Table 2.
Urine pharmacokinetic parameters for GS-9851, GS-566500, and GS-331007
| Drug and parameter | Mean (SD) value for day and dosea |
|||
|---|---|---|---|---|
| Day 1 |
Day 3 |
|||
| 200 mg | 400 mg | 200 mg | 400 mg | |
| GS-9851 | ||||
| Urine recovered (%)c | 0.81 (0.66) | 0.54 (0.41) | 0.72 (0.46) | 0.35 (0.31) |
| Ae0–24 (mg) | 1.61 (1.32) | 2.14 (1.66) | 1.44 (0.92) | 1.40 (1.23) |
| CLrenal (liters/min) | 0.192 (0.078) | 0.167 (0.090) | 0.185 (0.059) | 0.142 (0.096) |
| GS-566500 | ||||
| Urine recovered (%)c | 0.91 (0.95) | 0.87 (0.63) | 0.80 (0.37) | 0.56 (0.26) |
| Ae0–24 (mg) | 1.42 (1.47) | 2.70 (1.94) | 1.23 (0.57) | 1.70 (0.79) |
| CLrenal (liters/min) | 0.315 (0.241)b | 0.223 (0.204) | 0.449 (0.397) | 0.272 (0.312) |
| GS-331007 | ||||
| Urine recovered (%)c | 26.22 (6.93) | 14.01 (3.47) | 38.45 (9.58) | 25.81 (8.33) |
| Ae0–24 (mg) | 25.77 (6.81) | 27.55 (6.83) | 32.86 (8.38) | 35.76 (8.01) |
| CLrenal (liters/min) | 0.178 (0.048) | 0.172 (0.041) | 0.194 (0.046) | 0.183 (0.053) |
a
Values are for 8 subjects except where otherwise noted.
b
n = 7.
c
Percentage of study drug excreted in urine. Values for GS-566500 and GS-331007 are presented as GS-9851 equivalents given the difference in molecular weights between GS-9851 and its metabolites.