Drug intelligence / Profile preview

fruquintinib + trastuzumab + XELOX

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

Overview

This combination regimen consists of fruquintinib, trastuzumab, and the XELOX chemotherapy protocol (oxaliplatin and capecitabine). It is being investigated as a first-line treatment for patients with HER2-positive advanced gastric or gastroesophageal junction (GEJ) adenocarcinoma. Fruquintinib is a highly selective and potent oral tyrosine kinase inhibitor of VEGFR-1, -2, and -3, which inhibits tumor angiogenesis. Trastuzumab is a recombinant DNA-derived humanized monoclonal antibody that selectively binds to the extracellular domain of the human epidermal growth factor receptor 2 (HER2), inhibiting tumor cell proliferation. XELOX is a standard chemotherapy regimen where oxaliplatin acts as a DNA alkylating agent and capecitabine acts as a prodrug of 5-fluorouracil, inhibiting thymidylate synthase. The study is a Phase Ib/II trial sponsored by Henan Cancer Hospital to evaluate the safety and efficacy of this multi-targeted approach.

Brand names
XelodaEloxatin
Other names
fruquintinib + trastuzumab + oxaliplatin + capecitabinefruquintinib + trastuzumab + CapeOx
02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)TS (Thymidylate synthase)VEGFR2 (Vascular endothelial growth factor receptor 2)DNAVEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)

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