Drug intelligence / Profile preview

fluconazole + nystatin + amphotericin B

Development stage
Preclinical
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Oral, Topical, Intrathecal
01

Overview

This is a combination of three antifungal agents—fluconazole, nystatin, and amphotericin B—each with distinct mechanisms of action. Fluconazole is a triazole antifungal that inhibits fungal cytochrome P450-dependent enzyme lanosterol 14-α-demethylase, disrupting ergosterol synthesis and compromising cell membrane integrity. Nystatin and amphotericin B are both polyene antimycotics; they bind to ergosterol in the fungal cell membrane, forming pores that increase membrane permeability and lead to cell death. This combination would theoretically provide broad-spectrum coverage against various fungal pathogens by targeting different steps in the fungal cell membrane pathway[4][5][6][7]. Such combinations may be considered for severe or refractory mycotic infections but are not standard due to potential drug interactions, toxicity risks (notably with amphotericin B), and overlapping spectra[2][4].

02

Targets

ErgosterolCYP51A1 (Sterol 14α-demethylase)

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