Drug intelligence / Profile preview

echinocandin + fluconazole

Development stage
Preclinical
Lead developer
Merck
Modality
Peptides, Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination of two antifungal agents, an echinocandin (such as caspofungin, micafungin, or anidulafungin) and fluconazole. Echinocandins are a class of antifungal drugs that inhibit the synthesis of β-(1,3)-D-glucan in the fungal cell wall by noncompetitive inhibition of the enzyme 1,3-β-D-glucan synthase. This disrupts cell wall integrity and leads to fungal cell death or growth inhibition[6][8][10]. Fluconazole is a triazole antifungal that inhibits ergosterol synthesis in fungal cell membranes by targeting lanosterol 14α-demethylase[4]. The combination has been studied for potential additive or synergistic effects against Candida species and other fungi; however, clinical results have been mixed and often show no clear superiority over monotherapy with either agent[3][5]. Both drugs are used primarily for invasive candidiasis and other serious systemic fungal infections.

02

Targets

CYP51A1 (Sterol 14α-demethylase)FKS (1,3-beta-D-glucan synthase component FKS1)

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