Paltusotine

Storage temp: -20℃

Solubility: DMSO: 20 mg/mL (43.81 mM; ultrasonic and warming and heat to 60°C)

Form: Solid

Paltusotine, a somatostatin receptor agonist, reduces IGF-1 levels in acromegaly patients in a dose-dependent manner across the 20 to 60 mg therapeutic dose range. Paltusotine may inhibit gallbladder contractility and decrease bile secretion, potentially leading to gallbladder stones or sludge. Paltusotine can also cause changes in glucose metabolism, potentially resulting in hyperglycemia or, less commonly, hypoglycemia. Somatostatin analogs, including paltusotine, may suppress thyroid-stimulating hormone secretion, potentially leading to hypothyroidism. Additionally, they can inhibit pancreatic enzyme and bile acid secretion, potentially causing malabsorption of dietary fats and steatorrhea. Decreased vitamin B12 levels have also been observed.

Acromegaly is a hormonal disorder associated with excessive secretion of growth hormone (GH) and subsequent increase in the production of insulin-like growth factor I (IGF-I). Similar to the natural hormone somatostatin, paltusotine suppresses GH and IGF-1 secretion. Paltusotine exerts its pharmacological activity via selective agonism (>4000-fold) at somatostatin receptor 2 (SSTR2) and exhibits little or no affinity for other SST receptor subtypes. Paltusotine inhibited cyclic adenosine monophosphate accumulation via human SSTR2 activation with an average drug (agonist) concentration that results in half-maximal response (EC50) of 0.25 nM.