This is a Phase 1, randomized, open label, 4-period, 6-sequence, partial cross-over, single-dose study to evaluate the PK of age-appropriate tofacitinib MR formulations (release rates: MR-Slow, MR-Moderate, and MR-Fast) compared to tofacitinib IR solution under fasting conditions. The effect of food on the PK of MR-Slow and MR-Fast will also be assessed.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
24
For the the relative bioavailability (BA) assessment , the investigational product(s) are: Test: 10 mg dose of age-appropriate MR formulations (MR-fast, MR-moderate, MR-slow). Each formulation contains 0.025 mg of tofacitinib/mg of microsphere. Reference: 10 mg dose of tofacitinib IR solution (1 mg of tofacitinib/mL). For the the food effect assessment, the investigational product(s) are: Test: 10 mg dose of age-appropriate MR formulations (MR-fast or MR-slow) c-oadministered with high-fat FDA breakfast. Reference: 10 mg dose of age-appropriate MR formulations (MR-fast or MR-slow) administered under fasted state.
Pfizer New Haven Clinical Research Unit
New Haven, Connecticut, United States
Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] (AUCinf )
Area Under the Curve From Time Zero to Extrapolated Infinite Time \[AUC (0 - ∞)\]
Time frame: 0.5, 1, 2, 3, 4, 5, 6, 9, 21, 24, 36, and 48 hours post dose
Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)
Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast) of Modified Release (MR) formulation compared to Immediate Release (IR) solution
Time frame: 0.5, 1, 2, 3, 4, 5, 6, 9, 21, 24, 36, and 48 hours post dose
Maximum Observed Plasma Concentration (Cmax)
Maximum (or peak) plasma concentration of MR formulation compared to IR solution
Time frame: predose, 0.5, 1, 2, 3, 4, 5, 6, 9, 21, 24, 36, and 48 hours post dose
Time to Reach Maximum Observed Plasma Concentration (Tmax)
Maximum time to peak plasma concentration of MR formulation compared to IR solution
Time frame: predose, 0.5, 1, 2, 3, 4, 5, 6, 9, 21, 24, 36, and 48 hours post dose
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