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Article Abstract
Background: The human epidermal growth factor receptor 2 gene (HER2) has been identified as a potential therapeutic target in lung adenocarcinoma (LUAD). Non-invasive positron emission tomography (PET) imaging provides a reliable strategy for determination of HER2 expression through whole-body detection of abnormalities. The PET tracer Ga-NOTA-MAL-Cys-MZHER has shown promising results for HER2-positive breast and gastric cancers. This study aims to evaluate the performance of Ga-NOTA-MAL-Cys-MZHER and models and in clinical patients with HER2-positive LUAD.
Methods: NOTA-MAL-Cys-MZHER was synthesized and labeled with Ga. Cell uptake, cell binding ability, and stability studies of Ga-NOTA-MAL-Cys-MZHER were assessed both in the Calu-3 lung cancer (LC) cell line and normal mice. assessment in tumor-bearing mice was conducted using microPET imaging and biodistribution experiments. Additionally, preliminary PET/CT imaging analysis was performed on HER2-positive LC patients.
Results: Ga-NOTA-MAL-Cys-MZHER was prepared with a radiochemical purity (RCP) exceeding 95%. The tracer demonstrated high cell uptake in HER2-overexpressing Calu-3 cells, with an IC of 158.9, an adequate 1.73 nM. Good stability was exhibited both and . MicroPET imaging of Calu-3-bearing mice revealed high tumor uptake and notable tumor-to-background ratios. Positive outcomes were also observed in two HER2-positive LUAD patients.
Conclusion: Ga-NOTA-MAL-Cys-MZHER demonstrated satisfactory stability, sensitivity, and specificity. These findings suggest that Ga-NOTA-MAL-Cys-MZHER PET/CT imaging provides a novel tool for non-invasive visual assessment of HER2 expression in LUAD patients.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11347437 | PMC |
| http://dx.doi.org/10.3389/fmed.2024.1447500 | DOI Listing |
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