Table 2.
Biodistribution data for [99mTc]Tc–DT1, expressed as % IA/g mean ± SD in AsPC-1 xenograft-bearing SCID mice at 4 h pi, without or after treatment with Entresto + Lis.
| [99mTc]Tc–DT1: 4 h pi | |||||
|---|---|---|---|---|---|
| Controls 1 | Entresto + Lis 2 | Block 3 | |||
| Blood | 0.07 ± 0.01 | 0.08 ± 0.02 | 0.09 ± 0.01 | ||
| Liver | 0.44 ± 0.05 | 0.67 ± 0.06 | 0.55 ± 0.06 | ||
| Heart | 0.08 ± 0.01 | 0.11 ± 0.02 | 0.18 ± 0.11 | ||
| Kidneys | 4.18 ± 3.80 | ⇤ p < 0.0001 ⇥ | 6.81 ± 1.74 | ⇤ p < 0.001 ⇥ | 4.15 ± 1.75 |
| Stomach | 0.48 ± 0.26 | 0.57 ± 0.14 | 2.75 ± 1.63 | ||
| Intestines | 0.65 ± 0.04 | 2.13 ± 0.24 | 1.07 ± 0.01 | ||
| Spleen | 0.22 ± 0.05 | 0.58 ± 0.35 | 0.31 ± 0.07 | ||
| Muscle | 0.03 ± 0.01 | 0.06 ± 0.03 | 0.07 ± 0.06 | ||
| Lungs | 0.18 ± 0.03 | 0.62 ± 0.35 | 0.41 ± 0.07 | ||
| Pancreas | 0.05 ± 0.01 | 0.10 ± 0.01 | 0.08 ± 0.00 | ||
| Tumor | 1.25 ± 0.14 | ⇤ p < 0.0001 ⇥ | 7.05 ± 0.80 | ⇤ p < 0.0001 ⇥ | 0.74 ± 0.01 |
All animals were injected with 185 kBq/10 pmol peptide; 1 Control mice group (n = 4) with untreated animals; 2 Entresto + Lis mice group (n = 4) with animals receiving 12 mg Entresto per os 30 min prior to radiotracer co-injection, together with 200 µg Lis to in situ to inhibit NEP and ACE, respectively. 3 Block mice group (n = 3), with animals co-injected with 100 µg NT for in vivo NTS1R blockade, in addition to being treated with the Entresto + Lis combination.