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BVT.2733 is a small molecule, non-steroidal, isoform-selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), specifically optimized for the murine enzyme. Developed by Biovitrum, it served as a critical proof-of-concept compound to demonstrate that selective inhibition of 11β-HSD1 could lower blood glucose and improve insulin sensitivity in hyperglycemic and hyperinsulinemic mouse models. The enzyme 11β-HSD1 converts inactive glucocorticoids into active forms (e.g., cortisone to cortisol), and its overactivity is linked to metabolic disturbances. While BVT.2733 was primarily used in preclinical research, its development paved the way for human-active clinical candidates like BVT.3498.
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