The invention provides a method for the formation of a tissue-targeting thorium complex, said method comprising； a) forming an octadentate chelator comprising four hydroxypyridinone (HOPO) moieties, substituted in the N-position with a methyl group, and a coupling moiety terminating in a carboxylic acid group； b) coupling said octadentate chelator to at least one tissue-targeting moiety targeting HER2； and c) contacting said tissue-targeting chelator with an aqueous solution comprising an ion of at least one alpha-emitting thorium isotope. A method of treatment of a neoplastic or hyperplastic disease comprising admistration of such a tissue-targeting thorium complex, as well as the complex and corresponding pharmaceutical formulations are also provided.本發明提供一種用於形成組織靶向性釷錯合物之方法，該方法包含： a) 形成八牙螯合劑，其包含其中N位置經甲基取代之四個羥基吡啶酮(HOPO)部分體及以羧酸基封端之偶合部分體； b) 將該八牙螯合劑偶合至靶向HER2之至少一個組織靶向性部分體；及 c) 使該組織靶向螯合劑與包含至少一種α-發射性釷同位素之離子的水性溶液接觸。 亦提供一種包括投與此類組織靶向性釷錯合物以治療贅生性或增生性疾病之方法，以及該錯合物及對應醫藥調配物。
