Table 1.
In vitro data of the 4-(p-iodophenyl)butyrate-containing radioconjugates [225Ac]Ac-mcp-M-alb-PSMA and [225Ac]Ac-mcp-D-alb-PSMA in comparison to [225Ac]Ac-mcp-M-PSMA and [225Ac]Ac-mcp-D-PSMA without albumin-binding entities.
| Radio-conjugate | KD [HSA] (µM) | KD [PSMA] (nM) | Bmax (pmol/mg of protein) | EC50 (kBq/mL) for 1 h treatment |
|---|---|---|---|---|
| [225Ac]Ac-mcp-M-PSMA | 330 (240 to 460)* | 30.83 (16.44 to 56.72)# | 0.15 (0.12 to 0.19)# | 2.037 (1.323 to 3.130)# |
| [225Ac]Ac-mcp-D-PSMA | 150 (100 to 210)* | 10.20 (9.52 to 10.94)# | 1.55 (1.52 to 1.58)# | 0.1011 (0.0668 to 0.1530)# |
| [225Ac]Ac-mcp-M-alb-PSMA | 27 (19 to 37)* | 23.38 (18.97 to 28.72)# | 0.46 (0.43 to 0.49)# | 0.5233 (0.4010 to 0.6767)# |
| [225Ac]Ac-mcp-D-alb-PSMA | 15 (10 to 22)* | 11.56 (10.20 to 13.08)# | 1.96 (1.89 to 2.04)# | 0.0519 (0.0353 to 0.0753)# |
One experiment which was performed in triplicate. #95% confidence interval. *68.3% confidence interval.