copper-64 ATSM

Copper-64 ATSM (copper Cu 64-ATSM) is a first-in-class, hypoxia-targeting theranostic radiopharmaceutical. It consists of the lipophilic diacetyl-bis(N4-methylthiosemicarbazone) (ATSM) chelator radiolabeled with the positron-, beta-, and Auger electron-emitting copper-64 isotope. Due to its high membrane permeability and redox potential, copper-64 ATSM rapidly diffuses into cells and is selectively reduced from Cu(II) to Cu(I) under hypoxic conditions, leading to its intracellular trapping. This selective accumulation allows for both high-contrast positron emission tomography (PET) imaging of tumor hypoxia and targeted radionuclide therapy, where the emitted beta particles and high-linear energy transfer (LET) Auger electrons induce lethal DNA damage in hypoxic, treatment-resistant cancer cells. Originally developed by the National Institutes for Quantum Sciences and Technology (QST) and currently being developed by LinqMed in partnership with PDRadiopharma, copper-64 ATSM is undergoing Phase III clinical evaluation for the treatment of recurrent malignant glioma, and has been investigated in Phase II trials for cervical and rectal cancers.

Other names

64Cu-ATSMCu-64 ATSMCu64 ATSMCu 64 ATSM[64Cu]Cu-ATSM[64Cu][Cu(ATSM)]copper Cu 64-ATSMcopper-64 diacetyl-bis(N4-methylthiosemicarbazone)copper-64-diacetyl-bis(N4-methylthiosemicarbazone)