Table 2.
In vivo biodistribution summary of 68Ga labeled DOTA conjugated click cyclized peptides.§ Animals were injected via tail vein with approximately 25 MBq of 68Ga labeled compound with specific activity >35 MBq nmole-1 and >98% radiochemical purity. Animals were sacrificed at 90 min post injection.
| DOTA-GG-ClickMTII | DOTA-GG-ClickMTII (blocked) | ClickMTII-GGK-DOTA | Free 68Ga3+ | |
|---|---|---|---|---|
| Tissue | %ID/gδ | %ID/g | %ID/g | %ID/g |
| Blood | 3.2±1.0 | 3.6±0.6 | 3.2±1.0 | 12.5±3.2 |
| Heart | 4.6±2.5 | 1.8±0.3 | 5.0±0.2 | 5.4±0.5 |
| Liver | 1.1±0.7 | 2.5±1.2 | 1.3±0.1 | 2.0±0.8 |
| Kidney | 4.7±0.9 | 11.7±2.1 | 5.4±0.1 | 5.0±0.6 |
| Brain | 2.3±1.1 | 0.4±0.1 | 1.3±0.0 | 0.6±0.0 |
| Muscle | 3.1±1.8 | 1.7±0.4 | 2.9±0.4 | 2.6±0.9 |
| Lung | 4.9±1.3 | 3.8±0.9 | 4.2±0.5 | 6.9±4.4 |
| Tumor | 16.0±5.7 | 5.0±0.9 | 10.2±1.3 | 11.0±2.2 |
| Tumor:Blood | 5.0±3.4 | 1.4±0.7 | 3.2±1.1 | 0.9±2.7 |
| Tumor:Kidney | 3.4±3.3 | 0.4±1.5 | 1.9±0.7 | 2.2±1.4 |
| Tumor:Liver | 14.0±3.2 | 2.0±1.0 | 7.9±0.7 | 5.4±1.5 |
| %ID | %ID | %ID | %ID | |
| Excretion | 78.8±8.6 | 61.7±9.0 | NDζ | 12.9±1.7 |
§
mean ± std. dev. (n = 3);
δ
%ID/g = percent injected dose per gram.
ζ
not determined.