Primary objective: \- to investigate the effect of food on the bioavailability of DF 2156Y after single dose administration of 400 mg of ladarixin to healthy male and female volunteers under fed and fasting conditions. Secondary objectives: * to investigate the effect of gender on the bioavailability of DF 2156Y and its metabolites (DF 2108Y and DF 2227Y) after single dose administration of 400 mg of ladarixin to healthy male and female volunteers * to evaluate safety and tolerability of a single dose administration of ladarixin 400 mg to healthy male and female volunteers.
This is a Single center, single dose, open label, randomized, two-way, crossover, food effect on bioavailability study. More precisely, a single oral dose of 400 mg of ladarixin (two 200 mg capsules) was administered to healthy male and female volunteers under fed (Test treatment) and fasting (Reference treatment) conditions in two consecutive study periods, according to a two-way crossover design, with a wash-out interval of at least 14 days between the two administrations.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
36
A single oral dose of 400 mg of ladarixin (two 200 mg capsules) was administered to healthy male and female volunteers under fed (Test treatment) and fasting (Reference treatment) conditions in two consecutive study periods, according to a two-way crossover design, with a wash-out interval of at least 14 days between the two administrations.
CROSS Research S.A., I Unit
Arzo, Canton Ticino, Switzerland
Cmax of Plasma DF 2156Y
PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. Cmax = maximum plasma concentration
Time frame: At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose)
AUC0-t of Plasma DF 2156Y
PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. AUC0-t = area under the concentration-time curve (AUC) from zero to the last quantifiable concentrations
Time frame: At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose)
AUC0-∞ of Plasma DF 2156Y
PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions: AUC0-∞ = area under the concentration-time curve (AUC) from zero to infinity
Time frame: At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose)
Tmax of Plasma DF 2156Y
PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. tmax = time to maximum plasma concentration
Time frame: At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose)
t1/2 of Plasma DF 2156Y
PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. t1/2 = half life, is the time required for a quantity to reduce to half of its initial value
Time frame: At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose)
Lambda-zeta of Plasma DF 2156Y
PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. lambda-zeta is the Individual estimate of the terminal elimination rate constant, calculated using log-linear regression of the terminal portions of the plasma concentration-versus-time curves
Time frame: At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose)
Frel of Plasma DF 2156Y
PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. Frel: Relative bioavailability, calculated as ratio AUC0-t (T)/ AUC0-t (R) (multiplicated by 100)
Time frame: At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose)
Cmax of Plasma DF 2108Y (DF 2156Y Metabolite)
PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. Cmax = maximum plasma concentration
Time frame: At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose)
AUC0-t of Plasma DF 2108Y (DF 2156Y Metabolite)
PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. AUC0-t = area under the concentration-time curve (AUC) from zero to the last quantifiable concentrations
Time frame: At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose)
AUC0-∞ of Plasma DF 2108Y (DF 2156Y Metabolite)
PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. AUC0-∞ = area under the concentration-time curve (AUC) from zero to infinity
Time frame: At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose)
Tmax of Plasma DF 2108Y (DF 2156Y Metabolite)
PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. tmax = time to maximum plasma concentration
Time frame: At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose)
t1/2 of Plasma DF 2108Y (DF 2156Y Metabolite)
PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. t1/2 = half life, is the time required for a quantity to reduce to half of its initial value
Time frame: At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose)
Lambda-zeta of Plasma DF2108Y (DF 2156Y Metabolite)
PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. Lambda-zeta is the individual estimate of the terminal elimination rate constant, calculated using log-linear regression of the terminal portions of the plasma concentration-versus-time curves.
Time frame: At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose)
Frel of Plasma DF2108Y (DF 2156Y Metabolite)
PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. Frel: Relative bioavailability, calculated as ratio AUC0-t (T)/ AUC0-t (R) (multiplicated by 100)
Time frame: At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose)
Cmax of Plasma DF2227Y (DF 2156Y Metabolite)
PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. Cmax = maximum plasma concentration
Time frame: At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose)
AUC0-t of Plasma DF2227Y (DF 2156Y Metabolite)
PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. AUC0-t = area under the concentration-time curve (AUC) from zero to the last quantifiable concentrations
Time frame: At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose)
Tmax of Plasma DF2227Y (DF 2156Y Metabolite)
PK parameters were assessed after single dose of 400 mg of ladarixin under fed and fasting conditions. tmax = time to maximum plasma concentration
Time frame: At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose)
Frel of Plasma DF222Y (DF 2156Y Metabolite)
PK parameters were assessed after single dose administration of 400 mg of ladarixin under fed and fasting conditions. Frel: Relative bioavailability, calculated as ratio AUC0-t (T)/ AUC0-t (R) (multiplicated by 100)
Time frame: At day 1 (15 min, 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 and 18 hours postdose); at days 2 and 3 (24, 30, 36, 48, 54 and 60 hours post-dose); at day 4 (72 hours post-dose)
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