Select Preclinical PRIT and Targeted Radiotherapy Studies with Emphasis on Dosimetry
| Vehicle | TRT type | RIT/PRIT radiocarrier | cGy/MBq to tumor | cGy/37 MBq to tumor | TI | Reference | ||
|---|---|---|---|---|---|---|---|---|
| Blood | Kidney | Liver | ||||||
| IgG | RIT | 131I-3F8 (131I-naxitamab) | 237.4 ± 40.4 | 8,784 ± 1,495 | 3 | 13 | 19 | (51) |
| F(ab′)2 | RIT | 131I-F6 F(ab′)2 | 184 | 6,800 | 5 | 10 | 17 | (157) |
| Peptide | PRRT | 177Lu-DOTATATE (Lutathera*) | 34 ± 0.4 | 1,258 ± 14.8 | ND | 3 | 46 | (158) |
| IgG–streptavidin | PRIT | 177Lu-biotin or 90Y-biotin | 177Lu: 62 | 177Lu: 2,294 | 177Lu: 9 | 177Lu: 2 | 177Lu: 9 | (103) |
| 90Y: 134 | 90Y: 4,958 | 90Y: 12 | 90Y: 4 | 90Y: 8 | ||||
| scFv–streptavidin | PRIT | 90Y-biotin | 153.1 ± 8.3 | 5,665 ± 307 | 170 | 3 | 21 | (51) |
| Antitumor F(ab′)2 × anti-HSG Fab | PRIT | 177Lu-IMP241 or 90Y-IMP241 | 177Lu: 151 | 177Lu: 5,587 | 177Lu: 45 | 177Lu: 9 | 177Lu: 35 | (84) |
| 90Y: 388 | 90Y: 14,356 | 90Y: 35 | 90Y: 8 | 90Y: 26 | ||||
| DNL | PRIT | 177Lu-IMP325 or 90Y-IMP325 | 177Lu: 72.8 | 177Lu: 2,695 | 177Lu: 169 | 177Lu: 7 | ND | (91) |
| 90Y: 135 | 90Y: 5,011 | 90Y: 158 | 90Y: 7 | |||||
| IEDDA click | PRIT | 177Lu-Tz | 556 | 20,572 | 11 | 21 | 26 | (140) |
| DOTA-PRIT | PRIT | 177Lu-DOTA | 85 | 3,145 | 142 | 23 | 40 | (120) |
| Affibody-PNA | PRIT | 177Lu-HP2 | 108 | 3,996 | 269 | 5 | 81 | (132) |
| SADA-PRIT | PRIT | 177Lu-DOTA | 320 | 11,840 | 109 | 25 | 32 | (127) |
* Advanced Accelerator Applications.
TRT = targeted radiotherapy; RIT = radioimmunotherapy; ND = not determined; IEDDA = inverse electron-demand Diels–Alder.
All therapies were given intravenously to immunocompromised mice bearing subcutaneous human cancer xenografts.