BI 135585

BI 135585 is a potent, selective, and orally active small molecule inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), with an IC50 of approximately 13 nM and over a thousand-fold selectivity against other hydroxysteroid dehydrogenases. It was developed for the potential treatment of type 2 diabetes mellitus by reducing local glucocorticoid activation in metabolic tissues. Preclinical and early clinical studies demonstrated that it effectively inhibits hepatic and adipose tissue 11β-HSD1 activity, leading to changes in cortisol metabolism. The drug was well tolerated in healthy volunteers and patients with type 2 diabetes during phase I trials, showing dose-proportional pharmacokinetics and no major safety issues over short-term administration[1][4][6][8].

Other names

BI 135585 monohydrateBI135585 monohydrateBI-135585 monohydrate