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Tissue pharmacokinetics of antifungal drugs: A review

Felix Bergmann1, Marlene Prager1, Lena Pracher1

  • 1Department of Clinical Pharmacology, Medical University of Vienna, Vienna, Austria.

International Journal of Antimicrobial Agents
|February 14, 2026
PubMed

Insights

Plasma drug levels may not predict antifungal drug exposure in tissues for invasive fungal infections. Tissue pharmacokinetics (PK) are crucial for optimizing antifungal dosing and treatment success in critically ill patients.

Area of Science:

  • Pharmacology
  • Infectious Diseases
  • Clinical Pharmacy

Background:

  • Invasive fungal infections pose significant risks, especially for immunocompromised individuals.
  • Current antifungal drug dosing relies heavily on plasma pharmacokinetics (PK).
  • Plasma PK may not accurately represent drug concentrations at infection sites, impacting treatment efficacy.

Purpose of the Study:

  • To review clinical data on the tissue pharmacokinetics (PK) of approved antifungal agents.
  • To compare tissue penetration of various antifungal drug classes.
  • To highlight the importance of tissue drug exposure in guiding antifungal therapy.

Main Methods:

  • Systematic literature search of PubMed for prospective human trials up to July 2025.
  • Included studies reporting both plasma and tissue drug concentrations.
  • Focused on approved antifungal agents: triazoles, echinocandins, amphotericin B, and flucytosine.

Main Results:

  • Significant variability observed in antifungal drug penetration across different tissues and compartments.
  • Tissue drug concentrations did not always correlate with plasma PK profiles.
  • Drug penetration varied notably among triazoles, echinocandins, amphotericin B, and flucytosine.

Conclusions:

  • Relying solely on plasma concentrations for antifungal dosing is insufficient.
  • Tissue penetration is a critical factor in achieving therapeutic success.
  • Antifungal selection and dosing should incorporate tissue PK data for improved patient outcomes.
Keywords:
AntimycoticsDrug dispositionDrug distributionFungal infectionInfectious diseasesPK/PD

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