Objectives: Pharmacokinetics of dapaconazole and inhibition of cytochrome P450 family 51.
Methods: Pharmacokinetics of dapaconazole, a novel imidazolic antifungal compound, was studied in
male beagle dogs following intravenous (1, 2 and 20 mg/kg) and oral (20 mg/kg) administration.
Results: Oral bioavailability was calculated to be 97.3%. The elimination half-life (t½) after intravenous
administration was 2.1-2.5 h, the total body clearance was 2.5-4.2 L/h/kg and the apparent volume of
distribution was 9.0-14.4 L/kg. Dapaconazole caused concentration-dependent inhibition of cytochrome
P450 family 51 (CYP51) activity with an IC50 of 1.4 ± 0.3 μM (mean ± SEM, n=3), compared to that of
ketoconazole (IC50 = 1.2 ± 0.6 μM, n=3).
Conclusion: Results indicate that dapaconazole could be a potentially useful drug for systemic administration.