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Sixty years of Amphotericin B: An Overview of the Main Antifungal Agent Used to Treat Invasive Fungal Infections

Journal

INFECTIOUS DISEASES AND THERAPY
Volume 10, Issue 1, Pages 115-147

Publisher

SPRINGER LONDON LTD
DOI: 10.1007/s40121-020-00382-7

Keywords

Fungal disease; Lipid formulation; Polyenes; Safety; Tolerability

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Polyenes, the oldest family of antifungal drugs introduced in the late 1950s, remain useful in the treatment of invasive fungal diseases due to their broad spectrum of activity, low resistance rate, and excellent clinical and pharmacological action despite their toxic potential. Focus has been placed on developing new products to minimize the known toxicity of the conventional drug.
Introduced in the late 1950s, polyenes represent the oldest family of antifungal drugs. The discovery of amphotericin B and its therapeutic uses is considered one of the most important scientific milestones of the twentieth century . Despite its toxic potential, it remains useful in the treatment of invasive fungal diseases owing to its broad spectrum of activity, low resistance rate, and excellent clinical and pharmacological action. The well-reported and defined toxicity of the conventional drug has meant that much attention has been paid to the development of new products that could minimize this effect. As a result, lipid-based formulations of amphotericin B have emerged and, even keeping the active principle in common, present distinct characteristics that may influence therapeutic results. This study presents an overview of the pharmacological properties of the different formulations for systemic use of amphotericin B available for the treatment of invasive fungal infections, highlighting the characteristics related to their chemical, pharmacokinetic structures, drug-target interactions, stability, and others, and points out the most relevant aspects for clinical practice.

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