Drug intelligence / Profile preview

mifepristone + itraconazole

Development stage
Discontinued
Lead developer
Danco Laboratories
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of two small-molecule pharmaceuticals: **mifepristone**, a selective antagonist of the progesterone receptor and glucocorticoid receptor, primarily indicated for the medical termination of intrauterine pregnancy and for controlling hyperglycemia secondary to hypercortisolism in Cushing’s syndrome; and **itraconazole**, a triazole antifungal agent used to treat various systemic and superficial fungal infections by inhibiting the synthesis of ergosterol, a key component of fungal cell membranes. There is no recognized fixed-dose or branded pharmaceutical product that combines these two drugs, but they may rarely be used concomitantly in complex cases. Their co-administration is associated with significant pharmacokinetic interaction risks: itraconazole, a strong inhibitor of CYP3A4, can markedly increase mifepristone exposure, while mifepristone itself inhibits multiple CYP enzyme systems and prolongs QTc. Their combination is not recommended unless absolutely necessary due to the risk of adverse effects, including increased risk of QT prolongation, hazardous increases in systemic exposure, and more acute monitoring needs[1][2][3][5].

02

Targets

GR (Glucocorticoid receptor)CYP3A4 (Cytochrome P450 3A4)CYP51A1 (Sterol 14α-demethylase)PR (Progesterone receptor)

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