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 prolyl endopeptidase FAP； 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靶向組織之釷複合物之方法，該方法包含： a) 形成八齒螯合劑，其包含在N位經甲基取代之四個羥基吡啶酮(HOPO)部分及以羧酸基終端之偶合部分； b) 將該八齒螯合劑偶合至至少一種靶向脯胺醯基內肽酶FAP之靶向組織之部分；及 c) 使該靶向組織之螯合劑與包含至少一種發射α釷同位素之離子之水溶液接觸。 本發明亦提供一種治療贅生性或增生性疾病之方法，該方法包含投與此靶向組織之釷複合物，且亦提供該複合物及對應醫藥調配物。
