Posaconazole in prophylaxis and treatment of invasive fungal infections: a pharmacokinetic, pharmacodynamic and clinical evaluation

Expert Opin Drug Metab Toxicol. 2020 Jul;16(7):539-550. doi: 10.1080/17425255.2020.1764939. Epub 2020 Jun 1.

Abstract

Introduction: Invasive fungal infections (IFIs) are associated with a high morbidity and mortality and their incidence is rising. Posaconazole is a triazole antifungal drug that has an important place in the prophylaxis and salvage treatment of these infections.

Areas covered: This review focuses on the efficacy, safety, pharmacokinetics, pharmacodynamics, and drug-drug interactions of posaconazole. Literature search was conducted in PubMed.

Expert opinion: Posaconazole has a broad antifungal spectrum for both yeasts and molds, with a manageable safety profile. Its efficacy for IFIs is shown in both prophylaxis and salvage treatment. This drug is available as a suspension, tablet, and solution for intravenous administration. The suspension is associated with an erratic absorption, but this is (largely) overcome with the new formulations. Posaconazole is a CYP3A4 inhibitor and substrate for UGT1A4 and P-gp so drug-drug interactions can occur. The exposure in certain subgroups needs to be studied further and the place of routine therapeutic drug monitoring is still to be established.

Keywords: Drug-drug interactions; efficacy; invasive fungal infections; pharmacodynamics; pharmacokinetics; posaconazole.

Publication types

  • Review

MeSH terms

  • Antifungal Agents / administration & dosage*
  • Antifungal Agents / adverse effects
  • Antifungal Agents / pharmacokinetics
  • Cytochrome P-450 CYP3A Inhibitors / administration & dosage
  • Cytochrome P-450 CYP3A Inhibitors / adverse effects
  • Cytochrome P-450 CYP3A Inhibitors / pharmacokinetics
  • Drug Interactions
  • Drug Monitoring
  • Humans
  • Invasive Fungal Infections / drug therapy*
  • Invasive Fungal Infections / prevention & control
  • Salvage Therapy
  • Triazoles / administration & dosage*
  • Triazoles / adverse effects
  • Triazoles / pharmacokinetics

Substances

  • Antifungal Agents
  • Cytochrome P-450 CYP3A Inhibitors
  • Triazoles
  • posaconazole