Table 1.

Pharmacokinetic and pharmacodynamic properties of isavuconazole compared with other azole antifungals¹⁰,¹²,⁴⁸–⁵²

Characteristic	Antifungal drug
	Isavuconazole	Voriconazole	Itraconazole	Posaconazole	Fluconazole
Available formulations	Oral and IV	Oral and IV	Oral*	Oral	Oral and IV
Bioavailability	Very high	Up to 95%	30% capsules 50% solution	Not applicable	95%
Protein binding	98%	58%	>99%	99%	10%
Food effect	No effect	Negative effect	Positive effect for capsules Negative effect for solution	Positive effect	Negative effect
Volume of distribution (L/kg)	High (4.4–7.7)	High (4.6)	Very high (10.7)	High (6.5)	Low (0.7)
CNS penetration	Low in CSF, high in brain	High (>50%)	Low (<10%)	Low	High (>60%)
Clearance (L/h)	Low (1.9–2.8)	High (8.4)	Very high (15.9)	Very high (21.7)	Low (1.2)
Half-life (h)	56–104	6–12	24–30	16–35	24–30
Probability of drug interactions	Moderate	High	High	Moderate	Moderate
Use in hepatic insufficiency	Reduce dose; avoid in severe hepatic disease	Reduce dose; avoid in severe hepatic disease	Reduce dose; avoid in severe hepatic disease	No dose adjustment; monitor carefully; avoid in severe hepatic disease	Reduce dose; avoid in severe hepatic disease

Note:

^*The IV formulation of itraconazole is no longer widely available in the international market.

Abbreviations: CNS, central nervous system; CSF, cerebrospinal fluid; IV, intravenous; L/h, liter/hour; h, hour.