Somatostatin (SRIF) eptidomimetic with high affinity for somatostatin receptor subtypes STT1/2/3/5 and in vivo efficacy for suppressing GH secretion.
Pasireotide (SOM230) is a somatostatin (somatotropin release inhibiting factor, SRIF) eptidomimetic with high affinity for somatostatin receptor subtypes STT1/2/3/5 (IC50 = 9.3/1/1.5/0.16 nM), but not STT4 (IC50 > 1 μM). SOM230 potently inhibits the growth hormone (GH) releasing hormone (GHRH)-induced GH release in primary r at pituitary cultures (IC50 = 0:4 nM) and suppresses the secretion of GH, insulin and glucagon in rats in vivo (ED50 in μg/kg post 1h administration via s.c. = 0.22, 3.4, 74, respectively; GH ED50 post 6h = 5.5 μg/kg).
