Pasireotide (SOM230) acetate is a long-acting cyclohexapeptide somatostatin analogue that enhances agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5). It can suppress growth hormone, IGF-I, and ACTH secretion, indicating potential efficacy in treating acromegaly and Cushing's disease. This compound also demonstrates antisecretory, antiproliferative, and proapoptotic activities.
- Exhibits unique high-affinity binding to human somatostatin receptors.
- Effectively inhibits growth hormone releasing hormone (GHRH) induced growth hormone (GH) release in primary cultures of rat pituitary cells.
- Significantly decreases serum insulin and increases serum glucose.
- Reduces tumor size and increases apoptosis.
- Exerts antinociceptive and antiinflammatory actions via the SSTR2 receptor.