Table 3.
Derived pharmacokinetic parameters for GS-566500
| Parameter | Mean (SD) value for doseb |
||||||
|---|---|---|---|---|---|---|---|
| 25 mg, capsule (6) | 50 mg, capsule (8) | 50 mg, solution (7) | 100 mg, capsule (8) | 200 mg, capsule (8) | 400 mg, capsule (7) | 800 mg, capsule (8) | |
| Cmax (ng/ml) | 21.0 (4.9) | 29.6 (5.7) | 34.4 (11.9) | 38.4 (30.4) | 59.7 (13.4) | 175.3 (160.8) | |
| tmax (h) | 3.0 [1.5–3.0] | 1.5 [1.5–2.0] | 2.0 [1.0–4.0] | 2.0 [1.0–2.0] | 1.5 [1.5–3.0] | 3.0 [2.0–4.0] | |
| AUC0–t (h · ng/ml) | 53.2 (23.7) | 76.9 (23.2) | 102.8 (42.8) | 133.2 (127.3) | 271.9 (75.4) | 799.8 (586.0) | |
| AUC0–∞ (h · ng/ml) | 149.1 (–) | 161.8 (53.0) | 294.7 (79.6) | 338.6 (87.8) | 926.8 (601.1) | ||
| t1/2 (h) | 1.7 | 2.0 (0.2) | 1.9 (0.1) | 2.4 (1.0) | 2.8 (0.5) | 3.2 (0.9) | |
| CLrenal (liters/h) | 0.09 | 0.11 (0.02) | 0.13 (0.02) | 0.10 (0.02) | 0.11 (0.02) | ||
| Urine %a | 0.78 (0.34) | 1.00 (0.48) | 1.76 (0.43) | 1.10 (0.33) | 0.75 (0.63) | 0.62 (0.17) | 0.88 (0.65) |
a
Urine %, percentage of study drug or its metabolites excreted in urine, adjusted to molecular weight.
b
No. of subjects tested is given in parentheses after the dose. Data for tmax are presented as median [range].