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      Biological and Biochemical Basis of the Differential Efficacy of First and Second Generation Somatostatin Receptor Ligands in Neuroendocrine Neoplasms

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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 (SST 5 > SST 2 > SST 3 > SST 1). 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.

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          Lanreotide in metastatic enteropancreatic neuroendocrine tumors.

          Martyn Caplin, Marianne Pavel, Jarosław B. Ćwikła … (2014)
          Somatostatin analogues are commonly used to treat symptoms associated with hormone hypersecretion in neuroendocrine tumors; however, data on their antitumor effects are limited. We conducted a randomized, double-blind, placebo-controlled, multinational study of the somatostatin analogue lanreotide in patients with advanced, well-differentiated or moderately differentiated, nonfunctioning, somatostatin receptor-positive neuroendocrine tumors of grade 1 or 2 (a tumor proliferation index [on staining for the Ki-67 antigen] of <10%) and documented disease-progression status. The tumors originated in the pancreas, midgut, or hindgut or were of unknown origin. Patients were randomly assigned to receive an extended-release aqueous-gel formulation of lanreotide (Autogel [known in the United States as Depot], Ipsen) at a dose of 120 mg (101 patients) or placebo (103 patients) once every 28 days for 96 weeks. The primary end point was progression-free survival, defined as the time to disease progression (according to the Response Evaluation Criteria in Solid Tumors, version 1.0) or death. Secondary end points included overall survival, quality of life (assessed with the European Organization for Research and Treatment of Cancer questionnaires QLQ-C30 and QLQ-GI.NET21), and safety. Most patients (96%) had no tumor progression in the 3 to 6 months before randomization, and 33% had hepatic tumor volumes greater than 25%. Lanreotide, as compared with placebo, was associated with significantly prolonged progression-free survival (median not reached vs. median of 18.0 months, P<0.001 by the stratified log-rank test; hazard ratio for progression or death, 0.47; 95% confidence interval [CI], 0.30 to 0.73). The estimated rates of progression-free survival at 24 months were 65.1% (95% CI, 54.0 to 74.1) in the lanreotide group and 33.0% (95% CI, 23.0 to 43.3) in the placebo group. The therapeutic effect in predefined subgroups was generally consistent with that in the overall population, with the exception of small subgroups in which confidence intervals were wide. There were no significant between-group differences in quality of life or overall survival. The most common treatment-related adverse event was diarrhea (in 26% of the patients in the lanreotide group and 9% of those in the placebo group). Lanreotide was associated with significantly prolonged progression-free survival among patients with metastatic enteropancreatic neuroendocrine tumors of grade 1 or 2 (Ki-67 <10%). (Funded by Ipsen; CLARINET ClinicalTrials.gov number, NCT00353496; EudraCT 2005-004904-35.).
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            Acromegaly: an endocrine society clinical practice guideline.

            Laurence Katznelson, Edward Laws, Shlomo Melmed … (2014)
            The aim was to formulate clinical practice guidelines for acromegaly.
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              Medical progress: Acromegaly.

              Shlomo Melmed (2006)
              Article 0 comments Cited 277 times – based on 0 reviews     Review now
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                Author and article information

                Journal
                Journal ID (nlm-ta): Int J Mol Sci
                Journal ID (iso-abbrev): Int J Mol Sci
                Journal ID (publisher-id): ijms
                Title: International Journal of Molecular Sciences
                Publisher: MDPI
                ISSN (Electronic): 1422-0067
                Publication date (Electronic): 13 August 2019
                Publication date Collection: August 2019
                Volume: 20
                Issue: 16
                Electronic Location Identifier: 3940
                Affiliations
                [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 notes
                [* ]Correspondence: tullio.florio@ 123456unige.it ; Tel.: +90-0103-5388-06
                [†]

                These authors contributed equally to this work.

                Author information
                https://orcid.org/0000-0002-5062-9208
                https://orcid.org/0000-0001-8988-6896
                https://orcid.org/0000-0002-2394-996X
                Article
                Publisher ID: ijms-20-03940
                DOI: 10.3390/ijms20163940
                PMC ID: 6720449
                PubMed ID: 31412614
                SO-VID: 27e6adfb-c8e0-4102-b399-1a5ff50fca3e
                Copyright © © 2019 by the authors.
                License:

                Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( http://creativecommons.org/licenses/by/4.0/).

                History
                Date received : 01 January 1970
                Date accepted : 08 August 2019
                Categories
                Subject: Review

                ScienceOpen disciplines: Molecular biology
                Keywords: somatostatin receptors,somatostatin receptor ligands,pituitary adenomas,neuroendocrine tumors
                Data availability:
                ScienceOpen disciplines: Molecular biology
                Keywords: somatostatin receptors, somatostatin receptor ligands, pituitary adenomas, neuroendocrine tumors

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