Protocol for Clinical GLP-1 Receptor PET/CT Imaging with [68Ga]Ga-NODAGA-Exendin-4

Methods Mol Biol. 2023:2592:143-153. doi: 10.1007/978-1-0716-2807-2_9.

Abstract

Imaging with radiolabeled exendin enables detection and characterization of glucagon-like peptide 1 receptors (GLP-1Rs) in vivo with high specificity. The novel radiotracer [68Ga]Ga-NODAGA-exendin-4 forms a stable complex after a simple and fast labeling procedure. Beta-cell mass in the islets of Langerhans can be visualized using [68Ga]Ga-NODAGA-exendin-4, which is promising for research into diabetes mellitus (DM) pathophysiology. Furthermore, this radiotracer enables very sensitive detection of insulinomas, resulting from vast overexpression of GLP-1Rs, and seems promising for the detection of focal lesions in congenital hyperinsulinism (CHI). Here, we describe the procedures involved in [68Ga]Ga-NODAGA-exendin-4 positron emission tomography (PET)/computed tomography (CT) imaging including the radiolabeling of the NODAGA-exendin conjugate with 68Ga, quality controls, and PET/CT.

Keywords: Congenital hyperinsulinism; Exendin PET; Exendin-4; GLP-1; GLP-1R; Ga-68; Insulinoma; PET/CT imaging; β cell mass; β cells.

MeSH terms

  • Exenatide
  • Gallium Radioisotopes
  • Glucagon-Like Peptide-1 Receptor*
  • Humans
  • Pancreatic Neoplasms* / pathology
  • Peptides / chemistry
  • Positron Emission Tomography Computed Tomography
  • Positron-Emission Tomography / methods

Substances

  • Glucagon-Like Peptide-1 Receptor
  • Exenatide
  • Gallium Radioisotopes
  • Peptides
  • 1-(1,3-carboxypropyl)-4,7-carboxymethyl-1,4,7-triazacyclononane