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RK-163 is a synthetic alpha-galactosylceramide (α-GalCer) analog developed as a potent activator of natural killer T (NKT) cells. It functions as a ligand for the CD1d molecule expressed on antigen-presenting cells, such as dendritic cells. Once loaded onto CD1d, the RK-163/CD1d complex is recognized by the semi-invariant T-cell receptor (TCR) of NKT cells, leading to their activation, proliferation, and the secretion of Th1-type cytokines like interferon-gamma (IFN-γ). To overcome challenges such as low NKT cell frequency and off-target immunosuppression, RK-163 has been formulated into size-modulated glycoliposomes (approximately 100 nm) designed to optimize lymphatic delivery and dendritic cell uptake. This approach has demonstrated significant antitumor efficacy and improved survival in preclinical models of triple-negative breast cancer (TNBC).
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