Drug intelligence / Profile preview

folinic acid + 5-fluorouracil + oxaliplatin + irinotecan

Development stage
Phase 3
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous
01

Overview

FOLFOXIRI is a chemotherapy combination regimen consisting of four drugs: folinic acid (also known as leucovorin or calcium folinate), 5-fluorouracil (5-FU), oxaliplatin, and irinotecan. It is primarily used for the treatment of advanced or metastatic colorectal cancer. The regimen works by combining three cytotoxic agents—fluorouracil, oxaliplatin, and irinotecan—which target rapidly dividing cancer cells through different mechanisms. Folinic acid enhances the effectiveness of 5-fluorouracil by stabilizing its binding to thymidylate synthase, thereby increasing cytotoxicity against tumor cells. Oxaliplatin is a platinum-based agent that causes DNA crosslinking and apoptosis; irinotecan inhibits topoisomerase I, leading to DNA damage; and 5-fluorouracil acts as an antimetabolite inhibiting thymidylate synthase and interfering with DNA synthesis. This combination has been shown in clinical trials to improve progression-free survival in patients with metastatic colorectal cancer compared to doublet regimens[2][3][7].

Brand names
FOLFOXIRI
Other names
FOLFOXIRIfluorouracil leucovorin oxaliplatin irinotecanfolinic acid fluorouracil oxaliplatin irinotecan
02

Targets

TOP1 (DNA Topoisomerase I)DNATS (Thymidylate synthase)

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