TABLE 2

Lesinurad atropisomer urine pharmacokinetic parameters (geometric mean and 95% confidence interval)

The P values were determined using a paired t test. The fraction excreted in urine and CLr values for each atropisomer were calculated using one-half of the racemate dose based on the fact that the racemate exists as a 50:50 mixture of two atropisomers and absorption of lesinurad was assumed to be nonstereoselective.

TreatmentLesinuradAe0–24feCLr
mg%ml/min
Multiple doses day 14Atropisomer 165.9 (49.78–87.3)32.9 (24.8–43.7)40.8 (31.5–52.9)
Multiple doses day 14Atropisomer 2101 (81.1–127)50.7 (40.6–63.3)48.6 (37.3–63.4)
Multiple doses day 14Atropisomer 1/atropisomer 2 ratio0.650 (0.602–0.702)0.648 (0.61–0.69)0.839 (0.818–0.86)
Multiple doses day 14P value0.0050.0050.153
  • Ae0–24, amount excreted in urine from time zero to 24 hours; fe, fraction excreted in urine.