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bms-823778
- Development stage
- Phase 2
- Lead developer
- Bristol Myers Squibb
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
BMS-823778 is a potent and selective small molecule inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), an enzyme involved in tissue-specific intracellular glucocorticoid metabolism. It was developed by Bristol Myers Squibb as an oral therapy for metabolic disorders such as type 2 diabetes mellitus and hypercholesterolemia. The compound demonstrated high selectivity (>10,000-fold over 11β-HSD2), robust pharmacodynamic effects in preclinical models of obesity and diabetes, favorable pharmacokinetics including high adipose-to-plasma concentration ratio and good oral bioavailability. Clinical development reached phase II trials for metabolic indications but was discontinued[1][2][6].
- Other names
- 1140898-87-8UNII-C82R061MZ5UNII-C-82R061MZ5UNII-C 82R061MZ5(14C)BMS-8237782-(3-(1-(4-chlorophenyl)cyclopropyl)-(1,2,4)triazolo(4,3-a)pyridin-8-yl)propan-2-ol
02
Targets
HSD11B1 (11-beta-hydroxysteroid dehydrogenase type 1)
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