SCO-240 SSTR5 antagonist

Somatostatin is a peptide hormone secreted by the pituitary gland, pancreas, and gastrointestinal endocrine cells that regulates the secretion of endocrine hormones via five G-protein-coupled receptors (Somatostatin receptor, SSTR1–5). We primarily focused on SSTR5 and identified SCO-240, an orally available selective SSTR5 antagonist. Despite extensive research, the in vivo physiological role of SSTR5 in humans remains unknown.

We conducted a Phase 1 trial in healthy individuals to evaluate the single-dose profile of SCO-240. Notably, SCO-240 stimulated a robust growth hormone (GH) secretion without affecting the secretion of other pituitary hormones. This is the first clinical report, which suggests that SSTR5 antagonist has a pivotal role in stimulating GH secretion in humans. Overall, SCO-240 is safe and well-tolerated and exhibits once-daily oral dosing potential. Collectively, SCO-240-mediated SSTR5 antagonism is a novel oral therapy for GH-related disorders, including pediatric GH deficiency (PGHD). In addition, research evidence suggests that SCO-240 may also be effective in treating female infertility and alopecia, and detailed information is available upon request.