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Development and Evaluation of 18F-IRS for Molecular Imaging Mutant EGF Receptors in NSCLC
Yan Song1,2, Zunyu Xiao1,2, Kai Wang1,2
1Molecular Imaging Research Center, Harbin Medical University, Harbin, Heilongjiang, China.
Abstract:
To prepare and evaluate a new radiotracer 18F-IRS for molecular imaging mutant EGF Receptors in vitro and vivo. Uptake and efflux of 18F-IRS were performed with four NSCLC cell lines including HCC827, H1975, H358 and H520. In vivo tumor targeting and pharmacokinetics of the radiotracers were also evaluated in HCC827, H1975, H358 and H520 tumor-bearing nude mice by PET/CT imaging. Ex vivo biodistribution assays were performed to quantify the accumulation of 18F-IRS in vivo. We also performed 18F-IRS PET/CT imaging of three patients with NSCLC. We labeled this small molecule with QD620 for flow cytometry and confocal imaging analyses. The uptakes of 18F-IRS by HCC827 and HCC827 tumors were significantly higher than those of H358, H1975 and H520, and they were reduced by the addition of 100 μM of gefitinib. Biodistribution experiments showed an accumulation of 18F-IRS in tumors of HCC827 xenografts. Flow cytometry and confocal imaging with QD620-IRS further demonstrated that binding specifically to HCC827 cells. 18F-IRS accumulation was preferential in the tumor, which was NSCLC with responsive EGFR exon 19 deleted. 18F-IRS showed high binding stability and specificity to 19 exon deleted EGFR mutation in vitro and vivo.
Insights
A new radiotracer, 18F-IRS, effectively targets mutant epidermal growth factor receptors (EGFR) in non-small cell lung cancer (NSCLC) cells and tumors. This tracer shows high binding stability and specificity for EGFR exon 19 deletions in vitro and in vivo.
Area of Science:
- Molecular Imaging
- Radiochemistry
- Oncology
Background:
- Mutant epidermal growth factor receptors (EGFR) are key drivers in non-small cell lung cancer (NSCLC).
- Targeted molecular imaging tracers are crucial for diagnosing and monitoring NSCLC with specific EGFR mutations.
Purpose of the Study:
- To develop and assess the novel radiotracer 18F-IRS for molecular imaging of mutant EGFR in NSCLC.
- To evaluate the in vitro and in vivo performance of 18F-IRS in preclinical models and human patients.
Main Methods:
- Preparation and in vitro evaluation of 18F-IRS uptake and efflux in NSCLC cell lines (HCC827, H1975, H358, H520).
- In vivo evaluation using PET/CT imaging in NSCLC tumor-bearing nude mice.
- Ex vivo biodistribution assays and flow cytometry/confocal imaging with QD620-IRS.
- Clinical PET/CT imaging in three NSCLC patients.
Main Results:
- 18F-IRS demonstrated significantly higher uptake in HCC827 cells and tumors compared to other cell lines.
- Uptake was reduced by gefitinib, indicating specific targeting of EGFR.
- Biodistribution studies confirmed 18F-IRS accumulation in HCC827 xenograft tumors.
- QD620-IRS confirmed specific binding to HCC827 cells.
- 18F-IRS accumulation was preferential in NSCLC tumors with responsive EGFR exon 19 deletions.
Conclusions:
- 18F-IRS is a promising radiotracer for molecular imaging of NSCLC with EGFR exon 19 deletions.
- The tracer exhibits high binding stability and specificity in vitro and in vivo.
- 18F-IRS facilitates targeted imaging of specific EGFR mutations in NSCLC.
![Dynamic Imaging of Chimeric Antigen Receptor T Cells with [18F]Tetrafluoroborate Positron Emission Tomography/Computed Tomography](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F62334.jpg&w=3840&q=50)
