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.
Pfizer Global Research and Development, New London, CT 06320, USA. manoli.vourvahis@pfizer.com
M
M
Vourvahis
S
S
Banerjee
R
R
LaBadie
D
D
Gore
H
H
Mayer
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