Biodistribution Data (%)ID/g Tissue ± SD; Each Value is Average of 3 or 4 Animals
| Biodistribution | [99mTc/EDDA/HYNIC]-OC (99mTc-(1))4 h | [111In-DTPA]-OC | [99mTc/EDDA/HYNIC]-TOC (99mTc-(2)) | [99mTc/EDDA/HYNIC]-TATE (99mTc-(3)) | [111In-DOTA]-TATE | ANOVA (4-h values) | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 4 h | 4-h blocked* | 4 h | 4-h blocked* | 1 h | 4 h | 4-h blocked* | 4 h | 4-h blocked* | ||||||||||||||
| Blood | 0.02 ± 0.00 | 0.02 ± 0.00 | 0.01 ± 0.00 | 0.05 ± 0.03 | 0.03 ± 0.00 | 0.21 ± 0.03 | 0.09 ± 0.01 | 0.03 ± 0.00 | 0.08 ± 0.09 | 0.05 ± 0.00 | ||||||||||||
| Tumor | 0.70 ± 0.13†‡ | 0.99 ± 0.08†‡ | 0.06 ± 0.00 | 3.85 ± 1.0§ | 0.14 ± 0.02 | 5.01 ± 0.81 | 3.99 ± 0.58§ | 0.27 ± 0.02 | 4.12 ± 0.74§ | 0.17 ± 0.06 | P = 6·10−3 | |||||||||||
| Kidney | 2.79 ± 0.27 | 1.75 ± 0.16 | 1.39 ± 0.08 | 2.08 ± 0.05 | 1.80 ± 0.08 | 4.88 ± 0.38 | 1.60 ± 0.2 | 1.69 ± 0.18 | 2.42 ± 0.78 | 1.77 ± 0.75 | ||||||||||||
| Adrenals | 0.65 ± 0.35 | 0.70 ± 0.12 | 0.08 ± 0.04 | 3.58 ± 0.61 | 0.07 ± 0.02 | 5.50 ± 1.00 | 1.79 ± 0.36 | 0.29 ± 0.01 | 6.46 ± 1.56 | 0.38 ± 0.29 | ||||||||||||
| Pancreas | 0.71 ± 0.11†‡ | 0.87 ± 0.33†‡ | 0.04 ± 0.00 | 5.14 ± 1.46‡§ | 0.14 ± 0.02 | 10.71 ± 1.10 | 9.01 ± 0.86†§ | 0.56 ± 0.04 | 9.31 ± 1.00†§ | 0.17 ± 0.06 | P = 1·10−3 | |||||||||||
| Spleen | 0.07 ± 0.00 | 0.04 ± 0.01 | 0.03 ± 0.00 | 0.08 ± 0.02 | 0.05 ± 0.00 | 0.11 ± 0.01 | 0.08 ± 0.00 | 0.05 ± 0.00 | 0.11 ± 0.02 | 0.03 ± 0.01 | ||||||||||||
| Stomach | 0.24 ± 0.01 | 0.20 ± 0.02 | 0.01 ± 0.00 | 1.20 ± 0.15 | 0.05 ± 0.00 | 2.10 ± 0.22 | 0.56 ± 0.45 | 0.08 ± 0.01 | 1.08 ± 0.62 | 0.07 ± 0.04 | ||||||||||||
| Intestine | 0.07 ± 0.01 | 0.07 ± 0.02 | 0.02 ± 0.00 | 0.26 ± 0.02 | 0.04 ± 0.01 | 0.39 ± 0.08 | 0.19 ± 0.02 | 0.05 ± 0.01 | 0.24 ± 0.03 | 0.18 ± 0.27 | ||||||||||||
| Liver | 0.11 ± 0.01 | 0.09 ± 0.02 | 0.09 ± 0.01 | 0.09 ± 0.01 | 0.07 ± 0.00 | 0.17 ± 0.02 | 0.08 ± 0.01 | 0.05 ± 0.00 | 0.09 ± 0.06 | 0.03 ± 0.01 | ||||||||||||
| Lung | 0.06 ± 0.01 | 0.03 ± 0.01 | 0.02 ± 0.00 | 0.08 ± 0.01 | 0.05 ± 0.00 | 0.25 ± 0.04 | 0.09 ± 0.01 | 0.05 ± 0.00 | 0.09 ± 0.05 | 0.02 ± 0.01 | ||||||||||||
| Heart | 0.02 ± 0.00 | 0.01 ± 0.00 | 0.01 ± 0.00 | 0.03 ± 0.01 | 0.01 ± 0.00 | 0.13 ± 0.02 | 0.04 ± 0.00 | 0.02 ± 0.00 | 0.03 ± 0.02 | 0.01 ± 0.00 | ||||||||||||
| Bone | 0.02 ± 0.00 | 0.01 ± 0.01 | 0.01 ± 0.01 | 0.02 ± 0.00 | 0.01 ± 0.00 | 0.05 ± 0.01 | 0.03 ± 0.00 | 0.02 ± 0.01 | 0.03 ± 0.02 | 0.03 ± 0.02 | ||||||||||||
| Tumor-to-tissue radioactivity ratios at 4 h after injection | ||||||||||||||||||||||
| Tumor/blood | 35.0 | 49.5 | 77.0 | 44.3 | 51.5 | |||||||||||||||||
| Tumor/kidney | 0.3 | 0.6 | 1.9 | 2.5 | 1.7 | |||||||||||||||||
| Tumor/liver | 6.4 | 11.0 | 42.8 | 49.9 | 45.8 | |||||||||||||||||
↵* Blocked with 100 μg of [Tyr3]octreotide coinjected with radiopeptide.
↵† P < 0.05 vs. [99mTc/EDDA/HYNIC]-TOC.
↵‡ P < 0.05 vs. [99mTc/EDDA/HYNIC]-TATE.
↵§ P < 0.05 vs. [111In-DTPA]-OC.
Significance of tumor and pancreas uptake at 4 h was analyzed by Kruskal–Wallis ANOVA test (if >2 compounds) or Student t test (for 2 compounds).