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18F-Labeling of Radiotracers Functionalized with a Silicon Fluoride Acceptor SiFA for Positron Emission Tomography
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Preliminary evaluation of [18F]AlF-NOTA-MAL-Cys39-exendin-4 in insulinoma with PET

Qing Xu1, Chen Zhu1, Yuping Xu2

  • 1a Department of Radiation Oncology , The First Affiliated Hospital of Nanjing Medical University , Nanjing , China .

Journal of Drug Targeting
|March 12, 2015
PubMed
Abstract

Insights

A novel radiotracer, [(18)F]AlF-NOTA-MAL-Cys(39)-exendin-4, demonstrates high specificity and uptake for imaging glucagon-like peptide-1 receptor (GLP-1R) positive insulinomas. This tracer shows promise for future clinical applications in insulinoma detection.

Area of Science:

  • Nuclear Medicine
  • Radiochemistry
  • Oncology

Background:

  • Glucagon-like peptide-1 receptor (GLP-1R) is highly expressed in insulinomas, presenting a viable target for diagnostic imaging.
  • Exendin-4 analogs are established for GLP-1R imaging due to their specific binding properties.

Purpose of the Study:

  • To design and synthesize a novel GLP-1R imaging agent, [(18)F]AlF-NOTA-MAL-Cys(39)-exendin-4, for enhanced insulinoma visualization.
  • To evaluate the potential of this new agent in preclinical models of insulinoma.

Main Methods:

  • Cys(39)-exendin-4 was conjugated with NOTA-MAL and subsequently radiolabeled with [(18)F]AlF.
  • The tumor-targeting efficacy and specificity of [(18)F]AlF-NOTA-MAL-Cys(39)-exendin-4 were assessed in vitro using INS-1 cells and in vivo using BALB/c nude mice models.

Main Results:

  • The tracer was produced with high radiochemical purity (>95%) and a yield of 17.5%.
  • PET imaging revealed excellent tumor visualization with high tracer uptake and favorable tumor-to-background ratios (e.g., 63.25 for tumor-to-muscle at 60 min).
  • Specificity was confirmed by significant reduction in tumor uptake upon co-administration of unlabeled Cys(39)-exendin-4.

Conclusions:

  • [(18)F]AlF-NOTA-MAL-Cys(39)-exendin-4 exhibits promising characteristics for effective insulinoma imaging.
  • The developed tracer holds potential for translation into clinical diagnostic studies.
Keywords:
Expressionpeptideradio labelingtumor targeting

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