TC-99M-LABELED LAMININ FRAGMENTS FOR CANCER IMAGING

目标是开发一种放射性药物，使用一种合成的 ~(99)T放射性标记的层粘连蛋白九肽用于检测和 上皮源性转移瘤细胞的定位。层压板 将使用九肽来靶向层粘连蛋白受体；层粘连蛋白受体 已知在人类癌症和人类结肠癌中表达增加 尤其是癌症。这种特定的示踪剂可用于动物和 人类肿瘤模型，允许对人类进行理性推断。在第一阶段， 层粘连蛋白九肽将以一步直接标记的方式形成 试剂盒及其标记的层粘连蛋白与肿瘤细胞的结合 以I-125标记层粘连蛋白为参照进行测量。生物分布 研究将在正常C57BL/6小鼠和C57BL/6小鼠身上进行 荷瘤大鼠B16黑色素瘤的肿瘤影像研究 人结肠癌细胞株LoVo的异种移植在第二阶段， 将进行更广泛的动物研究，产品配方和 确定制造方案，进行急性毒性研究， 如果可行，初步的人体研究。

The objective is development of a radiopharmaceutical, using a synthetic laminin nonapeptide radiolabeled with Tc-99m, for detection and localization of metastatic tumor cells of epithelial origin. The laminin nonapeptide will be used to target the laminin receptor; laminin receptors are known to have an increased expression in human cancers, and human colon cancer in particular. This specific tracer can be used in both animal and human tumor models, allowing rational extrapolation to humans. In Phase I, the laminin nonapeptide will be formulated in single-step, direct labeling kits, and the binding of the Tc-99m-labeled laminin to tumor cells measured, using I-125-labeled laminin as a reference. Biodistribution studies will be conducted in normal C57BL/6 mice and in C57BL/6 mice bearing B16 melanomas, with tumor imaging studies in athymic rats bearing xeno-grafts of the human colon carcinoma cell line LoVo. In Phase II, extended animal studies will be conducted, product formulation and manufacturing protocols determined, acute toxicity studies conducted and, if feasible, preliminary human studies.