Pharmacodynamics of Isavuconazole for Invasive Mold Disease: Role of Galactomannan for Real-Time Monitoring of Therapeutic Response

Clin Infect Dis. 2017 Jun 1;64(11):1557-1563. doi: 10.1093/cid/cix198.

Abstract

Background.: The ability to make early therapeutic decisions when treating invasive aspergillosis using changes in biomarkers as a surrogate for therapeutic response could significantly improve patient outcome.

Methods.: Cox proportional hazards model and logistic regression were used to correlate early changes in galactomannan index (GMI) to mortality and overall response, respectively, from patients with positive baseline GMI (≥0.5) and serial GMI during treatment from a phase 3 clinical trial for the treatment of invasive mold disease. Pharmacokinetic/pharmacodynamic (PK/PD) analysis in patients with isavuconazole plasma concentrations was conducted to establish the exposure necessary for GMI negativity at the end of therapy.

Results.: The study included 158 patients overall and 78 isavuconazole patients in the PK/PD modeling. By day 7, GMI increases of >0.25 units from baseline (3/130 survivors; 9/28 who died) significantly increased the risk of death compared to those with no increase or increases <0.25 (hazard ratio, 9.766; 95% confidence interval [CI], 4.356-21.9; P < .0001). For each unit decrease by day 7 from baseline, the odds of successful therapy doubled (odds ratio, 2.154; 95% CI, 1.173-3.955). An area under the concentration-versus-time curve over half-maximal effective concentration (AUC:EC50) of 108.6 is estimated to result in a negative GMI at the end of isavuconazole therapy.

Conclusions.: Early trends in GMI are highly predictive of patient outcome. GMI increases by day 7 could be considered in context of clinical signs to trigger changes in treatment, once validated. Our data suggest that this improves survival by 10-fold and positive outcome by 3-fold. These data have important implications for individualized therapy for patients and clinical trials.

Clinical trials registration.: NCT00412893.

Keywords: aspergillosis; biomarker; galactomannan; isavuconazole; isavuconazonium sulfate..

Publication types

  • Clinical Trial, Phase III
  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Aged
  • Biomarkers / blood
  • Drug Monitoring*
  • Female
  • Galactose / analogs & derivatives
  • Humans
  • Invasive Fungal Infections / drug therapy
  • Invasive Fungal Infections / microbiology
  • Invasive Pulmonary Aspergillosis / drug therapy*
  • Invasive Pulmonary Aspergillosis / microbiology
  • Invasive Pulmonary Aspergillosis / mortality
  • Logistic Models
  • Male
  • Mannans / blood*
  • Middle Aged
  • Nitriles / administration & dosage
  • Nitriles / blood
  • Nitriles / pharmacokinetics*
  • Nitriles / therapeutic use*
  • Proportional Hazards Models
  • Pyridines / administration & dosage
  • Pyridines / blood
  • Pyridines / pharmacokinetics*
  • Pyridines / therapeutic use*
  • Survival Analysis
  • Treatment Outcome
  • Triazoles / administration & dosage
  • Triazoles / blood
  • Triazoles / pharmacokinetics*
  • Triazoles / therapeutic use*

Substances

  • Biomarkers
  • Mannans
  • Nitriles
  • Pyridines
  • Triazoles
  • galactomannan
  • isavuconazole
  • Galactose

Associated data

  • ClinicalTrials.gov/NCT00412893