Lack of a clinically relevant effect of an antacid on the pharmacokinetics of lersivirine.
Lersivirine (UK-453,061) is a next-generation nonnucleoside reverse transcriptase inhibitor that displays potent antiviral activity. Lersivirine solubility is pH dependent; therefore, the effect of coadministration of antacid on the pharmacokinetics of lersivirine in healthy subjects was investigated. The ratio of adjusted geometric means (750 mg lersivirine plus 20 ml Maalox Max/750 mg lersivirine alone) for the area under the curve from time zero extrapolated to infinite time (AUC(inf)) was 101.86%, showing that coadministration of an antacid had no effect on lersivirine exposure. Coadministration appeared to be safe and relatively well tolerated.
Vourvahis
M
M
Pfizer Global Research and Development, New London, CT 06320, USA. manoli.vourvahis@pfizer.com
Banerjee
S
S
LaBadie
R
R
Gore
D
D
Mayer
H
H
D000328:Adult; D000536:Aluminum Hydroxide / Q000008:administration & dosage*; D000863:Antacids / Q000008:administration & dosage*; D019540:Area Under Curve; D018592:Cross-Over Studies; D004338:Drug Combinations; D004347:Drug Interactions; D005260:Female; D015658:HIV Infections / Q000188:drug therapy; D006801:Humans; D008276:Magnesium Hydroxide / Q000008:administration & dosage*; D008297:Male; D008875:Middle Aged; D009570:Nitriles / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D011720:Pyrazoles / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D012016:Reference Values; D018894:Reverse Transcriptase Inhibitors / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D055815:Young Adult
D000863:Antacids; D004338:Drug Combinations; D009570:Nitriles; D011720:Pyrazoles; D018894:Reverse Transcriptase Inhibitors; C531151:UK 453,061; C013591:aluminum hydroxide, magnesium hydroxide, drug combination; D000536:Aluminum Hydroxide; D008276:Magnesium Hydroxide