Drug intelligence / Profile preview

fruquintinib + gefitinib

Development stage
Phase 2
Lead developer
HUTCHMED
Modality
Small Molecules
Administration
Oral
01

Overview

Fruquintinib + gefitinib is an investigational oral combination therapy for advanced non-small cell lung cancer (NSCLC), particularly in patients with EGFR-sensitive mutations. Fruquintinib is a highly selective small-molecule inhibitor of vascular endothelial growth factor receptors (VEGFR-1, -2, and -3), targeting tumor angiogenesis. Gefitinib is a small-molecule inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, blocking downstream signaling that promotes malignant cell proliferation. The rationale for this combination is to simultaneously inhibit both EGFR and VEGF/VEGFR pathways, potentially overcoming resistance to EGFR-targeted therapies and improving efficacy. Clinical studies have shown promising anti-tumor activity and acceptable safety in first-line treatment of advanced NSCLC[1][2][7].

02

Targets

EGFR (Epidermal growth factor receptor)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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