Drug intelligence / Profile preview

capecitabine + fluorouracil + leucovorin + oxaliplatin

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a four-drug chemotherapy combination regimen consisting of capecitabine, fluorouracil (5-FU), leucovorin (folinic acid), and oxaliplatin. Each component has a distinct mechanism of action but all are antineoplastic agents primarily used in the treatment of gastrointestinal cancers, especially colorectal cancer. - **Capecitabine** is an oral prodrug that is enzymatically converted to 5-fluorouracil in tumor tissues. It acts as an antimetabolite, interfering with DNA synthesis by inhibiting thymidylate synthase after conversion to 5-FU[8]. - **Fluorouracil (5-FU)** is a pyrimidine analog that inhibits thymidylate synthase, disrupting DNA synthesis and function. - **Leucovorin** enhances the binding of 5-FU to thymidylate synthase, increasing its cytotoxicity. - **Oxaliplatin** is a platinum-based chemotherapeutic agent that forms crosslinks in DNA, leading to apoptosis. This combination regimen leverages multiple mechanisms targeting rapidly dividing cancer cells and is commonly used for adjuvant or first-line treatment of advanced or metastatic colorectal cancer. The inclusion of both capecitabine and 5-FU with leucovorin may be part of clinical trials or specific protocols aiming for enhanced efficacy through dual fluoropyrimidine exposure; however, standard regimens typically use either capecitabine *or* infusional/bolus 5-FU plus leucovorin with oxaliplatin[6].

Other names
FOLFOX6 (modified) + capecitabinemFOLFOX6/XELOX
02

Targets

DNATS (Thymidylate synthase)

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