64Cu-DOTHA2-PSMA

64Cu-DOTHA2-PSMA is an experimental theranostic radiopharmaceutical developed for the imaging and treatment of prostate cancer. It consists of a small-molecule ligand that binds with high affinity to the prostate-specific membrane antigen (PSMA), also known as glutamate carboxypeptidase II, which is frequently overexpressed in prostate adenocarcinoma. The ligand is conjugated to the chelator DOTHA2, which securely holds the radionuclide copper-64 (64Cu). Copper-64 is a unique isotope that decays via positron emission, allowing for high-resolution PET imaging, as well as beta-minus and Auger electron emission, which provides a therapeutic effect by inducing localized DNA damage in tumor cells. Preclinical data suggests that 64Cu-DOTHA2-PSMA exhibits prolonged tumoral retention and efficacy comparable to or exceeding that of 177Lu-PSMA-617, with a manageable safety profile, although dosimetry studies indicate significant radiation exposure to the liver and gastrointestinal tract.

Other names

copper-64-DOTHA2-PSMAcopper64-DOTHA2-PSMAcopper 64-DOTHA2-PSMA64Cu-DOTHA2-Glu-urea-Lys