Table 5. Monkey PKa Profile of (+)-Lesinurad and (−)-Lesinurad.
| parameters | (−)-lesinurad | (+)-lesinurad | (−)/(+)-index | |
|---|---|---|---|---|
| IV | doseb (mg/kg) | 2 | 2 | |
| AUC0-inf (μM·h) | 26.7 ± 8.8 | 19.2 ± 7.3 | 1.4 | |
| CLp (mL/min/kg) | 3.3 ± 1.0 | 4.7 ± 1.5 | 0.7 | |
| C0–24h,urine (μM) | 16.3 ± 7.4 | 15.7 ± 3.3 | 1.0 | |
| PO | dosec (mg/kg) | 10 | 10 | |
| AUC0-inf (μM·h) | 83.9 ± 12.1 | 37.3 ± 6.9 | 2.2 | |
| C0–24h,urine (μM) | 120.1 ± 82.7 | 47.8 ± 20.3 | 2.5 | |
a
Monkey PK data is mean ± SD, n = 3.
b
IV formulation: 2.00 mg/mL in DMSO/PEG400/H2O(5/40/55), clear solution.
c
PO formulation: 2 mg/mL in DMSO/0.5%MC(5/95), suspension.