Table 4. Monkey PKa Profile of (+)/(−)-Lesinurad after a Single Dosing of (±)-Lesinurad.
parameters | (−)-lesinurad | (+)-lesinurad | (−)/(+)-index | |
---|---|---|---|---|
IV | doseb | 2 mg/kg of (±)-lesinurad | ||
AUC0-inf (μM·h) | 14.5 ± 3.3 | 10.0 ± 2.8 | 1.4 | |
CLp (mL/min/kg) | 5.9 ± 1.5 | 8.8 ± 2.7 | 0.7 | |
C0–24h,urine (μM) | 5.4 ± 0.9 | 2.8 ± 1.4 | 1.9 | |
PO | dosec | 10 mg/kg of (±)-lesinurad | ||
AUC0-inf (μM·h) | 99.4 ± 29.7 | 28.2 ± 19.2 | 3.5 | |
C0–24h,urine (μM) | 153.3 ± 93.5 | 38.0 ± 20.7 | 4.0 |
Monkey PK data is mean ± SD, n = 3.
IV formulation: 2.00 mg/mL in DMSO/PEG400/H2O(5/40/55), clear solution.
PO formulation: 2 mg/mL in DMSO/0.5%MC(5/95), suspension.