Drug intelligence / Profile preview

fruquintinib + fluorouracil + irinotecan + leucovorin + oxaliplatin

Development stage
Phase 2
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral, Intra-arterial
01

Overview

FOLFOXIRI-based HAIC + fruquintinib is an investigational combination regimen being evaluated for the treatment of unresectable colorectal cancer liver metastases (CRLM). The regimen consists of the FOLFOXIRI chemotherapy backbone—comprising fluorouracil (5-FU), leucovorin, oxaliplatin, and irinotecan—administered via hepatic arterial infusion chemotherapy (HAIC), combined with oral fruquintinib. HAIC allows for the delivery of high concentrations of cytotoxic agents directly into the hepatic artery supplying liver tumors, minimizing systemic toxicity while maximizing local efficacy. Fruquintinib is a highly selective and potent oral small-molecule inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3, which inhibits tumor angiogenesis. This combination aims to provide synergistic anti-tumor activity by combining targeted anti-angiogenic therapy with intensive regional chemotherapy in heavily pre-treated patients.

Other names
FOLFOXIRI-based HAIC + fruquintinibFOLFOXIRI-based Hepatic Arterial Infusion Combined With FruquintinibFOLFOXIRI-based HAIC Combined With Fruquintinib
02

Targets

DNATS (Thymidylate synthase)TOP1 (DNA Topoisomerase I)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)

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