levoketoconazole

Levoketoconazole is the levorotatory (2S,4R) enantiomer of ketoconazole and acts as a steroidogenesis inhibitor. It is used for the treatment of endogenous hypercortisolemia in adults with Cushing's syndrome who cannot undergo surgery or whose surgery was not curative. Levoketoconazole works by inhibiting multiple steroidogenic enzymes involved in cortisol biosynthesis, including CYP11B1 (11β-hydroxylase), CYP17A1 (17α-hydroxylase/17,20 lyase), and CYP21A2 (21-hydroxylase). This results in reduced glucocorticoid production and circulating cortisol levels. The drug also inhibits other enzymes such as CYP11A1 and CYP51A1 more potently than racemic ketoconazole. Levoketoconazole is associated with a lower risk of hepatotoxicity compared to racemic ketoconazole but still carries significant risks including serious liver injury and QT interval prolongation[3][6][7]. It was developed by Strongbridge Biopharma, now part of Xeris Pharmaceuticals.

Brand names

Recorlev

Other names

(2S,4R)-ketoconazoleNormoCort