αvβ3-DTX-PD

αvβ3-DTX-PD is a preclinical integrin αvβ3-targeted nanotherapy consisting of phospholipid/polysorbate-80 micelle nanoparticles (~12.5 nm) functionalized with an integrin αvβ3-targeting peptidomimetic ligand (a quinolone nonpeptide) and loaded with a lipase-labile Sn2 phosphatidylcholine prodrug of docetaxel (DTX-PD). Developed by researchers at Washington University School of Medicine, the University of Illinois, and Kereos, the nanotherapy is designed to selectively target activated integrin αvβ3, which is highly expressed on neo-angiogenic blood vessels, tumor-promoting macrophages, osteoclasts, and aggressive breast cancer cells. Upon binding to target cells, the micelle delivers the docetaxel prodrug via contact-facilitated drug delivery (membrane hemifusion), where intracellular phospholipases enzymatically cleave the Sn2 ester bond to release active docetaxel. In preclinical models, αvβ3-DTX-PD has demonstrated significant efficacy in reducing tumor burden and osteolytic bone destruction in breast cancer bone metastases with reduced systemic hepatotoxicity compared to free docetaxel.

Other names

integrin αvβ3-targeted lipase-labile docetaxel-prodrug micellesαvβ3-DTX-PD micellesαvβ3-Dxtl-PD NPαvβ3-Dxtl-PD nanoparticleαvβ3-MP/DTX-PD