Functional activity of the multiligand analog SOM230 at human recombinant somatostatin receptor subtypes supports its usefulness in neuroendocrine tumors.
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Schmid, Herbert and Schoeffter, Philippe (2004) Functional activity of the multiligand analog SOM230 at human recombinant somatostatin receptor subtypes supports its usefulness in neuroendocrine tumors. Neuroendocrinology, 80 Suppl 1. pp. 47-50. ISSN 0028-3835
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 sst(1,2,3) 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.
| Item Type: | Article |
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| Additional Information: | author can archive post-print (ie final draft post-refereeing); On author or institutional server; Publisher's version/PDF cannot be used |
| Keywords: | SOM230; Neuroendocrine tumors; Somatostatin; Acromegaly; Carcinoid |
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| Date Deposited: | 14 Dec 2009 13:55 |
| Last Modified: | 31 Jan 2013 01:08 |
| URI: | https://oak.novartis.com/id/eprint/722 |