title: Pasireotide, a multi-somatostatin receptor ligand with potential efficacy for treatment of pituitary and neuroendocrine tumors.
abstract: Somatostatin receptors are an important target for medical treatment of pituitary and neuroendocrine tumors. To date, five somatostatin receptor (sst) subtypes have been identified. The currently available somatostatin analogues octreotide and lanreotide have predominantly affinity for sst2. Pasireotide is a sst multireceptor ligand with affinity for sst1, sst2, sst3 and sst5 and this broader binding profile may translate into a higher efficacy with respect to suppression of hormone production and cell growth in certain tumors. Experimental animal studies and in vitro studies with cultured tumor cells have shown that pasireotide strongly suppresses growth hormone and adrenocorticotropin production. In addition, pasireotide can influence tumor cell growth via effects on apoptosis and angiogenesis. In this review, the role of somatostatin receptors in pituitary and neuroendocrine tumors is briefly discussed followed by an overview of possible applications of pasireotide based on recent trials in patients with acromegaly, Cushing's disease and neuroendocrine tumors.
authors: Department of Internal Medicine, Section of Endocrinology, Erasmus Medical Center, Rotterdam, The Netherlands. r.feelders@erasmusmc.nl
authors: R A
authors: RA
authors: Feelders
authors: W W
authors: WW
authors: de Herder
authors: S J
authors: SJ
authors: Neggers
authors: A J
authors: AJ
authors: van der Lely
authors: L J
authors: LJ
authors: Hofland
mesh_terms: D000172:Acromegaly / Q000188:drug therapy; D006801:Humans; D008024:Ligands; D018358:Neuroendocrine Tumors / Q000188:drug therapy*; D047748:Pituitary ACTH Hypersecretion / Q000188:drug therapy; D010911:Pituitary Neoplasms / Q000188:drug therapy*; D017481:Receptors, Somatostatin / Q000378:metabolism*; D013004:Somatostatin / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000627:therapeutic use
chemical_list: D008024:Ligands; D017481:Receptors, Somatostatin; D013004:Somatostatin; C517782:pasireotide
keywords: Cushing's disease; Growth hormone release inhibitors; Pasireotide; SOM-230