Table 1.
Summary of properties of RITs
| RIT names | IC50 (ng/ml) in KLM 1 |
Half Max Mesothelin Binding |
Half Life (min) | AUC | Rh | ||
|---|---|---|---|---|---|---|---|
| without PEG | with PEG (% Activity) |
(μg/ml) | Fast (α) | Slow (β) | (arbitrary unit, x104) |
(nm) | |
| SS1P | 0.19 | n/a | nt | 19 | n/a | nt | nt |
| LMB-12 | 0.22 | n/a | 0.022 ± 0.001 | 11 | n/a | 0.2 | 3.4 |
| LMB-84 | 0.19 | n/a | nt | nt | n/a | nt | nt |
| LMB-249 | 0.22 ± 0.06 | 1.18 ± 0.03(18%) | 0.027 ± 0.001 | 144 | 74400 | 5.9 | 7.1 |
| LMB-203 | 0.29 ± 0.02 | 1.10 ± 0.19 (26%) | 0.024 ± 0.004 | 59 | 51600 | 5.1 | 6.9 |
| LMB-163 | 0.22 ± 0.03 | 1.13 ± 0.19 (19%) | 0.029 ± 0.006 | 29 | 62284 | 4.3 | 5.6 |
| LMB-179 | 0.21 ± 0.01 | 1.09 ± 0.13 (19%) | 0.023 ± 0.002 | 38 | 26600 | 3.9 | 5.9 |
| LMB-244 | 0.16 ± 0.03 | 0.25 ± 0.05 (64%) | 0.013 ± 0.001 | 25 | 256 | 2.2 | 5.2 |
nt: not tested; n/a: not applicable
Bolded numbers refer to PEGylated RITs