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Original Research

Pharmacokinetics, pharmacodynamics, and safety of lesinurad, a selective uric acid reabsorption inhibitor, in healthy adult males

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Pages 3423-3434 | Published online: 02 Jul 2015

Figures & data

Table 1 Pharmacokinetics of single ascending doses of lesinurad in healthy fasted and fed male subjects

Figure 1 Plasma lesinurad concentration profiles. (A) and median percent change from baseline in serum uric acid profiles following single doses of lesinurad in healthy male subjects (B).

Notes: The points before “0” represent the pre-dose values for all groups.
Figure 1 Plasma lesinurad concentration profiles. (A) and median percent change from baseline in serum uric acid profiles following single doses of lesinurad in healthy male subjects (B).

Table 2 Pharmacokinetics and pharmacodynamics of multiple ascending doses of lesinurad in healthy fed and fasting male subjects

Figure 2 Median percent changes from baseline (time-matched, day −1) serum concentrations of urate following once-daily oral doses of lesinurad for 10 days.

Notes: The top x-axis labels refer to the hours of that day, where “0” of the next day is the same as 24 hours of the previous day.
Abbreviation: IR, immediate release.
Figure 2 Median percent changes from baseline (time-matched, day −1) serum concentrations of urate following once-daily oral doses of lesinurad for 10 days.

Figure 3 Median plasma concentration profiles from 0 to 24 hours post-dose following single doses of lesinurad: tablet versus capsule in healthy fed male subjects.

Abbreviation: IR, immediate release.
Figure 3 Median plasma concentration profiles from 0 to 24 hours post-dose following single doses of lesinurad: tablet versus capsule in healthy fed male subjects.

Figure 4 Dose linearity and proportionality of lesinurad under fasted (5–400 mg) or fed (100–600 mg) conditions in healthy subjects (A), and correlation between plasma lesinurad exposure or amount excreted in urine and serum uric acid-lowering effect (B).

Abbreviations: AUC, area under the plasma concentration–time curve; CI, confidence interval; Cmax, maximum observed plasma concentration.
Figure 4 Dose linearity and proportionality of lesinurad under fasted (5–400 mg) or fed (100–600 mg) conditions in healthy subjects (A), and correlation between plasma lesinurad exposure or amount excreted in urine and serum uric acid-lowering effect (B).

Table S1 Demographic and baseline characteristics of study subjects

Table S2 Plasma and urinary pharmacokinetics of lesinurad following single doses of lesinurad in healthy fed male subjects – tablet versus capsule (bioavailability study)

Table S3 AEs in MAD occurring in one or more subjects receiving lesinurad