GRI-0803 is a novel activator of human dNKT cells in development for the treatment of autoimmune disorders, with an initial focus on systemic lupus erythematosus (SLE). Activation of dNKT leads to a dendritic cell-mediated inhibition of iNKT cells. In our preclinical studies, dNKT activating molecules, GRI-0803 and GRI-0124, were observed to inhibit both murine and human iNKT cells. Oral administration of these dNKT activating molecules was observed to inhibit lupus nephritis and to significantly improve overall survival.