Table 3.
Biodistribution studies of 111In-DOTA-8-AOC-BBN(7-14)NH2, 111In-DOTA-8-ADS-BBN(7-14)NH2, 111In-DOTA-AMBA-BBN(7-14)NH2, 111In-DOTA-Gly-AMBA-BBN(7-14)NH2 and 111In-DOTA-Gly-AM2BA-BBN(7-14)NH2 at 1, 4 and 24 hr post-injection in PC-3 tumor bearing SCID mice.
| Tissue | 8-AOC | 8-ADS | AMBA | Gly-AMBA | Gly-AM2BA | Nonsense |
|---|---|---|---|---|---|---|
| 1 hr p.i. | ||||||
| Blood | 0.24 ± 0.03 | 0.28 ± 0.17 | 0.33 ± 0.23 | 0.64 ± 0.25 | 0.15 ± 0.07b | 0.35 ± 0.08 |
| Heart | 0.19 ± 0.20 | 0.10 ± 0.03 | 0.26 ± 0.21 | 0.38 ± 0.11 | 0.11 ± 0.05b | 0.19 ± 0.09 |
| Lung | 0.40 ± 0.09 | 0.36 ± 0.21 | 0.59 ± 0.40 | 0.72 ± 0.26 | 0.39 ± 0.21b | 0.44 ± 0.12 |
| Liver | 0.54 ± 0.09 | 0.17 ± 0.03 | 0.31 ± 0.05 | 0.40 ± 0.13 | 0.23 ± 0.11b | 0.70 ± 0.08 |
| Stomach | 0.89 ± 0.40 | 0.73 ± 0.26 | 0.91 ± 0.18 | 2.25 ± 1.04 | 1.20 ± 0.33b | 0.20 ± 0.18 |
| Small Intestines (%ID) | 9.95 ± 0.58 | 5.59 ± 0.88 | 6.43 ± 0.98 | 9.95 ± 1.82 | 9.52 ± 1.65b | 1.04 ± 0.25 |
| Large Intestines (%ID) | 1.65 ± 0.14 | 2.34 ± 0.67 | 2.29 ± 0.20 | 5.22 ± 0.49 | 4.07 ± 0.53b | 0.28 ± 0.17 |
| Kidney | 4.41 ± 1.16 | 3.54 ± 0.36 | 5.69 ± 1.51 | 17.34 ± 7.45 | 6.00 ± 3.05b | 3.10 ± 0.37 |
| Spleen | 0.54 ± 0.25 | 0.43 ± 0.14 | 0.90 ± 0.26 | 1.97 ± 0.63 | 0.65 ± 0.23b | 0.22 ± 0.06 |
| Brain | 0.02 ± 0.01 | 0.02 ± 0.01 | 0.02 ± 0.01 | 0.05 ± 0.03 | 0.03 ± 0.02b | 0.03 ± 0.02 |
| Pancreas | 30.85 ± 5.07 | 19.22 ± 1.89 | 30.15 ± 5.90 | 46.85 ± 6.13 | 28.55 ± 1.46b | 0.12 ± 0.02 |
| Muscle | 0.06 ± 0.01 | 0.06 ± 0.01 | 0.09 ± 0.04 | 0.21 ± 0.05 | 0.09 ± 0.03b | 0.12 ± 0.02 |
| Bone | 0.26 ± 0.20 | 0.12 ± 0.07 | 0.26 ± 0.11 | 0.93 ± 0.34 | 0.63 ± 0.35b | 0.22 ± 0.11 |
| Tumor | 1.95 ± 1.07 | 2.53 ± 0.78 | 3.34 ± 0.70 | 2.97 ± 0.88 | 2.68 ± 0.62b | 0.58 ± 0.20 |
| Excretion (%ID)a | 72.54 ± 0.96 | 80.67 ± 0.74 | 78.69 ± 2.53 | 54.64 ± 4.43 | 67.23 ± 1.02b | 90.85 ± 3.78 |
| 4 hr p.i. | ||||||
| Blood | 0.03 ± 0.01 | 0.02 ± 0.01 | 0.06 ± 0.02 | 0.19 ± 0.04 | 0.02 ± 0.01 | ----- |
| Heart | 0.03 ± 0.02 | 0.04 ± 0.01 | 0.06 ± 0.03 | 0.21 ± 0.16 | 0.03 ± 0.03 | ----- |
| Lung | 0.14 ± 0.06 | 0.13 ± 0.09 | 0.16 ± 0.08 | 0.24 ± 0.15 | 0.11 ± 0.03 | ----- |
| Liver | 0.15 ± 0.02 | 0.13 ± 0.03 | 0.28 ± 0.08 | 0.25 ± 0.04 | 0.19 ± 0.08 | ----- |
| Stomach | 0.44 ± 0.31 | 0.42 ± 0.11 | 0.41 ± 0.15 | 1.09 ± 0.40 | 0.76 ± 0.21 | ----- |
| Small Intestines (%ID) | 3.06 ± 1.00 | 2.01 ± 0.38 | 4.59 ± 0.88 | 6.94 ± 1.17 | 4.04 ± 0.94 | ----- |
| Large Intestines (%ID) | 8.67 ± 2.96 | 7.13 ± 1.75 | 4.05 ± 0.80 | 5.79 ± 1.27 | 6.22 ± 1.16 | ----- |
| Kidney | 2.15 ± 0.32 | 3.92 ± 0.86 | 4.28 ± 1.10 | 7.22 ± 2.67 | 3.24 ± 1.18 | ----- |
| Spleen | 0.34 ± 0.09 | 0.33 ± 0.09 | 0.60 ± 0.23 | 1.76 ± 0.91 | 1.98 ± 2.40 | ----- |
| Brain | 0.01 ± 0.00 | 0.01 ± 0.00 | 0.01 ± 0.01 | 0.04 ± 0.02 | 0.01 ± 0.01 | ----- |
| Pancreas | 21.51 ± 3.45 | 18.04 ± 1.47 | 30.53 ± 5.35 | 38.95 ± 6.32 | 35.12 ± 8.20 | ----- |
| Muscle | 0.02 ± 0.01 | 0.03 ± 0.02 | 0.04 ± 0.02 | 0.03 ± 0.05 | 0.04 ± 0.01 | ----- |
| Bone | 0.12 ± 0.03 | 0.14 ± 0.02 | 0.33 ± 0.21 | 0.65 ± 0.44 | 0.29 ± 0.10 | ----- |
| Tumor | 1.10 ± 0.23 | 1.61 ± 0.57 | 2.42 ± 0.81 | 2.46 ± 0.90 | 2.81 ± 0.56 | ----- |
| Excretion (%ID)a | 78.27 ± 4.22 | 84.82 ± 2.31 | 81.42 ± 2.85 | 68.74 ± 2.35 | 78.40 ± 2.48 | ----- |
| 24 hr p.i. | ||||||
| Blood | 0.01 ± 0.00 | 0.01 ± 0.00 | 0.02 ± 0.00 | 0.08 ± 0.04 | 0.01 ± 0.01 | ----- |
| Heart | 0.02 ± 0.02 | 0.02 ± 0.01 | 0.04 ± 0.01 | 0.14 ± 0.09 | 0.02 ± 0.02 | ----- |
| Lung | 0.07 ± 0.03 | 0.06 ± 0.01 | 0.08 ± 0.02 | 0.15 ± 0.06 | 0.10 ± 0.04 | ----- |
| Liver | 0.06 ± 0.01 | 0.07 ± 0.01 | 0.21 ± 0.03 | 0.26 ± 0.09 | 0.11 ± 0.06 | ----- |
| Stomach | 0.11 ± 0.04 | 0.17 ± 0.03 | 0.20 ± 0.08 | 1.33 ± 0.39 | 0.63 ± 0.28 | ----- |
| Small Intestines (%ID) | 1.30 ± 0.30 | 1.23 ± 0.23 | 3.43 ± 0.56 | 5.33 ± 0.64 | 2.13 ± 0.34 | ----- |
| Large Intestines (%ID) | 0.93 ± 0.13 | 0.86 ± 0.14 | 1.59 ± 0.11 | 2.84 ± 0.41 | 2.69 ± 1.19 | ----- |
| Kidney | 0.72 ± 0.09 | 2.36 ± 0.66 | 1.90 ± 0.47 | 3.71 ± 2.37 | 1.40 ± 0.85 | ----- |
| Spleen | 0.28 ± 0.36 | 0.33 ± 0.08 | 0.45 ± 0.09 | 1.28 ± 0.77 | 0.97 ± 0.73 | ----- |
| Brain | 0.00 ± 0.00 | 0.01 ± 0.00 | 0.01 ± 0.00 | 0.04 ± 0.04 | 0.01 ± 0.00 | ----- |
| Pancreas | 10.70 ± 2.40 | 17.04 ± 1.65 | 23.84 ± 2.97 | 28.19 ± 4.88 | 13.39 ± 3.20 | ----- |
| Muscle | 0.01 ± 0.01 | 0.02 ± 0.01 | 0.02 ± 0.01 | 0.11 ± 0.07 | 0.02 ± 0.02 | ----- |
| Bone | 0.12 ± 0.04 | 0.09 ± 0.02 | 0.15 ± 0.03 | 0.75 ± 0.33 | 0.23 ± 0.13 | ----- |
| Tumor | 0.76 ± 0.21 | 1.23 ± 0.30 | 1.69 ± 0.34 | 1.15 ± 0.57 | 1.96 ± 0.72 | ----- |
| Excretion (%ID)a | 93.72 ± 0.65 | 91.71 ± 0.89 | 87.35 ± 1.06 | 78.62 ± 1.88 | 89.61 ± 1.32 | ----- |
Organ uptake values expressed as %ID/g and n = 5 unless otherwise noted.
a
The biodistribution study of 111In-DOTA-8-AOC-NONSENSE was performed at 1 hr post-injection in PC-3 tumor bearing SCID mice.
b
Excretion values at 1, 4 and 24 hr time points were calculated using the activity values associated with the excreted urine and bladder contents at the time of sacrifice; at the 24 hr time point, excretion values also included the activity associated with fecal material.
c
n = 4