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.

中文翻译：

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黑色素瘤在小鼠和免疫抑制绵羊[（125）I] N-（4-二丙基氨基丁基）-4-碘代苯甲酰胺的一种新的靶向剂。

黑色素瘤的发病率不断增加，缺乏有效的治疗方法，已促使人们开发出更多针对色素沉着肿瘤的新载体，用于早期发现和治疗。靶向药物必须表现出快速，高肿瘤摄取，长肿瘤保留和快速从非靶器官清除的作用。这项共同的工作提出了使用新的黑色素瘤靶向剂[[（125）I] -N-（4-二丙基氨基丁基）-4-碘苯甲酰胺或[（125）I] BZ18获得的结果。用高比活性标记后，在小鼠和绵羊这两种动物模型中研究了该化合物的生物分布。观察到黑素瘤保留了几天。我们通过二次离子质谱成像可视化了黑素体内部试剂的内部化，我们测量了[（125）I] BZ18在合成黑色素模型上的亲和常数，并且由于其细胞内在化，我们证明了该标记试剂对B16F0黑色素瘤细胞培养物的放射毒性作用。通过这项工作，[（125）I] BZ18出现了核医学领域中有希望的黑素瘤靶向剂。