Description: Pasireotide (SOM230; Signifor) is a cyclohexapeptide-based somatostatin mimic approved for the treatment of Cushing's disease. It exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively). It is an orphan drug approved for the treatment of Cushing's disease in patients who fail or are ineligible for surgical therapy. It was developed by Novartis. Pasireotide is a somatostatin analogue with a 40-fold increased affinity to somatostatin receptor 5 compared to other somatostatin analogues.
References:
[1].A novel somatostatin mimic with broad somatotropin release
inhibitory factor receptor binding and superior therapeutic potential. J
Med Chem. 2003 Jun 5;46(12):2334-44.
[2].The novel somatostatin analog SOM230 is a potent inhibitor
of hormone release by growth hormone- and prolactin-secreting pituitary
adenomas in vitro. J Clin Endocrinol Metab. 2004 Apr;89(4):1577-85.
[3].The novel somatostatin ligand (SOM230) regulates human and
rat anterior pituitary hormone secretion. J Clin Endocrinol Metab. 2004
Jun;89(6):3027-32.
[4].Pasireotide (SOM230) is effective for the treatment of
pancreatic neuroendocrine tumors (PNETs) in a multiple endocrine
neoplasia type 1 (MEN1) conditional knockout mouse model. Surgery. 2012
Dec;152(6):1068-77.
[5].Differential antiinflammatory and antinociceptive effects of
the somatostatin analogs octreotide and pasireotide in a mouse model of
immune-mediated arthritis. Arthritis Rheum. 2011 Aug;63(8):2352-62.
Related CAS #: 396091-76-2 (acetate) 396091-79-5 (pamoate) 396091-73-9 (free base) 820232-50-6 (diaspartate)