Melanoma affinity in mice and immunosuppressed sheep of [125I]N-(4-dipropylaminobutyl)-4-iodobenzamide, a new targeting agent

Abstract The increasing incidence of melanoma and the lack of effective therapy have prompted the development of new vectors, more specific to the pigmented tumor, for early detection and treatment. Targeted agents have to exhibit a rapid, high tumor uptake, long tumor retention and rapid clearance from nontarget organs. This joint work presents results obtained with a new melanoma targeting agent, [ 125 I]- N -(4-dipropylaminobutyl)-4-iodobenzamide or [ 125 I]BZ18. After labeling with a high specific activity, the biodistribution of the compound was investigated in two animal models, the mouse and the sheep. Melanotic tumor retention was observed lasting several days. We visualized the internalization of the agent inside the melanosomes by secondary ion mass spectroscopy imaging, we measured the affinity constants of [ 125 I]BZ18 on a synthetic melanin model and we demonstrated a radiotoxic effect of this labeled agent on B16F0 melanoma cell culture due to its cellular internalization. From this work, [ 125 I]BZ18 appeared a promising melanoma targeting agent in the nuclear medicine field.