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C203214Level 4

Clofutriben

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable selective inhibitor of the enzyme 11beta-hydroxysteroid dehydrogenase type 1 (11b-HSD1; 11bHSD1; HSD11B1; HSD1; HSD-1), with potential protective activity for disorders of corticosteroid excess. Upon oral administration, clofutriben selectively binds to and inhibits the activity of HSD-1. This prevents the conversion of cortisone to the active hormone cortisol and thereby preventing the activation of the glucocorticoid receptors (GRs). By blocking cortisol production in metabolic tissues, clofutriben may inhibit the adverse metabolic effects that are caused by exogenous administration of glucocorticoids or in disorders in which cortisol is secreted in excess. HSD-1 is highly expressed in metabolic tissues, such as liver, skeletal muscle, and adipose tissue. It plays a crucial role in regulating the production of cortisol to activate the GRs.

**Synonyms:** - 11beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitor SPI-62 - AS2473662 - ASP 3662 - ASP-3662 - ASP3662 - CLOFUTRIBEN - HDD-1697 - SPI 62 - SPI-62 - SPI62

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