Somatostatin and somatostatin analogues: diagnostic and therapeutic uses.
Somatostatin and its octapeptide analogues exert their effects through interaction with somatostatin receptor (sst) subtypes 1 through 5 (sst 1-5 ). Somatostatin binds with high affinity to all sst subtypes, whereas the currently commercially available octapeptide analogues bind only with a high affinity to sst 2 and sst 5. Pituitary tumors, endocrine pancreatic tumors, and carcinoid tumors express multiple sst subtypes, but sst 2 predominance is found in 90% of carcinoids and 80% of endocrine pancreatic tumors. Sst 2 and sst 5 predominance is found in growth hormone-secreting pituitary tumors. In patients harboring sst 2 - or sst 5 -positive neuroendocrine tumors, clinical symptomatology can be controlled by the chronic administration of one of the currently commercially available octapeptide somatostatin analogues. Tumors and metastases that bear sst 2 or sst 5 can be visualized in vivo after injection of radiolabeled octapeptide analogues. Radiolabeled octapeptide analogues can also be used for radiotherapy of sst 2 - and sst 5 -positive advanced or metastatic neuroendocrine tumors.
de Herder
Wouter W
WW
Division of Endocrinology, Department of Internal Medicine, University Hospital, Erasmus Medical Center Rotterdam, Rotterdam, The Netherlands. deherder@inw3.azr.nl
Lamberts
Steven W J
SW
D018931:Antineoplastic Agents, Hormonal / Q000627:therapeutic use*; D005544:Forecasting; D006801:Humans; D018358:Neuroendocrine Tumors / Q000175:diagnosis / Q000000981:diagnostic imaging / Q000628:therapy*; D015282:Octreotide / Q000627:therapeutic use*; D010456:Peptides, Cyclic / Q000627:therapeutic use*; D011877:Radionuclide Imaging; D017481:Receptors, Somatostatin / Q000187:drug effects / Q000502:physiology; D013004:Somatostatin / Q000031:analogs & derivatives / Q000737:chemistry / Q000627:therapeutic use*
D018931:Antineoplastic Agents, Hormonal; D010456:Peptides, Cyclic; D017481:Receptors, Somatostatin; C060347:lanreotide; D013004:Somatostatin; C081788:pentetreotide; D015282:Octreotide