Paltusotine (CRN00808) is an orally bioavailable, nonpeptide, somatostatin receptor subtype 2 (SST2) agonist with EC50 of 0.25 nM.
Paltusotine is >4000-fold selective for SST2 over other somatostatin receptor subtypes.
Paltusotine suppresses stimulated-GH and IGF-1 secretion in rats. Paltusotine suppresses GH and IGF-1 in a dose-dependent fashion, with a safety profile similar to currently approved SST2 receptor ligands.
Paltusotine is a promising once-daily oral nonpeptide SST2 agonist candidate for managing acromegaly and neuroendocrine tumors.
