[111In]In-DTPA-trastuzumab biodistribution in organs at different time points and under different conditions. 20 kBq of the radioligands (corresponding to 0.05 μg radiolabelled antibody completed with 49.95 μg of cold antibody) was injected in mice bearing SK-OV-3 tumours (HER2-positive) or MDA-MB-231 tumours (HER2-negative). Specificity of [111In]In-DTPA-trastuzumab for SK-OV-3 tumors was tested by injection of cold DTPA-trastuzumab in excess. The results are expressed as a percentage of injected activity per gram of organs ± standard deviation (n = 3).
| Organ | SK-OV-3 [%IA per g] (HER2 positive) | MDA-MB-231 [%IA per g] (HER2 negative) | |||
|---|---|---|---|---|---|
| 2 h | 72 h | 144 h | Blocking (72 h) | 72 h | |
| Tumor | 7.16 ± 2.1 | 39.9 ± 15.4 | 30.3 ± 6.7 | 11.9 ± 2.4 | 20.7 ± 7.7 |
| Liver | 8.4 ± 2.0 | 5.0 ± 0.7 | 2.5 ± 0.1 | 4.9 ± 2.8 | 18.0 ± 8.5 |
| Kidney | 11.6 ± 2.2 | 7.1 ± 0.7 | 2.8 ± 0.7 | 4.4 ± 1.1 | 11.0 ± 4.6 |
| Adrenal glands | 14.0 ± 3.9 | 7.3 ± 1.8 | 5.0 ± 0.7 | 6.5 ± 1.5 | 12.5 ± 3.6 |
| Lungs | 19.3 ± 9.5 | 12.0 ± 1.0 | 4.0 ± 1.2 | 6.6 ± 1.9 | 14.6 ± 3.1 |
| Spleen | 8.1 ± 2.3 | 6.2 ± 0.8 | 2.7 ± 1.0 | 5.0 ± 2.3 | 15.2 ± 6.5 |
| Heart | 9.7 ± 0.9 | 5.8 ± 0.7 | 2.6 ± 0.7 | 3.7 ± 1.2 | 8.59 ± 4.3 |
| Muscle | 1.8 ± 0.2 | 2.0 ± 0.3 | 1.0 ± 0.2 | 1.3 ± 0.4 | 2.8 ± 0.6 |
| Bone | 3.7 ± 0.5 | 3.1 ± 0.3 | 1.5 ± 0.3 | 1.8 ± 0.5 | 5.0 ± 2.7 |
| Skin | 3.5 ± 0.6 | 5.2 ± 0.8 | 2.4 ± 0.7 | 3.4 ± 1.1 | 12.9 ± 2.3 |
| Stomach | 1.4 ± 0.5 | 1.3 ± 0.3 | 0.7 ± 0.2 | 0.8 ± 0.1 | 1.8 ± 0.0 |
| Small intestine | 4.6 ± 1.0 | 1.9 ± 0.2 | 0.9 ± 0.2 | 1.3 ± 0.4 | 5.4 ± 0.3 |
| Large intestine | 4.3 ± 1.1 | 1.4 ± 0.1 | 0.7 ± 0.1 | 1.6 ± 0.6 | 5.6 ± 1.8 |
| Pancreas | 3.8 ± 1.8 | 2.7 ± 0.6 | 1.1 ± 0.0 | 1.5 ± 0.5 | 6.0 ± 0.4 |
| Uterus | 5.2 ± 2.2 | 7.0 ± 3.3 | 2.1 ± 0.9 | 2.8 ± 1.1 | 15.3 ± 1.8 |
| Blood | 36.56 ± 5.4 | 18.7 ± 2.3 | 7.7 ± 2.6 | 9.4 ± 1.9 | 27.2 ± 8 |