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Original Research

Supratherapeutic dose evaluation and effect of lesinurad on cardiac repolarization: a thorough QT/QTc study

, , , , , , & show all
Pages 3509-3517 | Published online: 27 Oct 2016

Figures & data

Table 1 Demographic characteristics at screening – MTD and TQT studies

Table 2 Plasma pharmacokinetics of lesinurad following a single dose of lesinurad 800 mg, 1,200 mg, or 1,600 mg to healthy male and female subjects – MTD and TQT study

Figure 1 Dose linearity assessment of Cmax (A) and AUC[0–inf] (B) for lesinurad in males and females – MTD study.

Notes: The 200 mg, 400 mg, and 600 mg data for males were taken from study RDEA594-109, while the 400 mg data for females were from study RDEA594-105.
Abbreviations: AUC[0–inf], area under the plasma concentration–time curve from zero to infinity; Cmax, maximum observed plasma concentration; MTD, maximum tolerated dose; SE, standard error.
Figure 1 Dose linearity assessment of Cmax (A) and AUC[0–inf] (B) for lesinurad in males and females – MTD study.

Figure 2 Placebo-corrected change from baseline QTcI versus sample time.

Abbreviation: QTcI, QT interval corrected using an individual-specific interval correction for heart rate.
Figure 2 Placebo-corrected change from baseline QTcI versus sample time.

Figure 3 QTcI placebo-corrected change from baseline versus lesinurad plasma concentration.

Abbreviation: QTcI, QT interval corrected using an individual-specific interval correction for heart rate.
Figure 3 QTcI placebo-corrected change from baseline versus lesinurad plasma concentration.

Table 3 Effect of sex on lesinurad pharmacokinetics following lesinurad dosing at 400 mg and 1,600 mg – TQT study