Drug intelligence / Profile preview

glyburide + fluconazole

Development stage
Unknown
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination of two approved small molecule drugs, glyburide and fluconazole. Glyburide is a second-generation sulfonylurea used to improve glycemic control in adults with type 2 diabetes mellitus by stimulating insulin secretion from pancreatic beta cells through closure of ATP-sensitive potassium channels. Fluconazole is a triazole antifungal agent that inhibits fungal cytochrome P450 enzyme 14α-demethylase, impairing ergosterol synthesis and thus inhibiting fungal cell membrane formation. There is no fixed-dose combination product marketed under this name; however, co-administration may occur clinically. Notably, fluconazole can increase serum concentrations of glyburide by inhibiting its metabolism, raising the risk for hypoglycemia[1][3][6].

02

Targets

SUR1 (Sulfonylurea receptor 1)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)CYP51A1 (Sterol 14α-demethylase)

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