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Table of Contents
Vol. 80, Suppl. 1, 2004
Issue release date: October 2004
Section title: Paper
Neuroendocrinology 2004;80(suppl 1):47–50
(DOI:10.1159/000080741)

Functional Activity of the Multiligand Analog SOM230 at Human Recombinant Somatostatin Receptor Subtypes Supports Its Usefulness in Neuroendocrine Tumors

Schmid H.A. · Schoeffter P.
Novartis Institutes for Biomedical Research, Novartis Pharma AG, Oncology and Neuroscience Research, WSJ.386.425, Basel, Switzerland

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Article / Publication Details

First-Page Preview
Abstract of Paper

Published online: October 15, 2004
Issue release date: October 2004

Number of Print Pages: 4
Number of Figures: 1
Number of Tables: 2

ISSN: 0028-3835 (Print)
eISSN: 1423-0194 (Online)

For additional information: http://www.karger.com/NEN

Abstract

Functional gastroenteropancreatic tumors express all 5 somatostatin receptor subtypes (sst) in different quantities. Octreotide and lanreotide treat patients with these tumors by binding preferentially to sst2 and, to a lesser extent, to sst3 and sst5 receptors, thereby controlling prominent symptoms caused by hormone hypersecretion (diarrhea and flushing). Although symptoms initially improve in most patients, a loss of response occurs in about 50% during continuous treatment. The functional activity at sst receptors of SOM230, a new multiligand somatostatin analog, has been described and compared with that of somatostatin (SRIF-14) and octreotide. These data show that SOM230 is a full agonist with nanomolar potency at sst1,2,3 and sst5 receptors. The multiligand activity profile of SOM230, together with its nondesensitizing inhibitory effect on growth hormone and insulin-like growth factor-I secretion in rats, may underlie its successful use in clinical trials and its potential for use in refractory patients with carcinoid tumors.

© 2004 S. Karger AG, Basel


Article / Publication Details

First-Page Preview
Abstract of Paper

Published online: October 15, 2004
Issue release date: October 2004

Number of Print Pages: 4
Number of Figures: 1
Number of Tables: 2

ISSN: 0028-3835 (Print)
eISSN: 1423-0194 (Online)

For additional information: http://www.karger.com/NEN


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Drug Dosage: The authors and the publisher have exerted every effort to ensure that drug selection and dosage set forth in this text are in accord with current recommendations and practice at the time of publication. However, in view of ongoing research, changes in government regulations, and the constant flow of information relating to drug therapy and drug reactions, the reader is urged to check the package insert for each drug for any changes in indications and dosage and for added warnings and precautions. This is particularly important when the recommended agent is a new and/or infrequently employed drug.
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