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Antimicrob Agents Chemother. 2010 May;54(5):2209-11. doi: 10.1128/AAC.01110-09. Epub 2010 Feb 16.

Lack of a clinically relevant effect of an antacid on the pharmacokinetics of lersivirine.

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  • 1Pfizer Global Research and Development, New London, CT 06320, USA. manoli.vourvahis@pfizer.com


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.

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