pasireotide-pamoate

Description: Pasireotide pamoate, formerly known as SOM230, is a potent and stable cyclohexapeptide somatostatin mimic that 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. Lewis I, et al. 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. Hofland LJ, et al. 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. Murray RD, et al. The novel somatostatin ligand (SOM230) regulates human and rat anterior pituitary hormone secretion. J Clin Endocrinol Metab. 2004 Jun; 89(6):3027-32.

4. Quinn TJ, et al. 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. Imhof AK, et al. 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) 396091-73-9 (free base) 396091-79-5 (pamoate) 820232-50-6 (diaspartate)