uk-453-061 and aluminum-hydroxide--magnesium-hydroxide--drug-combination

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.

Topics: Adult; Aluminum Hydroxide; Antacids; Area Under Curve; Cross-Over Studies; Drug Combinations; Drug Interactions; Female; HIV Infections; Humans; Magnesium Hydroxide; Male; Middle Aged; Nitriles; Pyrazoles; Reference Values; Reverse Transcriptase Inhibitors; Young Adult