In vitro and in vivo characterization of [Cu][Cu(elesclomol)] as a novel theranostic agent for hypoxic solid tumors.

Purpose: Hypoxic tumors are associated with therapy resistance and poor cancer prognosis, but methods to detect and counter tumor hypoxia remain insufficient. Our purpose was to investigate Cu(II)-elesclomol ([Cu][Cu(ES)]) as a novel theranostic agent for hypoxic tumors, by implementing an improved production method and assessing its therapeutic and diagnostic potential compared to the established Cu-64 radiopharmaceuticals [Cu]CuCl and [diacetyl-bis(N4-methylthiosemicarbazone) [Cu][Cu(ATSM)].

Methods: Cu-64 was produced using a biomedical cyclotron at 12 MeV with the reaction Ni(p,n)Cu, followed by synthesis of [Cu]CuCl, [Cu][Cu(ATSM)], and [Cu][Cu(ES)].