Drug intelligence / Profile preview

MGCD290 + fluconazole

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

MGCD290 + fluconazole is an investigational **oral combination product** consisting of MGCD290, a first-in-class small molecule inhibitor of the fungal enzyme **Hos2 histone deacetylase (HDAC)**, and **fluconazole**, a widely used triazole antifungal. MGCD290 is developed to enhance fluconazole’s antifungal activity, overcoming both primary and acquired fluconazole resistance in various fungal species. In vitro and early clinical studies, the combination demonstrated **broad antifungal synergy**, especially against azole-resistant yeasts and molds, including *Candida*, *Aspergillus*, *Zygomycetes*, and others. The combination has completed multiple Phase I trials in healthy volunteers, showing a good safety and pharmacokinetic profile, and is in Phase II trials for moderate-to-severe vulvovaginal candidiasis. MGCD290 is being developed by MethylGene.

02

Targets

Hos2 (Fungal histone deacetylase Hos2)CYP51A1 (Sterol 14α-demethylase)

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