Drug intelligence / Profile preview

fruquintinib + tislelizumab + FOLFOX

Development stage
Phase 2
Lead developer
HUTCHMED
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination regimen consisting of fruquintinib, tislelizumab, and the FOLFOX chemotherapy protocol. Fruquintinib is an oral small molecule inhibitor targeting vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3, thereby inhibiting angiogenesis in tumors. Tislelizumab is a humanized IgG4 monoclonal antibody that acts as an immune checkpoint inhibitor by binding to programmed death-1 (PD-1) receptor on T cells, blocking its interaction with PD-L1/PD-L2 and enhancing anti-tumor immune responses. FOLFOX is a standard chemotherapy regimen composed of folinic acid (leucovorin), fluorouracil (5-FU), and oxaliplatin; it works by interfering with DNA synthesis and function in rapidly dividing cancer cells[1][2][4]. This combination aims to leverage antiangiogenic therapy, immunotherapy, and cytotoxic chemotherapy for synergistic effects against cancers such as colorectal cancer.

02

Targets

FGFR1 (Fibroblast growth factor receptor 1)PDCD1 (Programmed cell death protein 1 receptor)RET (Rearranged during transfection receptor tyrosine kinase)TS (Thymidylate synthase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)Pt-DNA adduct (DNA-oxaliplatin adduct)DHFR (Dihydrofolate reductase)

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