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EJNMMI Radiopharmacy and Chemistry

Table 3 In vivo stability comparing investigated compounds with [99mTc]DB-15, without (controls) or during NEP-inhibition (induced by Entresto®, or phosphoramidon, PA)

From: Preclinical evaluation of new GRPR-antagonists with improved metabolic stability for radiotheranostic use in oncology

Radioligand

Control

vs. ref

Between groups

 + Entresto®

vs. ref

[99mTc]DB15

76 ± 2%

 

ns

83 ± 2% (PA)

 

[111In]In-AU-SAR-M1

69 ± 2%

*

**

84 ± 7%

ns

[111In]In-AU-SAR-M2

72 ± 3%

ns

***

93.5 ± 0.8%

**

[111In]In-AU-SAR-M3

67 ± 3%

**

****

91 ± 1%

*

  1. For statistical analysis, two-way ANOVA test was used, with Sidak post-hoc analysis for the multiple comparisons. ⁕: p < 0.05, ⁕⁕: p < 0.01, ⁕⁕⁕: p < 0.001, ⁕⁕⁕⁕: p < 0.0001, ns: non-significant
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