Recent Advances in 64Cu/67Cu-Based Radiopharmaceuticals

Abstract

Copper-64 (T1/2 = 12.7 h) is a positron and beta-emitting isotope, with decay characteristics suitable for both positron emission tomography (PET) imaging and radiotherapy of cancer. Copper-67 (T1/2 = 61.8 h) is a beta and gamma emitter, appropriate for radiotherapy β-energy and with a half-life suitable for single-photon emission computed tomography (SPECT) imaging. The chemical identities of 64Cu and 67Cu isotopes allow for convenient use of the same chelating molecules for sequential PET imaging and radiotherapy. A recent breakthrough in 67Cu production opened previously unavailable opportunities for a reliable source of 67Cu with high specific activity and purity. These new opportunities have reignited interest in the use of copper-containing radiopharmaceuticals for the therapy, diagnosis, and theranostics of various diseases. Herein, we summarize recent (2018–2023) advances in the use of copper-based radiopharmaceuticals for PET, SPECT imaging, radiotherapy, and radioimmunotherapy.

PYTA: a universal chelator for advancing the theranostic palette of nuclear medicine

“…DOTA plays a central role in theranostics as the bifunctional chelator in several clinically approved gallium-68 ( 68 Ga) and 177 Lu radiopharmaceuticals for PET imaging and targeted β − therapy of cancer, respectively. 22–25 Targeted constructs comprising DOTA are also being investigated in clinical trials for use with copper-64 ( 64 Cu) for PET 26,27 and with 225 Ac and other α emitters for targeted α therapy (TAT). 28,29…”