Drug intelligence / Profile preview

amphotericin B + fluconazole + micafungin

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

Overview

This is a combination of three antifungal agents—amphotericin B, fluconazole, and micafungin—used together for the treatment of severe or refractory fungal infections. - **Amphotericin B** is a polyene antifungal that binds to ergosterol in fungal cell membranes, creating pores that lead to cell death. It has broad-spectrum activity but notable toxicity. - **Fluconazole** is a triazole antifungal that inhibits the fungal cytochrome P450 enzyme 14α-demethylase, impairing ergosterol synthesis and thus disrupting membrane formation. - **Micafungin** is an echinocandin antifungal that inhibits β-(1,3)-D-glucan synthase, an enzyme essential for fungal cell wall synthesis. The rationale for combining these drugs includes broadening the spectrum of activity against various fungi (notably *Candida* and *Cryptococcus* species), overcoming resistance mechanisms, achieving synergistic effects in some cases (especially with amphotericin B plus micafungin or fluconazole), and potentially reducing individual drug toxicities by allowing lower doses[1][6][9]. This combination may be considered in complex or refractory cases where monotherapy has failed or resistance patterns are problematic.

02

Targets

ErgosterolCYP51A1 (Sterol 14α-demethylase)FKS (1,3-beta-D-glucan synthase component FKS1)

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