Synthesis and preclinical evaluation of DOTAGA-conjugated PSMA ligands for functional imaging and endoradiotherapy of prostate cancer

EJNMMI Research

Table 2 Internalization of radiometalated ligands in percentage of external reference ([¹²⁵I]I-BA)KuE

Ligand		Internalization(1 h)in%of([¹²⁵I]I-BA)KuE
[⁶⁸Ga]HBED-CC-Ahx-KuE		91.1 ± 1.7
[⁶⁸Ga]DOTA-FFK(Sub-KuE)	(⁶⁸Ga-10)	14.6 ± 0.8
[¹⁷⁷Lu]DOTA-FFK(Sub-KuE)	(¹⁷⁷Lu-10)	19.3 ± 0.9
[⁶⁸Ga]DOTAGA-FFK(Sub-KuE)	(⁶⁸Ga-11)	28.4 ± 0.7
[¹⁷⁷Lu]DOTAGA-FFK(Sub-KuE)	(¹⁷⁷Lu-11)	36.1 ± 1.1
[⁶⁸Ga]DOTAGA-ffk(Sub-KuE)	(⁶⁸Ga-12)	42.5 ± 1.7
[¹⁷⁷Lu]DOTAGA-ffk(Sub-KuE)	(¹⁷⁷Lu-12)	44.4 ± 1.8

Data is corrected for unspecific binding, c = 0.2 nM for ⁶⁸Ga, c = 0.5 nM for ¹⁷⁷Lu compounds, 37°C, 1 h, 125,000 cells/well, PLL-coated plates.