Exendin‐4 analogs in insulinoma theranostics

• Published in: Journal of labelled compounds & radiopharmaceuticals Vol. 62; no. 10; pp. 656 - 672
• Main Authors: Jansen, Tom.J.P., Lith, Sanne.A.M., Boss, Marti, Brom, Maarten, Joosten, Lieke, Béhé, Martin, Buitinga, Mijke, Gotthardt, Martin
• Format: Journal Article
• Language: English
• Published: England Wiley Subscription Services, Inc 01.08.2019; John Wiley and Sons Inc
• Subjects: Animals; Beta cells; Computed tomography; Diagnostic Imaging - methods; Exenatide - chemistry; Exenatide - therapeutic use; exendin‐4; GLP‐1 receptor; Glucagon; Humans; Insulinoma; Insulinoma - diagnostic imaging; Insulinoma - drug therapy; Insulinoma - therapy; Localization; Medical imaging; Neuroendocrine tumors; Pancreas; peptide receptor radionuclide therapy (PRRT); Peptides; Photochemotherapy; Photodynamic therapy; Photon emission; Positron emission; Positron emission tomography; positron emission tomography (PET); Precision medicine; Radiation therapy; Radioisotopes; Single photon emission computed tomography; single‐photon emission computed tomography (SPECT); Special Issue Review; targeted photodynamic therapy (tPDT); theranostics; Therapeutic applications; Tomography; Tracers; peptide receptor radionuclide therapy (PRRT); positron emission tomography (PET); GLP-1 receptor; insulinoma; targeted photodynamic therapy (tPDT); theranostics; single-photon emission computed tomography (SPECT); exendin-4
• ISSN: 0362-4803; 1099-1344
• DOI: 10.1002/jlcr.3750

Insulinomas are neuroendocrine tumors arising from the pancreatic beta cells. Currently, surgical resection is the therapy of choice, and therefore, preoperative localization of insulinomas is essential. Nearly all insulinomas show overexpression of the glucagon‐like peptide‐1 receptor (GLP‐1R), and therefore, radiolabeled GLP‐1 peptide analog exendin‐4 can be used for diagnosis and preoperative localization with nuclear imaging. Here, we present an overview of the development and clinical implementation of exendin‐4–based tracers for single‐photon emission computed tomography (SPECT) and positron emission tomography (PET) imaging of insulinomas, and we address the potential use of this molecule for optical imaging. At last, we discuss the possibilities and pitfalls of the use of exendin‐4–based tracers for therapeutic applications such as peptide receptor radionuclide therapy (PRRT) or targeted photodynamic therapy (tPDT), giving a future outlook on the use of exendin‐4 in insulinoma theranostics. Insulinomas, neuroendocrine tumors arising from pancreatic beta cells, often show overexpression of the glucagon‐like peptide‐1 receptor. Therefore, imaging with glucagon‐like peptide analog exendin‐4 can be used for diagnosis and preoperative localization. This review presents an overview of the development and clinical implementation of exendin‐based tracers for nuclear imaging, and the potential use of exendin‐4 based tracers for optical imaging and therapeutic applications such as peptide receptor radionuclide therapy or targeted photodynamic therapy.