molecules of the month


oral tissue-targeting 11β-HSD1 inhibitor

Ph. II in T2DM/obesity completed (QD)

scaffold-hopping from cortisone and prior 11β-HSD1 inh

Bioorg. Med. Chem. Lett.

Incyte Research Institute, Wilmington, DE

INCB13739 Chemical Structure, oral tissue-targeting 11β-HSD1 inhibitor - Incyte Research Institute, Wilmington, DE
5 mins read

Context. INCB13739 (Incyte) is an oral 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) antagonist. Inhibition of the tissue-specific generation of cortisol using agents that antagonize 11β-HSD1, the key metabolic enzyme involved in the conversion of inactive glucocorticoids to active ones, has been considered a desirable therapeutic strategy for type 2 diabetes and metabolic syndrome. Indeed, at least 25 compounds from natural or synthetic sources have been evaluated in preclinical and some Ph. I-II studies over the last decade, although none have progressed to Ph. III studies. Early clinical data reported by Incyte scientists have demonstrated the successful reduction of HbA1C and fasting plasma glucose levels by INCB13739, while the compound was also found to improve hyperlipidemia and hypertriglyceridemia; however, the molecule appears to…

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