Antimicrobials
Isavuconazole

Isavuconazole

Restricted

None
Excellent (90 to 100%)
IV: $235/dose; PO: $69.25/dose

Spectrum of Activity

General Information

  • LFTs

  • Routine therapeutic drug monitoring is NOT indicated

  • Increasing LFTs

  • Nausea, vomiting, diarrhea

  • Infusion-related reactions (IV)

Cresemba

  • Distribution (IV): ~450 L
  • Protein Binding: >99% (primarily to albumin)
  • Metabolism: 
    • Isavuconazonium sulfate (prodrug) is rapidly hydrolyzed in the blood by esterases to active isavuconazole and an inactive cleavage product
    • Isavuconazole is metabolized by CYP3A4, CYP 3A5, and UGT
  • Bioavailability: Oral: 98%
  • Half-Life Elimination (IV): 130 hours
  • Time to Peak (oral): 2-3 hours
  • Excretion: 
    • Urine (<1% as unchanged isavuconazole)
    • Feces (33% as unchanged isavuconazole)