Drug intelligence / Profile preview

liposomal irinotecan + raltitrexed + fruquintinib

Development stage
Unknown
Lead developer
The First Affiliated Hospital of USTC
Modality
Small Molecules, Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous, Oral
01

Overview

liposomal irinotecan + raltitrexed + fruquintinib is a combination chemotherapy and targeted therapy regimen being investigated for the treatment of advanced colorectal cancer. The regimen is primarily being developed by The First Affiliated Hospital of the University of Science and Technology of China. It consists of three active agents: liposomal irinotecan, a nanoparticle-encapsulated topoisomerase I inhibitor that induces DNA damage; raltitrexed, a quinazoline folate analogue that acts as a potent and specific inhibitor of thymidylate synthase, thereby disrupting DNA synthesis; and fruquintinib, a highly selective small-molecule inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3, which blocks tumor angiogenesis. This triplet combination is designed to provide a multi-pronged attack on tumor cells by simultaneously inhibiting DNA replication and the formation of new blood vessels, particularly in patients who have progressed on standard therapies.

Other names
Fruquintinib plus Liposomal Irinotecan and Raltitrexed
02

Targets

TOP1 (DNA Topoisomerase I)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)

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