| First Author | Murakami T | Year | 2021 |
| Journal | Sci Rep | Volume | 11 |
| Issue | 1 | Pages | 15014 |
| PubMed ID | 34294854 | Mgi Jnum | J:308631 |
| Mgi Id | MGI:6740078 | Doi | 10.1038/s41598-021-94595-6 |
| Citation | Murakami T, et al. (2021) Distinctive detection of insulinoma using [(18)F]FB(ePEG12)12-exendin-4 PET/CT. Sci Rep 11(1):15014 |
| abstractText | Specifying the exact localization of insulinoma remains challenging due to the lack of insulinoma-specific imaging methods. Recently, glucagon-like peptide-1 receptor (GLP-1R)-targeted imaging, especially positron emission tomography (PET), has emerged. Although various radiolabeled GLP-1R agonist exendin-4-based probes with chemical modifications for PET imaging have been investigated, an optimal candidate probe and its scanning protocol remain a necessity. Thus, we investigated the utility of a novel exendin-4-based probe conjugated with polyethylene glycol (PEG) for [(18)F]FB(ePEG12)12-exendin-4 PET imaging for insulinoma detection. We utilized [(18)F]FB(ePEG12)12-exendin-4 PET/CT to visualize mouse tumor models, which were generated using rat insulinoma cell xenografts. The probe demonstrated high uptake value on the tumor as 37.1 +/- 0.4%ID/g, with rapid kidney clearance. Additionally, we used Pdx1-Cre;Trp53(R172H);Rb(f/f) mice, which developed endogenous insulinoma and glucagonoma, since they enabled differential imaging evaluation of our probe in functional pancreatic neuroendocrine neoplasms. In this model, our [(18)F]FB(ePEG12)12-exendin-4 PET/CT yielded favorable sensitivity and specificity for insulinoma detection. Sensitivity: 30-min post-injection 66.7%, 60-min post-injection 83.3%, combined 100% and specificity: 30-min post-injection 100%, 60-min post-injection 100%, combined 100%, which was corroborated by the results of in vitro time-based analysis of internalized probe accumulation. Accordingly, [(18)F]FB(ePEG12)12-exendin-4 is a promising PET imaging probe for visualizing insulinoma. |
