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European Journal of Nuclear Medicine and Molecular Imaging

Published in:

01-02-2012 | Original Article

PET imaging of EGF receptors using [¹⁸F]FBEM-EGF in a head and neck squamous cell carcinoma model

Authors: Weihua Li, Gang Niu, Lixin Lang, Ning Guo, Ying Ma, Dale O. Kiesewetter, Joseph M. Backer, Baozhong Shen, Xiaoyuan Chen

Published in: European Journal of Nuclear Medicine and Molecular Imaging | Issue 2/2012

Abstract

Purpose

To prepare and evaluate a new radiotracer for molecular imaging of cell surface receptors for epidermal growth factor (EGF).

Methods

Cys-tagged EGF (cEGF) was labeled with ¹⁸F by coupling the free thiol group of the Cys tag with N-[2-(4-[¹⁸F]fluorobenzamido)ethyl]maleimide ([¹⁸F]FBEM) to form [¹⁸F]FBEM-cEGF. Cell uptake, internalization and efflux of [¹⁸F]FBEM-cEGF were tested in human head and neck squamous carcinoma UM-SCC1 cells. In vivo tumor targeting and pharmacokinetics of the radiotracers were evaluated in UM-SCC1 tumor-bearing athymic nude mice by static and dynamic microPET imaging. Ex vivo biodistribution assays were performed to confirm the noninvasive imaging results.

Results

The radiolabeling yield for [¹⁸F]FBEM-cEGF was over 60%, based on starting [¹⁸F]FBEM. [¹⁸F]FBEM-cEGF exhibited rapid blood clearance through both hepatobiliary and renal excretion. UM-SCC1 tumors were clearly visualized and showed modest tracer uptake of 2.60 ± 0.59 %ID/g at 30 min after injection. Significantly higher tumor uptake of [¹⁸F]FBEM-cEGF (5.99 ± 1.61%ID/g at 30 min after injection, p < 0.01) and tumor/nontumor ratio were achieved by coinjection of 50 μg of unlabeled EGF. Decreased liver uptake of [¹⁸F]FBEM-cEGF was observed when unlabeled EGF was coadministered.

Conclusion

With optimized liver blocking, [¹⁸F]FBEM-cEGF has the potential to be used in a noninvasive and quantitative manner for detection of malignant lesions and evaluation of EGFR activity.

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Title: PET imaging of EGF receptors using [18F]FBEM-EGF in a head and neck squamous cell carcinoma model
Authors: Weihua Li
Gang Niu
Lixin Lang
Ning Guo
Ying Ma
Dale O. Kiesewetter
Joseph M. Backer
Baozhong Shen
Xiaoyuan Chen
Publication date: 01-02-2012
Publisher: Springer-Verlag
Published in: European Journal of Nuclear Medicine and Molecular Imaging / Issue 2/2012
Print ISSN: 1619-7070
Electronic ISSN: 1619-7089
DOI: https://doi.org/10.1007/s00259-011-1969-8

Keynote webinar | Spotlight on medication adherence

Springer Medicine

PET imaging of EGF receptors using [¹⁸F]FBEM-EGF in a head and neck squamous cell carcinoma model

Abstract

Purpose

Methods

Results

Conclusion

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Abstract

Purpose

Methods

Results

Conclusion

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