Table 2.
Pharmacokinetics of 111In-DOTA-GSG-J18 | |||||
---|---|---|---|---|---|
%ID/g | |||||
Tissues | 30 min | 1 h† | 1 h-block | 2 h‡ | 4 h |
Tumor | 1.63 ± 0.68 | 0.60 ± 0.32 | 0.31 ± 0.12* | 0.18 ± 0.03 | 0.10 ± 0.02 |
Blood | 2.37 ± 0.94 | 0.40 ± 0.24 | 0.23 ± 0.11 | 0.03 ± 0.03 | 0.19 ± 0.02 |
Heart | 0.67 ± 0.27 | 0.13 ± 0.08 | 0.07 ± 0.03 | 0.02 ± 0.01 | 0.05 ± 0.01 |
Lung | 2.42 ± 0.48 | 1.06 ± 0.82 | 0.83 ± 0.19 | 0.49 ± 0.36 | 0.62 ± 0.32 |
Liver | 1.42 ± 0.37 | 0.51 ± 0.48 | 0.37 ± 0.02 | 0.23 ± 0.11 | 0.84 ± 0.13 |
Spleen | 1.77 ± 0.46 | 0.68 ± 1.01 | 0.16 ± 0.03 | 0.19 ± 0.24 | 1.58 ± 0.36 |
Stomach | 0.36 ± 0.14 | 0.11 ± 0.04 | 0.08 ± 0.03 | 0.04 ± 0.02 | 0.04 ± 0.00 |
Large intestine | 0.34 ± 0.17 | 0.15 ± 0.05 | 0.07 ± 0.02 | 0.27 ± 0.06 | 0.28 ± 0.19 |
Small intestine | 0.63 ± 0.29 | 0.32 ± 0.11 | 0.15 ± 0.04 | 0.15 ± 0.08 | 0.06 ± 0.01 |
Intestines | 0.49 ± 0.22 | 0.25 ± 0.08 | 0.12 ± 0.03 | 0.20 ± 0.07 | 0.15 ± 0.08 |
Kidneys | 6.71 ± 3.08 | 2.70 ± 0.95 | 1.98 ± 0.29 | 1.67 ± 0.43 | 1.75 ± 0.17 |
Brain | 0.09 ± 0.03 | 0.03 ± 0.01 | 0.02 ± 0.00 | 0.01 ± 0.00 | 0.01 ± 0.00 |
Muscle | 0.32 ± 0.17 | 0.06 ± 0.03 | 0.04 ± 0.01 | 0.01 ± 0.00 | 0.01 ± 0.00 |
Pancreas | 0.65 ± 0.18 | 0.11 ± 0.05 | 0.08 ± 0.01 | 0.02 ± 0.01 | 0.04 ± 0.01 |
Bone | 0.31 ± 0.13 | 0.06 ± 0.05 | 0.05 ± 0.03 | 0.02 ± 0.01 | 0.08 ± 0.02 |
Skin | 1.28 ± 0.68 | 0.22 ± 0.11 | 0.22 ± 0.08 | 0.09 ± 0.03 | 0.10 ± 0.01 |
Uptake ratio | |||||
Tumor to blood | 0.69 | 1.50 | 1.35 | 6.00 | 0.53 |
Tumor to muscle | 5.10 | 10.00 | 7.75 | 18.00 | 10.00 |
Data are represented as %ID/g (mean ± SD), or as uptake ratio of tumor to normal tissue for female nude mice (n=4) bearing SKOV-3 xenografted tumors. Mice were sacrificed at different times post-injection of 111In-DOTA-GSG-J18.
n=7;
n=5;
p=0.03; significant difference between tumor uptake of radiolabeled peptide 1 h post-injection with and without the presence of its non-radioactive counterpart.