The purpose of this study is to estimate the pharmacokinetics (PK) of 3 different modified-release formulations of lersivirine and compare it to the PK of the immediate-release tablet. The effect of food on the PK of one of the modified-release tablets will also be assess along with the safety and tolerability of each treatment.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
16
Single 500 mg dose of Lersivirine Immediate-Release Tablets (2 x 250 mg)
Single 500 mg dose of Lersivirine Modified-Release Tablet #1
Single 500 mg dose of Lersivirine Modified-Release Tablet #2
Pfizer Investigational Site
Brussels, Belgium
Lersivirine Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)]
Time frame: T = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36 and 48 hours post dose
Lersivirine Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)
Time frame: T = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36 and 48 hours post dose
Lersivirine Maximum Observed Plasma Concentration (Cmax)
Time frame: T = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36 and 48 hours post dose
Lersivirine Plasma Decay Half-Life (t1/2)
Time frame: T = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36 and 48 hours post dose
Lersivirine Time to Reach Maximum Observed Plasma Concentration (Tmax)
Time frame: T = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36 and 48 hours post dose
Lersivirine Observed Plasma Concentration at time 24hr (C24)
Time frame: T = 24 hours post dose
Lersivirine Last Observed Plasma Concentration (Clast)
Time frame: T = 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36 and 48 hours post dose
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Single 500 mg dose of Lersivirine Modified-Release Tablet #3
Single 500 mg dose of Lersivirine Modified-Release Tablet dosed with food.