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Table 1 Inhibition constants (Ki in nM) and internalization values (%IA = % internalized activity) of [nat/68Ga]Ga-PSMA-11, [nat/68Ga]Ga-, [nat/44Sc]Sc-, [nat/177Lu]Lu-DOTA-PSMA-617 and [nat/68Ga]Ga-, [nat/44Sc]Sc-, [nat/177Lu]Lu-AAZTA5-PSMA-617

From: 68Ga, 44Sc and 177Lu-labeled AAZTA5-PSMA-617: synthesis, radiolabeling, stability and cell binding compared to DOTA-PSMA-617 analogues

derivative Ki ± SD
/ nM
  Internalization ± SD
/ %IA/106 cells
 
[nat/68Ga]Ga-PSMA-11 12.0 ± 2.8 (Eder et al. 2012a) 9.5 ± 2.6 (Benešová et al. 2015)
[nat/68Ga]Ga-PSMA-617 6.4 ± 1.0 (Benešová et al. 2015) 17.7 ± 4.4 (Benešová et al. 2015)
[nat/68Ga]Ga-AAZTA5-PSMA 8.7 ± 0.9   13.0 ± 0.2  
[nat/44Sc]Sc-PSMA-617 4.7 ± 0.8 (Eppard et al. 2017) 15.8 ± 2.1 (Eppard et al. 2017)
[nat/44Sc]Sc-AAZTA5-PSMA 30.6 ± 11.5   20.0 ± 0.9  
[nat/177Lu]Lu-PSMA-617 6.9 ± 1.3 (Benešová et al. 2015) 17.5 ± 3.1 (Benešová et al. 2015)
[nat/177Lu]Lu-AAZTA5-PSMA 26.6 ± 11.1   18.0 ± 2.0