis and DNA integrity. While the FOLFOX regimen (fluorouracil, leucovorin, oxaliplatin) is standard for colorectal cancer[6][8][10], the addition of floxuridine is less common but may be used in specific investigational or off-label settings. The primary indication for similar regimens is colorectal cancer.

02

Targets

DNATS (Thymidylate synthase)

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