PMID: 16625843Apr 22, 2006Paper

Pre-clinical and clinical experiences with novel somatostatin ligands: advantages, disadvantages and new prospects

Journal of Endocrinological Investigation
Leo J HoflandS W J Lamberts

Abstract

Since the cloning and characterization of the five human somatostatin receptor (SSTR) subtypes, our understanding of the expression and functional role of the five SSTR subtypes in human (neuro-)endocrine tumors has increased significantly. The majority of human (neuro-)endocrine tumors express multiple SSTR. GH-secreting pituitary adenomas preferentially express SSTR2 and SSTR5, prolactinomas SSTR1 and SSTR5, and corticotroph adenomas express SSTR2 (low number) and predominantly SSTR5s. In addition, gastroenteropancreatic (GEP) neuroendocrine tumors frequently express multiple SSTR as well, with SSTR2 being expressed at the highest level. Treatment with the current generation of octapeptide somatostatin-analogs, e.g. octreotide and lanreotide, normalizes circulating GH- and IGF-I levels in approximately 60-70% of acromegalic patients, thereby remaining about one-third of patients uncontrolled. In patients with GEP neuroendocrine tumors, both somatostatin-analogs effectively suppress the production of bioactive peptides and hormones by the tumor cells, resulting in an important improvement of the related clinical symptomatology. However, a considerable proportion of patients experience an escape from treatment within months to ...Continue Reading

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