molecules of the month


oral, non-peptide SST2 agonist

Ph. III for acromegaly + Ph. II for NETs

in-house focused library screen + opt.

ACS Med. Chem. Lett., December 10, 2022

Crinetics Pharmaceuticals, San Diego, CA

paltusotine chemical structure oral, non-peptide SST2 agonist - Crinetics Pharmaceuticals, San Diego, CA
5 mins read

Toward an oral, once-daily non-peptide STT2 agonist. Paltusotine a novel oral somatostatin receptor 2 (SST2) agonist and Crinetics’ lead investigational drug (WO2022251212A2), is intended to treat acromegaly and neuroendocrine tumors (NETs) in carcinoid syndrome. Both diseases have been treated with surgery and injectable somatostatin analogues for disease control, such as octreotide (Sandostatin), lanreotide (Somatuline), targeting somatostatin receptor subtype 2 (SST2) and pasireotide (Signifor), targeting SST5. Although some of these peptide injectables are long-acting (monthly), delivered IM or SC, the burden of injectables detrimentally affects patient quality of life and treatment adherence. An oral option would be preferable for patients as evidenced by the fact that in Ph. II studies, paltusotine administered as a once-daily oral medication was preferred by 89%…

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