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. This combination may be considered in complex or refractory cases where monotherapy has failed or resistance patterns are problematic.

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Targets

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