Table 2.
Biodistribution data for [99mTc]Tc-DB4, expressed as %IA/g mean ± SD, n = 4, in PC-3 xenograft-bearing SCID mice at 4 h pi without or during treatment with either LBQ657 or Entresto.
| Tissue | [99mTc]Tc-DB4—4 h pi | |||
|---|---|---|---|---|
| Controls 1 | LBQ657 2 | Entresto 3 | Block 4 | |
| Blood | 0.12 ± 0.11 | 0.14 ± 0.03 | 0.17 ± 0.03 | 0.08 ± 0.01 |
| Liver | 1.76 ± 0.74 | 1.61 ± 0.19 | 1.27 ± 0.20 | 0.90 ± 0.10 |
| Heart | 0.24 ± 0.13 | 0.26 ± 0.03 | 0.23 ± 0.07 | 0.13 ± 0.00 |
| Kidneys | 9.56 ± 4.35 | 4.67 ± 1.03 | 7.86 ± 2.46 | 4.72 ± 0.72 |
| Stomach | 1.50 ± 0.71 | 1.12 ± 0.20 | 1.66 ± 0.30 | 0.20 ± 0.04 |
| Intestines | 7.99 ± 0.08 | 9.00 ± 0.64 | 11.36 ± 0.95 | 1.23 ± 0.21 |
| Spleen | 1.92 ± 0.75 | 2.46 ± 0.95 | 1.93 ± 0.44 | 2.60 ± 0.48 |
| Muscle | 0.06 ± 0.02 | 0.06 ± 0.01 | 0.10 ± 0.09 | 0.03 ± 0.00 |
| Lungs | 0.40 ± 0.21 | 0.52 ± 0.18 | 0.66 ± 0.11 | 0.72 ± 0.26 |
| Pancreas | 27.71 ± 6.36 | 56.06 ± 4.24 | 60.98 ± 6.41 | 0.68 ± 0.04 |
| Tumor | 7.13 ± 1.76 | 16.17 ± 0.71 | 17.50 ± 3.70 | 0.55 ± 0.04 |
All animals were injected with 200 kBq/10 pmol peptide. 1 Mice co-injected with vehicle, 2 mice co-injected with LBQ657, 3 mice co-injected with vehicle 30 min after oral administration of Entresto and 4 mice co-injected with [Tyr4]BBN 30 min after oral administration of Entresto for in vivo GRPR-blockade.