The objectives of this study are to evaluate the effect of the timing of a moderate-fat meal on the single dose pharmacokinetics of entinostat and to evaluate the safety and tolerability of entinostat under fed and fasting conditions in healthy adult subjects.
This is a 2-stage food effect (timing of the meal) study. A total of 48 subjects will be dosed if Stage 2 is conducted. Stage 1 will be conducted as an open-label, randomized, 2-way crossover study. On Day 1 of each period, subjects will receive a single, oral dose of entinostat under fasting or fed conditions. If preliminary results in Stage 1 indicate that the timing of a meal exhibits significant effect on the bioavailability of entinostat, then Stage 2 will be conducted which will investigate the effect of a meal either before or after dosing of entinostat on entinostat PK. Stage 2 will be conducted as an open-label, randomized, 3-way crossover study. On Day 1 of each period, subjects will receive a single, oral dose of entinostat under fasting or fed conditions.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
OTHER
Masking
NONE
Enrollment
47
HDAC (histone deacetylase) inhibitor
Celerion
Lincoln, Nebraska, United States
AUC0-t (area under the concentration-time curve, from time 0 to the last observed non-zero concentration (t) for entinostat under fed and fasting conditions
Time frame: Pre-dose through Day 22
AUC0-inf (area under the concentration-time curve, from time 0 extrapolated to infinity) for entinostat under fed and fasting conditions
Time frame: Pre-dose through Day 22
Cmax (maximum observed concentration) of entinostat under fed and fasting conditions
Time frame: Pre-dose through Day 22
AUC%extrap (percent of AUC0-inf extrapolated) of entinostat under fed and fasting conditions
Time frame: Pre-dose through Day 22
Tmax (time to reach maximum observed concentration) of entinostat under fed and fasted conditions
Time frame: Pre-dose through Day 22
Kel (apparent terminal elimination rate constant) of entinostat under fed and fasted conditions
Time frame: Pre-dose through Day 22
T1/2 (apparent terminal elimination half-life) of entinostat under fed and fasted conditions
Time frame: Pre-dose through Day 22
Changes from baseline in physical exam
Time frame: Baseline through Day 1
Changes from baseline in vital signs
Time frame: Baseline through Day 22
Changes from baseline in ECG results
Time frame: Baseline through Day 22
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Changes from baseline in adverse events
Time frame: Baseline through 14 days after last sample collection
Changes from baseline in clinical laboratory tests
Time frame: Baseline through Day 1