levoketoconazole + metformin

**levoketoconazole + metformin** refers to the coadministration of two small-molecule drugs, levoketoconazole (Recorlev) and metformin (Glucophage). Levoketoconazole is a stereoisomer of ketoconazole and acts as a cortisol synthesis inhibitor by blocking enzymes involved in corticosteroid production, particularly 11β-hydroxylase, for the treatment of endogenous hypercortisolemia in adults with Cushing’s syndrome who are not candidates for surgery or in whom surgery has failed[3][2][5]. Metformin is a biguanide class antihyperglycemic agent widely used as first-line therapy for type 2 diabetes, primarily reducing hepatic glucose production and increasing insulin sensitivity. Combined use is not a distinct marketed product but occurs frequently in Cushing’s syndrome patients with comorbid diabetes; levoketoconazole can improve glycemic parameters such as HbA1c and fasting glucose[2][4]. However, levoketoconazole inhibits multiple transporters (OCT2, MATE1) and CYP enzymes, which increases metformin plasma concentration and risk of metformin-related adverse effects, thus requiring close monitoring of glucose levels, kidney function, and B12[3][1][5].

Other names

levoketoconazolemetformin