Antifungal Drugs

We reviewed the licensed antifungal drugs and summarized their mechanisms of action, pharmacological profiles, and susceptibility to specific fungi. Approved antimycotics inhibit 1,3-&#946;-<span style="font-variant: small-caps;">d</span>-glucan synthase, lanosterol 14-&...

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Main Authors: Jiří Houšť, Jaroslav Spížek, Vladimír Havlíček
Format: Article
Language:English
Published: MDPI AG 2020-03-01
Series:Metabolites
Subjects:
Online Access:https://www.mdpi.com/2218-1989/10/3/106
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author Jiří Houšť
Jaroslav Spížek
Vladimír Havlíček
author_facet Jiří Houšť
Jaroslav Spížek
Vladimír Havlíček
author_sort Jiří Houšť
collection DOAJ
description We reviewed the licensed antifungal drugs and summarized their mechanisms of action, pharmacological profiles, and susceptibility to specific fungi. Approved antimycotics inhibit 1,3-&#946;-<span style="font-variant: small-caps;">d</span>-glucan synthase, lanosterol 14-&#945;-demethylase, protein, and deoxyribonucleic acid biosynthesis, or sequestrate ergosterol. Their most severe side effects are hepatotoxicity, nephrotoxicity, and myelotoxicity. Whereas triazoles exhibit the most significant drug&#8722;drug interactions, echinocandins exhibit almost none. The antifungal resistance may be developed across most pathogens and includes drug target overexpression, efflux pump activation, and amino acid substitution. The experimental antifungal drugs in clinical trials are also reviewed. Siderophores in the Trojan horse approach or the application of siderophore biosynthesis enzyme inhibitors represent the most promising emerging antifungal therapies.
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spelling doaj.art-cf9b50680ec2431686ae85112b9b06e12022-12-21T21:11:38ZengMDPI AGMetabolites2218-19892020-03-0110310610.3390/metabo10030106metabo10030106Antifungal DrugsJiří Houšť0Jaroslav Spížek1Vladimír Havlíček2Institute of Microbiology of the Czech Academy of Sciences, Vídeňská 1083, 14220 Prague, Czech RepublicInstitute of Microbiology of the Czech Academy of Sciences, Vídeňská 1083, 14220 Prague, Czech RepublicInstitute of Microbiology of the Czech Academy of Sciences, Vídeňská 1083, 14220 Prague, Czech RepublicWe reviewed the licensed antifungal drugs and summarized their mechanisms of action, pharmacological profiles, and susceptibility to specific fungi. Approved antimycotics inhibit 1,3-&#946;-<span style="font-variant: small-caps;">d</span>-glucan synthase, lanosterol 14-&#945;-demethylase, protein, and deoxyribonucleic acid biosynthesis, or sequestrate ergosterol. Their most severe side effects are hepatotoxicity, nephrotoxicity, and myelotoxicity. Whereas triazoles exhibit the most significant drug&#8722;drug interactions, echinocandins exhibit almost none. The antifungal resistance may be developed across most pathogens and includes drug target overexpression, efflux pump activation, and amino acid substitution. The experimental antifungal drugs in clinical trials are also reviewed. Siderophores in the Trojan horse approach or the application of siderophore biosynthesis enzyme inhibitors represent the most promising emerging antifungal therapies.https://www.mdpi.com/2218-1989/10/3/106antifungal drugsamphotericin bflucytosinetriazolesechinocandinsinvasive fungal infectionsresistancesiderophores
spellingShingle Jiří Houšť
Jaroslav Spížek
Vladimír Havlíček
Antifungal Drugs
Metabolites
antifungal drugs
amphotericin b
flucytosine
triazoles
echinocandins
invasive fungal infections
resistance
siderophores
title Antifungal Drugs
title_full Antifungal Drugs
title_fullStr Antifungal Drugs
title_full_unstemmed Antifungal Drugs
title_short Antifungal Drugs
title_sort antifungal drugs
topic antifungal drugs
amphotericin b
flucytosine
triazoles
echinocandins
invasive fungal infections
resistance
siderophores
url https://www.mdpi.com/2218-1989/10/3/106
work_keys_str_mv AT jirihoust antifungaldrugs
AT jaroslavspizek antifungaldrugs
AT vladimirhavlicek antifungaldrugs