Drug intelligence / Profile preview

oxaliplatin + irinotecan + leucovorin + fluorouracil

Development stage
Unknown
Lead developer
Sanofi
Modality
Small Molecules
Administration
Intravenous
01

Overview

This is a combination chemotherapy regimen used primarily in the treatment of advanced or metastatic colorectal cancer. The regimen combines four agents with distinct mechanisms of action to maximize anticancer effects. Oxaliplatin is a platinum-based agent that forms DNA adducts, inhibiting DNA replication and transcription. Irinotecan is a topoisomerase I inhibitor that causes DNA damage during replication. Leucovorin (folinic acid) enhances the activity of fluorouracil by stabilizing its binding to thymidylate synthase, thereby increasing inhibition of DNA synthesis. Fluorouracil (5-FU) itself is an antimetabolite that interferes with thymidylate synthase and RNA processing[6][9]. This combination has been explored in clinical trials for patients with gastrointestinal cancers who have failed prior 5-FU-based therapy[6].

Other names
oxaliplatin/irinotecan/leucovorin/fluorouraciloxaliplatin, irinotecan, leucovorin, and fluorouracil
02

Targets

TOP1 (DNA Topoisomerase I)DNATS (Thymidylate synthase)

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