Preparation and preliminary studies of [64Cu]-antiMUC-1 for breast cancer targeting

MUC1-Targeted Radiopharmaceuticals in Cancer Imaging and Therapy

“…The radio-immunoconjugate displayed a high radiochemical efficiency, high in vitro stability, and a minimum loss of immunoreactivity. Compared to its high immunoreactivity toward MCF7 expressing MUC1 antigen, 64 Cu-DOTA-PR81 did not interact with CHO cell line as the control. The maximum internalized radioactivity was seen after a 4−8 h incubation that was reduced at 48 h. The authors explained the falloff in cell-related activity by a proteolytic degradation of the antibody in lysosomes, which results in a copper transchelatation of biomolecules containing internal copper such as superoxide dismutase (SOD).…”

“…For single photon-emission tomography (SPECT), γ-emitters with energies in the range from 100 to 250 keV are optimal and are mainly represented by 99m Tc, 123 I, and 111 In. High-energy positron-emitters such as 18 F, 68 Ga, 64 Cu, and 11 C can be used for positron-emission tomography (PET) by emitting 511 keV photons. 55−58 For therapeutic purposes, αor β-particles or low-energy electron emitters are ideal radioisotopes for the treatment of tumor cells.…”

“…60−62 Over the last decades, several anti-MUC1 mAbs have been reported for the radioimmunoscintigraphy (RIS) and radioimmunotherapy (RIT) of a variety of human malignancies. 48,63,64 Herein we have summarized the radiolabeled anti-MUC1 antibodies and their fragments used for the diagnosis and treatment of cancers.…”

“…PR81 is a murine IgG1 class containing light κ-chain produced against human MUC1 by immunizing mice with homogenized breast cancer tissues, and it has shown a high affinity toward human breast carcinoma. 65 The radiolabeling of PR81 and its fragments have been performed with many radioisotopes such as 99m Tc, 131 I, 64 Cu, and 177 Lu indicating the potential of this mAb for the RIS and RIT of MUC-1-positive cancers. 66−68 Using labeled PR81 for the imaging of breast tumors has been reported by Salouti et al in several studies.…”

“…The results from this study illustrated 177 Lu-DOTA-PR81 to be a potential agent for the therapy of human breast cancer. 67 In a more recent study published in 2015 by Alirezapour et al, 64 Cu-DOTA-PR81 was prepared and evaluated for an immuno-PET imaging of breast cancer. The radio-immunoconjugate displayed a high radiochemical efficiency, high in vitro stability, and a minimum loss of immunoreactivity.…”