⁶⁸Ga-NeoB: Präklinische Ergebnisse zur Bildgebung gastrointestinaler Stromatumoren und zur Bestimmung der Zielrezeptordichte im Gastrointestinaltrakt

Zusammenfassung

⁶⁸Ga-NeoB (früher bekannt als NeoBOMB1) ist ein neuartiger DOTA-gekoppelter Gastrin-Releasing-Peptid-Rezeptor(GRPR)-Antagonist mit hoher Bindungsaffinität zum GRPR und ausgezeichneter In-vivo-Stabilität. Ziel dieser präklinischen Studie war es, die Verwendung von ⁶⁸Ga-NeoB zur Bestimmung der GRPR-Expression im Pankreasgewebe weiter zu erforschen, indem der GRPR-Sättigungsgrad im Pankreas bei der Verwendung verschiedener molarer Stoffmengen von ⁶⁸Ga-NeoB geschätzt wurde. Darüber hinaus wurde ⁶⁸Ga-NeoB als Tracer für gastrointestinale Stromatumoren (GIST) in 2 verschiedenen Mausstämmen untersucht. Anschließende Ex-vivo-Biodistributionsstudien mit verschiedenen Stoffmengen des antagonistischen Tracers ⁶⁸Ga-NeoB mit hoher Bindungsaffinität zu GRPR wurden zur Abschätzung der Rezeptordichte in Organen oder Geweben mit hoher Expression dieses Rezeptors genutzt. Die Kombination von PET/CT und MRT-Datensätzen unterstützte die Ermittlung von Organanreicherungen auch bei Erreichen des Sättigungsgrades des Radiotracers in gastrointestinalen Organen.

Abstract

⁶⁸Ga-NeoB (formerly known as NeoBOMB1) is a novel DOTA-coupled gastrin releasing peptide receptor (GRPR) antagonist with high binding affinity for GRPR and excellent in vivo stability. The aim of this preclinical study was to further explore the use of ⁶⁸Ga-NeoB to determine GRPR expression in pancreatic tissue by estimating the GRPR saturation level in the pancreas when using different molar activities of ⁶⁸Ga-NeoB. In addition, ⁶⁸Ga-NeoB was investigated as a tracer for gastrointestinal stromal tumors (GIST) in 2 different mouse strains. Subsequent ex vivo biodistribution studies using different molar amounts of the antagonistic tracer ⁶⁸Ga-NeoB with high binding affinity for GRPR were used to estimate receptor density in organs or tissues with high expression of this receptor. The combination of PET/CT and MRI datasets supported the determination of organ enrichment even when the saturation level of the radiotracer was reached in gastrointestinal organs.

Schlüsselwörter

NeoBombesin - Gallium-68 - PET - GIST430 - GRPR

Keywords

NeoBombesin - Gallium-68 - PET - GIST430 - GRPR

Publication History

Article published online:
10 June 2021

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