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Pharmaceuticals 2017, 10(1), 30; doi:10.3390/ph10010030

Current Status of Radiopharmaceuticals for the Theranostics of Neuroendocrine Neoplasms

1
Division of Radiopharmaceutical Chemistry, University Hospital of Basel, 4031 Basel, Switzerland
2
Department of Nuclear Medicine, University Medical Centre Ljubljana, 1000 Ljubljana, Slovenia
3
Department of Medicinal Chemistry, Uppsala University, 751 23 Uppsala, Sweden
*
Author to whom correspondence should be addressed.
Academic Editor: Klaus Kopka
Received: 7 February 2017 / Revised: 8 March 2017 / Accepted: 9 March 2017 / Published: 15 March 2017
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Abstract

Abstract: Nuclear medicine plays a pivotal role in the management of patients affected by neuroendocrine neoplasms (NENs). Radiolabeled somatostatin receptor analogs are by far the most advanced radiopharmaceuticals for diagnosis and therapy (radiotheranostics) of NENs. Their clinical success emerged receptor-targeted radiolabeled peptides as an important class of radiopharmaceuticals and it paved the way for the investigation of other radioligand-receptor systems. Besides the somatostatin receptors (sstr), other receptors have also been linked to NENs and quite a number of potential radiolabeled peptides have been derived from them. The Glucagon-Like Peptide-1 Receptor (GLP-1R) is highly expressed in benign insulinomas, the Cholecystokinin 2 (CCK2)/Gastrin receptor is expressed in different NENs, in particular medullary thyroid cancer, and the Glucose-dependent Insulinotropic Polypeptide (GIP) receptor was found to be expressed in gastrointestinal and bronchial NENs, where interestingly, it is present in most of the sstr-negative and GLP-1R-negative NENs. Also in the field of sstr targeting new discoveries brought into light an alternative approach with the use of radiolabeled somatostatin receptor antagonists, instead of the clinically used agonists. The purpose of this review is to present the current status and the most innovative strategies for the diagnosis and treatment (theranostics) of neuroendocrine neoplasms using a cadre of radiolabeled regulatory peptides targeting their receptors. View Full-Text
Keywords: neuroendocrine neoplasms; theranostics; radiolabeled peptides; somatostatin receptor antagonists; GLP-1R; exendin-4; CCK2; gastrin; GIP neuroendocrine neoplasms; theranostics; radiolabeled peptides; somatostatin receptor antagonists; GLP-1R; exendin-4; CCK2; gastrin; GIP
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Fani, M.; Peitl, P.K.; Velikyan, I. Current Status of Radiopharmaceuticals for the Theranostics of Neuroendocrine Neoplasms. Pharmaceuticals 2017, 10, 30.

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