Table 3.
Biodistribution data over 48 h after injection of ibuprofen-derivatized PSMA radioligands in PC-3 PIP/flu tumor-bearing mice. The values are indicated as average ± SD obtained from each group of mice (n = 3-6) and listed as percentage of injected activity per gram tissue [% IA/g].
| 1 h p.i. | 4 h p.i. | 24 h p.i. | 48 h p.i. | |
|---|---|---|---|---|
| 177Lu-Ibu-PSMA | ||||
| Blood | 15 ± 2 | 6.0 ± 1.5 | 0.59 ± 0.11 | 0.50 ± 0.02 |
| Kidneys | 30 ± 4 | 33 ± 1 | 16 ± 3 | 11 ± 1 |
| Intestines | 2.4 ± 0.3 | 1.0 ± 0.3 | 0.21 ± 0.05 | 0.14 ± 0.01 |
| Liver | 5.9 ± 0.4 | 2.8 ± 0.5 | 0.95 ± 0.11 | 0.85 ± 0.06 |
| Salivary glands | 4.2 ± 0.4 | 1.7 ± 0.4 | 0.32 ± 0.07 | 0.26 ± 0.02 |
| Bone | 2.2 ± 0.3 | 1.0 ± 0.2 | 0.17 ± 0.05 | 0.13 ± 0.01 |
| PC-3 PIP Tumor | 49 ± 6 | 81 ± 7 | 77 ± 21 | 58 ± 4 |
| PC-3 flu Tumor | 4.4 ± 1.3 | 2.2 ± 0.6 | 0.60 ± 0.19 | 0.51 ± 0.15 |
| 177Lu-Ibu-Dα-PSMA | ||||
| 1 h p.i. | 4 h p.i. | 24 h p.i. | 48 h p.i. | |
| Blood | 18 ± 3 | 2.3 ± 0.8 | 0.33 ± 0.05 | 0.33 ± 0.13 |
| Kidneys | 73 ± 2 | 27 ± 4 | 18 ± 3 | 7.2 ± 1.2 |
| Intestines | 1.6 ± 0.4 | 0.49 ± 0.08 | 0.10 ± 0.02 | 0.07 ± 0.02 |
| Liver | 6.5 ± 0.1 | 0.84 ± 0.22 | 0.40 ± 0.05 | 0.28 ± 0.06 |
| Salivary glands | 4.6 ± 0.2 | 0.74 ± 0.20 | 0.19 ± 0.05 | 0.42 ± 0.55 |
| Bone | 2.0 ± 0.1 | 0.37 ± 0.10 | 0.10 ± 0.02 | 0.07 ± 0.01 |
| PC-3 PIP Tumor | 43 ± 5 | 49 ± 6 | 77 ± 15 | 49 ± 4 |
| PC-3 flu Tumor | 3.2 ± 0.4 | 1.0 ± 0.3 | 0.38 ± 0.03 | 0.20 ± 0.09 |
| 177Lu-Ibu-N-PSMA | ||||
| 1 h p.i. | 4 h p.i. | 24 h p.i. | 48 h p.i. | |
| Blood | 17 ± 3 | 3.6 ± 1.4 | 0.25 ± 0.07 | 0.25 ± 0.04 |
| Kidneys | 33 ± 4 | 27 ± 9 | 8.0 ± 1.1 | 6.8 ± 1.3 |
| Intestines | 1.9 ± 0.3 | 0.50 ± 0.18 | 0.09 ± 0.02 | 0.10 ± 0.04 |
| Liver | 3.6 ± 0.7 | 1.3 ± 0.6 | 0.32 ± 0.05 | 0.46 ± 0.05 |
| Salivary glands | 3.6 ± 0.5 | 0.94 ± 0.38 | 0.57 ± 0.35 | 0.10 ± 0.02 |
| Bone | 2.0 ± 0.4 | 0.56 ± 0.22 | 0.08 ± 0.02 | 0.07 ± 0.02 |
| PC-3 PIP Tumor | 52 ± 3 | 65 ± 16 | 58 ± 21 | 52 ± 8 |
| PC-3 flu Tumor | 2.9 ± 0.7 | 1.2 ± 0.6 | 0.23 ± 0.01 | 0.15 ± 0.03 |
| 177Lu-Ibu-DAB-PSMA | ||||
| 1 h p.i. | 4 h p.i. | 24 h p.i. | 48 h p.i. | |
| Blood | 13 ± 4 | 3.7 ± 0.5 | 0.16 ± 0.02 | 0.10 ± 0.04 |
| Kidneys | 30 ± 4 | 19 ± 2 | 6.0 ± 0.7 | 4.1 ± 0.9 |
| Intestines | 1.6 ± 0.5 | 0.71 ± 0.05 | 0.11 ± 0.03 | 0.05 ± 0.01 |
| Liver | 3.1 ± 1.0 | 1.5 ± 0.2 | 0.56 ± 0.10 | 0.49 ± 0.08 |
| Salivary glands | 3.2 ± 1.1 | 0.86 ± 0.38 | 0.56 ± 0.37 | 0.09 ± 0.03 |
| Bone | 1.6 ± 0.5 | 0.62 ± 0.08 | 0.09 ± 0.02 | 0.06 ± 0.01 |
| PC-3 PIP Tumor | 61 ± 10 | 66 ± 11 | 52 ± 3 | 36 ± 10 |
| PC-3 flu Tumor | 2.7 ± 0.7 | 1.2 ± 0.3 | 0.17 ± 0.01 | 0.15 ± 0.04 |