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BI 187004 is a selective, orally available small molecule inhibitor of the enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), which catalyzes the conversion of inactive cortisone to active cortisol in tissues such as liver and adipose tissue. By inhibiting this enzyme, BI 187004 reduces local cortisol production, aiming to improve insulin sensitivity and metabolic parameters. It was developed for potential use in metabolic disorders including type 2 diabetes mellitus and obesity. Clinical studies demonstrated that it achieves significant inhibition of its target with once-daily dosing and is generally well tolerated; however, despite complete target engagement, no clinically relevant therapeutic effects were observed in trials[3][4][6][8].
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