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SOM230

Pasireotide

A multiligand somatostatin analogue

Somatostatin is a peptide hormone expressed in many tissues throughout the body. It regulates the release of hormones such as Growth Hormone (GH), glucagons, insulin, gastrin, secretin, and Thyroid-Stimulating Hormone (TSH). Somatostatin inhibitors block GH release.¹

The potential of somatostatin analogues as cancer therapies has recently been explored following demonstration of antineoplastic activity of these compounds in a variety of experimental models in vitro and in vivo.²

Pasireotide is the next generation in somatostatin analogues. This multiligand-targeting agent is currently in Phase III development for acromegaly Gastroenteropancreatic Neuroendocrine Tumors (GEP/NET) and Cushing's disease.

Pasireotide exhibits a broad spectrum of somatostatin receptor activation. Compared with octreotide in vitro, pasireotide has far higher binding affinity for sst-1 (20 to 30 times), sst-3 (5 times), and sst-5 receptors (40 to 100 times) and a comparable affinity for sst-2 receptors.¹

1. Bruns C, Lewis I, Briner U, Meno-Tetang G, Weckbecker G. SOM230: a novel somatostatin peptidomimetic with broad somatotropin release inhibiting factor (SRIF) receptor binding and a unique antisecretory profile. Eur J Endocrinol. 2002;146:707-716.
2. Hejna M, Schmidinger M, Raderer M. The clinical role of somatostatin analogues as antineoplastic agents: much ado about nothing? Ann Oncol. 2002;13:653-668.
3. Adams RL, Adams IP, Zhong W, Atkin SL. Inhibition of endothelial proliferation by the new somatostatin analog, SOM230, and expression of somatostatin receptors in proliferating and quiescent endothelium. Presented at: The 85th Annual Meeting of the Endocrine Society. June 19-22, 2003; Philadelphia, Pa. Abstract P3-371.