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Table 3 Representative studies evaluating 64Cu-labeled nanoparticles in preclinical cancer models

From: Radiolabeled nanomaterials for biomedical applications: radiopharmacy in the era of nanotechnology

64Cu-labeled NPs NPs/Chelate Experimental contitions t (min)/T(ºC)/pH Radiochemical yield (%) Evaluated applications References
[64Cu]Cu-DOX-anti-PD-1-Liposomes
[64Cu]Cu-PEG-Liposomes (MM-DX-929)
Liposomes/DOTA
Liposomes/4-DEAP-ATSC
2 h/43 °C/pH 6.5
1 min/25 °C/pH 6
62%
 > 90%
PET imaging of PD-1-overexpressing breast tumors. In vitro and in vivo results of enhanced chemotherapy effects
PET imaging of breast tumors
Du et al. 2017)
Lee et al. 2018)
[64Cu]Cu-AGuIX
[64Cu]Cu-IR783 –AguIX
AGuIX/DOTA
AGuIX/NODAGA
1 h/37 °C/pH 5.5
45 min/37 °C/pH 5.5
 > 98%
PET imaging of liver cancer. Positive in vivo results of radionuclide therapy with AGuIX after irradiation using an X-ray source
PET/MRI/ optical imaging of TSA tumors
Hu et al. 2017)
Thakare et al. 2019)
[64Cu]Cu-DOX-PEG-LNP
[64Cu]Cu- cys-DB- PEG-LNP
[64Cu]Cu-anti-CEA- PEG-DBCO LND
LNP/DOTA
LND/DOTA
45 min/43 °C/pH 5.5
 > 75%
70%
PET imaging of prostate cancer. In vivo results of enhanced chemotherapy effects
PET imaging by targeting carcinoembryonic antigen (CEA) in breast cancer
Wong et al. 2017)
Wong et al. 2020)
[64Cu]Cu-PEG-Fe-GA-CPNs Fe-GA-CPNs/chelate-free 60 min/37 °C/pH 5.5 75% PET imaging and photoacoustic tomography/MRI of breast cancer. In vitro and in vivo results of photothermal therapy Jin et al. 2017)
[64Cu]Cu-Macrin Macrin/NODAGA 30 min/90 °C/pH 6  > 99% PET and optical imaging of tumor-associated macrophages in lung carcinoma Kim et al. 2018)
[64Cu]Cu-SiGdNP SiGdNP/NODAGA 30 min/37 °C/pH 5.8 No reported PET/MRI dual imaging of metastatic mammary adenocarcinoma (TS/A) Tran et al. 2018)
[64Cu]Cu-PEG-dopamine-RGD-MnFe2O4 MnFe2O4/DOTA 40 min/50 °C/pH 6.5 65% PET/MRI dual imaging by targeting integrin α(v)β(3) in glioblastoma Shi and Shen 2018)
[64Cu]Cu-silicon
[64Cu]Cu-CQDs
Silicon and CQDs /NOTA 30 min/25 °C/pH 6  > 99% PET imaging of epidermoid carcinoma Licciardello et al. 2018)
[64Cu]CuS-PEG-RGD
[64Cu]CuS-PEG-bombesin
[64Cu]CuS-PEG
CuS/chelate-free
CuS/chelate-free
CuS/chelate-free
15 min/95 °C
15 min/65 °C/pH 9
15 min/95 °C
 > 98%
 > 98%
PET imaging by targeting integrin α(v)β(3) in glioblastoma. In vitro and in vivo results of photothermal therapy
PET imaging by GRPr in prostate cancer
PET imaging of melanoma and ovarian cancer. In vitro and in vivo results of photothermal therapy combined with immunotherapy
Cui et al. 2018)
Cai et al. 2018)
Cao et al. 2020)
[64Cu]Cu-GE11-micelles Micelles/NOTA 15 min/37 °C/pH 5.5 23% PET imaging by targeting the epidermal growth factor receptor in colon cancer Paiva et al. 2020)
[64Cu]Cu-PEG- melanin Melanin/chelate-free 1 h/40 °C/pH 5.5 PET imaging of epidermoid carcinoma. In vivo results of radionuclide therapy Zhou et al. 2020)
[64Cu]Cu-UPS polymers UPS polymers/NOTA 15 min/37 °C/pH 6.5  > 95% PET imaging of small occult tumors in the brain, head, neck and breast of mice by targeting tumor-acidosis Huang et al. 2020)
[64Cu]Cu-PEG-PPa-Trp2 Trp2 peptide-coassembled NPs /chelate-free 30 min/25 °C  > 97% PET imaging of melanoma. In vivo results of dendritic cell-based immunotherapy He et al. 2021)