Drug intelligence / Profile preview

lipo-sunitinib

Development stage
Preclinical
Lead developer
Pfizer
Modality
Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems, Small Molecules
Administration
Intravenous
01

Overview

Lipo-sunitinib is a novel nanotherapeutic formulation consisting of the multi-targeted tyrosine kinase inhibitor sunitinib encapsulated within PEGylated liposomes. Developed by researchers at institutions including National Yang Ming Chiao Tung University, this formulation is designed to improve the therapeutic index of sunitinib by utilizing the enhanced permeability and retention (EPR) effect for passive tumor targeting. By encapsulating sunitinib in a PEGylated nanocarrier, the drug's half-life is prolonged and its accumulation in tumor tissue is increased, which aims to reduce the systemic toxicities (such as liver, heart, and kidney damage) associated with conventional sunitinib treatment. Preclinical studies in renal cell carcinoma (RCC) models have demonstrated that lipo-sunitinib not only inhibits tumor growth and angiogenesis but also modulates the tumor immune microenvironment by increasing the infiltration of activated effector T cells and type 1 dendritic cells while inhibiting immune suppressors.

Other names
liposome encapsulated sunitinibPEGylated liposome encapsulated sunitinib
02

Targets

KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)PDGFRB (Platelet-derived growth factor receptor beta)CSF1R (Macrophage colony-stimulating factor receptor)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)PDGFRA (Platelet-derived growth factor receptor alpha)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)

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