Pharmacodynamics of Isavuconazole in a Dynamic In Vitro Model of Invasive Pulmonary Aspergillosis

Antimicrob Agents Chemother. 2015 Oct 26;60(1):278-87. doi: 10.1128/AAC.01364-15. Print 2016 Jan.

Abstract

Isavuconazonium sulfate is a novel triazole prodrug that has been recently approved for the treatment of invasive aspergillosis by the FDA. The active moiety (isavuconazole) has a broad spectrum of activity against many pathogenic fungi. This study utilized a dynamic in vitro model of the human alveolus to describe the pharmacodynamics of isavuconazole against two wild-type and two previously defined azole-resistant isolates of Aspergillus fumigatus. A human-like concentration-time profile for isavuconazole was generated. MICs were determined using CLSI and EUCAST methodologies. Galactomannan was used as a measure of fungal burden. Target values for the area under the concentration-time curve (AUC)/MIC were calculated using a population pharmacokinetics-pharmacodynamics (PK-PD) mathematical model. Isolates with higher MICs required higher AUCs in order to achieve maximal suppression of galactomannan. The AUC/MIC targets necessary to achieve 90% probability of galactomannan suppression of <1 were 11.40 and 11.20 for EUCAST and CLSI, respectively.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antifungal Agents / pharmacokinetics*
  • Antifungal Agents / pharmacology
  • Area Under Curve
  • Aspergillus fumigatus / drug effects*
  • Aspergillus fumigatus / growth & development
  • Bioreactors
  • Diffusion Chambers, Culture
  • Drug Resistance, Fungal
  • Galactose / analogs & derivatives
  • Humans
  • Mannans / metabolism
  • Mannans / pharmacology
  • Microbial Sensitivity Tests
  • Models, Biological
  • Models, Statistical*
  • Nitriles / pharmacokinetics*
  • Nitriles / pharmacology
  • Pulmonary Alveoli / drug effects
  • Pulmonary Alveoli / metabolism
  • Pulmonary Alveoli / microbiology
  • Pyridines / pharmacokinetics*
  • Pyridines / pharmacology
  • Triazoles / pharmacokinetics*
  • Triazoles / pharmacology

Substances

  • Antifungal Agents
  • Mannans
  • Nitriles
  • Pyridines
  • Triazoles
  • galactomannan
  • isavuconazole
  • Galactose