Fig. 4
Effects of lesinurad on OAT1 and ABCG2. a Lesinurad inhibits OAT1. Cells transfected with control plasmid (pSPORT6, open circles) or OAT1-expressing plasmid (pSPORT6-hOAT1) were incubated with different concentrations of lesinurad. Data are from an individual representative experiment, shown as the mean ± SEM of samples in triplicate. The dashed line indicates the maximum plasma- free concentration (Cmax,free) of a single 200-mg dose of lesinurad obtained in the clinic. This concentration does not inhibit OAT1 in vitro. b Lesinurad does not affect ABCG2 activity. Caco-2 cells were either untreated or treated with the indicated concentrations of lesinurad (open bars) for 30 minutes prior to the addition of the ABCG2 substrate genistein for 120 minutes. The inhibitor chrysin was used as a positive control (solid bar). Results are the mean ± SEM from samples in triplicate