Drug intelligence / Profile preview

azd8329

Development stage
Phase 1
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

AZD8329 is a potent and selective small molecule inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), an enzyme that converts inactive glucocorticoids into their active forms. It demonstrates high selectivity for 11β-HSD1 over related enzymes such as 11β-HSD2, 17β-HSD1, and 17β-HSD3. In preclinical studies, AZD8329 showed strong inhibition of human recombinant and adipocyte-derived 11β-HSD1 with low nanomolar IC50 values. The drug was developed primarily for metabolic indications such as type 2 diabetes mellitus and obesity. It is orally administered and has low central nervous system penetration[1][4][5]. Clinical development reached phase I trials in healthy volunteers, overweight individuals, and patients with type 2 diabetes mellitus[2][5].

Other names
4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid
02

Targets

HSD11B1 (11-beta-hydroxysteroid dehydrogenase type 1)

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