Drug intelligence / Profile preview

fluconazole + liposomal amphotericin b

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Oral, Intravenous
01

Overview

Fluconazole + liposomal amphotericin B is a combination antifungal therapy used primarily for the treatment of severe systemic fungal infections, including cryptococcal meningitis and other invasive mycoses. Fluconazole is a triazole antifungal that inhibits the fungal cytochrome P450 enzyme 14α-demethylase, thereby blocking ergosterol synthesis and disrupting cell membrane formation. Liposomal amphotericin B is a polyene antifungal encapsulated in liposomes to reduce toxicity; it binds to ergosterol in fungal cell membranes, creating pores that lead to cell death. The combination aims to leverage the broad-spectrum activity of amphotericin B with the oral availability and CNS penetration of fluconazole. However, their interaction can be concentration-dependent—at higher concentrations of fluconazole, antagonism may occur due to reduced ergosterol content impairing amphotericin B’s action[1]. This regimen is especially relevant for immunocompromised patients (e.g., those with HIV/AIDS) facing life-threatening mycoses.

Brand names
AmBisomeDiflucan
Other names
AmBisome + fluconazoleSingle-dose liposomal amphotericin B plus fluconazole
02

Targets

CYP51A1 (Sterol 14α-demethylase)Ergosterol

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