What type of study is this?

This is a In Vitro Study study.

November 30, 2025

A Novel Radiotracer for NTSR1-Targeted PET Imaging of Tumor: Preclinical and First-in-Human Studies

Puntos clave

Tracer achieves a tumor-to-lung ratio of 7.89 ± 0.76 in lung adenocarcinoma; supports potential for clinical use.
Development of a new probe, combining DOTA-NT-20.3 with an albumin-binding moiety, improving stability and uptake.
Preclinical studies validate high specificity for neurotensin receptor 1, comparing favorably to prior imaging agents.
Biodistribution profile highlights significant accumulation in tumors, encouraging further clinical exploration.

Resumen

Neurotensin receptor 1 (NTSR1) is overexpressed in various cancers, making it an attractive target for tumor imaging and therapy. However, current NTSR1-targeting peptides derived from neurotensin (NT) analogs face challenges including rapid metabolic clearance and insufficient tumor uptake, limiting their clinical translation. To address this, we developed a novel probe, 68GaGa-DOTA-NT-20.3-IPBA, by conjugating the DOTA-NT-20.3 probe with an albumin-binding moiety (4-(p-iodophenyl)butyric acid IPBA). The resulting tracer exhibited enhanced lipophilicity and albumin-binding capacity, while maintaining reasonable in vitro stability, radiochemical yield, and purity (all >95%). In vitro and in vivo evaluations confirmed its high affinity and specificity for NTSR1. Clinical PET/CT imaging demonstrated significant tracer accumulation in lung adenocarcinoma, with a tumor-to-lung ratio of 7.89 ± 0.76 at 60 min postinjection and a favorable biodistribution profile. Collectively, 68GaGa-DOTA-NT-20.3-IPBA shows high potential as a PET tracer for NTSR1-expressing tumors and DOTA-NT-20.3-IPBA may be a promising candidate for future theranostic development.

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