Drug intelligence / Profile preview

amphotericin B + itraconazole

Development stage
Preclinical
Lead developer
Complutense University of Madrid
Modality
Small Molecules
Administration
Oral
01

Overview

Amphotericin B + itraconazole is a fixed-dose combination of two antifungal agents, each with distinct mechanisms of action. Amphotericin B is a polyene antifungal that binds to ergosterol in fungal cell membranes, creating pores and causing cell death. Itraconazole is a triazole antifungal that inhibits the synthesis of ergosterol by blocking the enzyme lanosterol 14α-demethylase, disrupting membrane formation and function. This combination has been investigated for enhanced pharmacological effects and improved oral bioavailability, particularly in the treatment of invasive mycoses such as candidiasis and histoplasmosis. The formulation aims to leverage potential synergistic or additive effects against fungal pathogens; however, studies have reported both antagonistic interactions (notably in murine models of candidiasis) and possible benefits depending on disease context and formulation[1][2][4][5].

02

Targets

ErgosterolCYP51A1 (Sterol 14α-demethylase)

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