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Somatostatin Analogues in the Treatment of Neuroendocrine Tumors: Past, Present and Future
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Biological and Biochemical Basis of the Differential Efficacy of First and Second Generation Somatostatin Receptor Ligands in Neuroendocrine Neoplasms

1
Dipartimento di Medicina Interna & Centro di Eccellenza per la Ricerca Biomedica (CEBR), Università di Genova, 16132 Genova, Italy
2
Istituto di Ricerca e Cura a Carattere Scientifico (IRCCS) Ospedale Policlinico San Martino, 16132 Genova, Italy
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Int. J. Mol. Sci. 2019, 20(16), 3940; https://doi.org/10.3390/ijms20163940
Received: 1 January 1970 / Revised: 5 August 2019 / Accepted: 8 August 2019 / Published: 13 August 2019
(This article belongs to the Special Issue Somatostatin)
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PDF [1948 KB, uploaded 13 August 2019]
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Abstract

Endogenous somatostatin shows anti-secretory effects in both physiological and pathological settings, as well as inhibitory activity on cell growth. Since somatostatin is not suitable for clinical practice, researchers developed synthetic somatostatin receptor ligands (SRLs) to overcome this limitation. Currently, SRLs represent pivotal tools in the treatment algorithm of neuroendocrine tumors (NETs). Octreotide and lanreotide are the first-generation SRLs developed and show a preferential binding affinity to somatostatin receptor (SST) subtype 2, while pasireotide, which is a second-generation SRL, has high affinity for multiple SSTs (SST5 > SST2 > SST3 > SST1). A number of studies demonstrated that first-generation and second-generation SRLs show distinct functional properties, besides the mere receptor affinity. Therefore, the aim of the present review is to critically review the current evidence on the biological effects of SRLs in pituitary adenomas and neuroendocrine tumors, by mainly focusing on the differences between first-generation and second-generation ligands. View Full-Text
Keywords: somatostatin receptors; somatostatin receptor ligands; pituitary adenomas; neuroendocrine tumors somatostatin receptors; somatostatin receptor ligands; pituitary adenomas; neuroendocrine tumors
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Gatto, F.; Barbieri, F.; Arvigo, M.; Thellung, S.; Amarù, J.; Albertelli, M.; Ferone, D.; Florio, T. Biological and Biochemical Basis of the Differential Efficacy of First and Second Generation Somatostatin Receptor Ligands in Neuroendocrine Neoplasms. Int. J. Mol. Sci. 2019, 20, 3940.

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