BVT-2733 is a selective 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor, which attenuates obesity and inflammation in diet-induced obese mice. BVT-2733 protects osteoblasts against endogenous glucocorticoid induced dysfunction. BVT-2733 exhibits an anti-inflammatory effect on CIA. This protective effect is, at least partly, mediated by inhibition of the NF-κB and NLRP1 inflammasome signaling pathways. 11β-Hydroxysteroid dehydrogenase 1 (11β-HSD1) plays an important role in inflammation. 11β-HSD1 inhibition may represent a potential therapeutic target for RA patients.