Table 3.
Ex vivo biodistribution. Female Balb/c nu/nu mice with HER3-expressing BxPC-3 xenografts were injected with 2 µg [57Co]Co-(HE)3-ZHER3-X (X = NOTA, NODAGA, DOTA, DOTAGA).
| Organ | NOTA | NODAGA | DOTA | DOTAGA | ||||
|---|---|---|---|---|---|---|---|---|
| 3 h | 24 h | 3 h | 24 h | 3 h | 24 h | 3 h | 24 h | |
| Blood | 1.0 ± 0.1 a,b,c,* | 0.31 ± 0.04 a,b,c,* | 0.61 ± 0.09 a,d,* | 0.18 ± 0.02 a,* | 0.33 ± 0.04 b,d,f,* | 0.14 ±0.02 b,f,* | 0.52 ±0.04 c,f,* | 0.22 ±0.02 c,* |
| Salivary Gland | 0.9 ± 0.2 a,b | 0.6 ± 0.2 | 1.6 ± 0.4 a,e | 1 ± 1 | 1.5 ± 0.1 b,f,* | 0.9 ± 0.1 * | 0.64 ±0.09 e,f | 0.4 ±0.1 |
| Lung | 1.0 ± 0.1 a,b,* | 0.41 ± 0.07 * | 1.7 ± 0.3 a,e,* | 0.47 ± 0.04 * | 1.7 ± 0.2 b,f,* | 0.6 ± 0.2 e,* | 0.8 ± 0.1 e,f,* | 0.33 ± 0.04 e,* |
| Liver | 1.56 ± 0.52 a,b | 1.1 ± 0.2 | 3.3 ± 0.8 a,* | 1.4 ± 0.2 * | 3.7 ± 0.5 b,f,* | 1.6 ± 0.2 * | 2.4 ± 0.2 e,f,* | 1.5 ± 0.2 * |
| Spleen | 0.57 ± 0.04 c | 0.6 ± 0.2 | 0.47 ±0.09 e | 0.35 ±0.05 e | 0.43 ± 0.05 f | 0.42 ± 0.08 | 0.8 ± 0.1 c,e,f | 0.7 ± 0.1 e |
| Stomach | 0.78 ± 0.06 a,b,* | 0.35 ± 0.04 a,b,* | 1.5 ±0.5 a,e,* | 0.65 ± 0.06 a,e,* | 1.5 ± 0.3 b,f,* | 0.65 ± 0.05 b,f,* | 0.6 ± 0.1 e,f,* | 0.31 ± 0.05 b,f,* |
| Small intestine | 1.6 ±0.3 a,b,* | 0.7 ± 0.1 a,b,* | 4 ± 1 a,e,* | 1.6 ±0.3 a,e,* | 4.6 ± 0.8 b,f,* | 2.1 ± 0.04 b,f,* | 0.9 ± 0.2 e,f | 0.6 ± 0.10 e,f |
| Kidneys | 194 ± 17 * | 106 ± 67 a,b,* | 279 ± 84 | 213 ± 7 a | 253 ± 54 | 223 ± 23 b,f | 156 ± 27 c | 131 ±13 f |
| Tumor | 1.55 ± 0.26 a,b | 1.1 ± 0.3 b | 2.6 ± 0.6 a,e,* | 1.4 ± 0.4 d,* | 2.8 ± 0.4 b,f | 2.4 ± 0.4 b,d,f | 0.9 ± 0.2 e,f | 0.8 ± 0.1 f |
| Muscle | 0.19 ± 0.04 | 0.13 ± 0.04 | 0.20 ± 0.06 * | 0.09 ± 0.02 * | 0.19 ± 0.01 * | 0.09 ± 0.02 * | 0.16 ± 0.02 | 0.11 ± 0.03 |
| Bone | 0.3 ± 0.1 | 0.25 ± 0.05 | 0.3 ± 0.1 | 0.15 ±0.05 | 0.25 ± 0.06 | 0.20 ± 0.03 | 0.28 ± 0.09 | 0.19 ± 0.07 |
| GI (%ID) | 2.4 ± 0.5 a,b,* | 1.3 ± 0.2 * | 5.0 ± 0.4 a,* | 2.8 ± 0.7 * | 5.7 ± 0.9 b,f,* | 2.7 ± 0.7 * | 4.78 ± 0.9f | 1.13 ±0.2 |
| Body (%ID) | 5.9 ± 0.4 a,b | 3 ± 2 a,b | 10 ± 2 a,e,* | 4.5 ± 0.7 a,e,* | 9.0 ± 1.0 b,f,* | 4.9 ± 0.56 b,f,* | 2 ± 0.6 e,f,* | 3.1 ±0.3 e,f,* |
Data presented as % ID/g and average ± SD of n = 4 animals per group. Significant difference (p < 0.05) between a: NOTA vs. NODAGA, b: NOTA vs. DOTA, c: NOTA vs. DOTAGA, d: NODAGA vs. DOTA, e: NODAGA vs. DOTAGA, f: DOTA vs. DOTAGA. * Significant difference between 3 and 24 h.