This is a phase 1, randomized, open-label, single-dose, two-period, two-sequence crossover study in healthy male and female subjects to evaluate the relative oral bioavailability of levoketoconazole tablets (the test drug) and ketoconazole tablets (the reference drug product).
This is a phase 1, randomized, open-label, single-dose, two-period, two-sequence crossover study in healthy male and female subjects to evaluate the relative oral bioavailability of levoketoconazole tablets (the test drug) and ketoconazole tablets (the reference drug product). Subjects will be randomized to receive a single oral dose of 150 mg levoketoconazole (Study Drug A) or a single oral dose of 200 mg ketoconazole (Study Drug B) in each period.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
OTHER
Masking
NONE
Enrollment
34
Levoketoconazole tablet
Ketoconazole tablet
Pharmaceutical Research Associates, Inc.
Salt Lake City, Utah, United States
Ratio of geometric least squares means for AUClast of plasma levoketoconazole (2S,4R-ketoconazole)
Point estimates and 90 percent (%) confidence intervals (CIs) for the dose-normalized ratios of geometric least squares means between Test (levoketoconazole) and Reference (ketoconazole)
Time frame: 24 hours
Ratio of geometric least squares means for AUCinf of plasma levoketoconazole (2S,4R-ketoconazole)
Point estimates and 90 percent (%) confidence intervals (CIs) for the dose-normalized ratios of geometric least squares means between Test (levoketoconazole) and Reference (ketoconazole)
Time frame: 24 hours
Ratio of geometric least squares means for Cmax of plasma levoketoconazole (2S,4R-ketoconazole)
Point estimates and 90 percent (%) confidence intervals (CIs) for the dose-normalized ratios of geometric least squares means between Test (levoketoconazole) and Reference (ketoconazole)
Time frame: 24 hours
Terminal phase rate constant (λz)
Single-dose plasma PK parameters after a single administration of levoketoconazole and ketoconazole in the fasted state including λz
Time frame: 24 hours
Time to Maximum Plasma concentration (Tmax)
Single-dose plasma PK parameters after a single administration of levoketoconazole and ketoconazole in the fasted state including Tmax
Time frame: 24 hours
Lag-time (Tlag)
Single-dose plasma PK parameters after a single administration of levoketoconazole and ketoconazole in the fasted state including: Tlag
Time frame: 24 hours
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Apparent systemic clearance (CL/F)
Single-dose plasma PK parameters after a single administration of levoketoconazole and ketoconazole in the fasted state including: CL/F
Time frame: 24 hours
The percentage of area under the plasma concentration-time curve extrapolated from time 0 to infinity as a percentage of total AUC (%AUCext)
Single-dose plasma PK parameters after a single administration of levoketoconazole and ketoconazole in the fasted state including: %AUCext
Time frame: 24 hours
Volume of Distribution (Vz/F)
Single-dose plasma PK parameters after a single administration of levoketoconazole and ketoconazole in the fasted state including: Vz/F
Time frame: 24 hours
Elimination half-life (T1/2)
Single-dose plasma PK parameters after a single administration of levoketoconazole and ketoconazole in the fasted state including: t½
Time frame: 24 hours
Incidence of adverse events (AEs)
Incidence of Treatment-Emergent AEs (TEAEs), AEs of special interest, and Serious Adverse Events (SAEs)
Time frame: 35 days