TABLE 2.
Summary of telbivudine pharmacokinetic parameters following oral administrationa
| Parameter | Valuea for patients in the following renal function category (dose):
|
|||||
|---|---|---|---|---|---|---|
| Normal (600 mg) | Mild impairment (600 mg) | Moderate impairment (400 mg) | Severe impairment (200 mg) | ESRD (200 mg)
|
||
| Pre-dialysis dosing | Post-dialysis dosing | |||||
| Cmax (μg/ml) | 3.4 ± 0.9 | 3.2 ± 0.9 | 2.8 ± 1.3 | 1.6 ± 0.8 | 1.2 ± 0.1 | 2.1 ± 0.9 |
| AUC0-t (μg·h/ml) | 26.5 ± 8.6 | 29.2 ± 8.8 | 30.1 ± 12.0 | 25.3 ± 13.1 | 26.5 ± 4.8 | 41.8 ± 21.5 |
| AUC0-∞ (μg·h/ml) | 28.5 ± 9.6 | 32.5 ± 10.1 | 36.0 ± 13.2 | 32.5 ± 13.2 | 43.4 ± 12.9 | 67.4 ± 36.9 |
| Tmax (h)b | 4.0 (2.0-4.0) | 4.0 (2.0-4.0) | 4.0 (1.0-4.0) | 4.0 (4.0-4.0) | 8.0 (1.0-8.0) | 3.5 (2.0-4.0) |
| t1/2 (h) | ||||||
| Elimination | 20.5 ± 4.5 | 26.7 ± 6.0 | 31.2 ± 13.0 | 32.9 ± 16.3 | 35.2 ± 8.9 | 37.9 ± 8.7 |
| Initial decline | 2.32 ± 0.24 | 3.42 ± 0.57 | 3.82 ± 0.76 | 4.50 ± 1.20 | NA | 4.87 ± 1.66 |
| Absorption | 1.00 ± 0.23 | 1.04 ± 0.17 | 1.12 ± 0.46 | 1.02 ± 0.22 | NA | 0.90 ± 0.05 |
| CL/F (liters/h) | 22.9 ± 6.2 | 20.7 ± 9.1 | 13.6 ± 8.7 | 7.1 ± 2.8 | 4.9 ± 1.2 | 3.6 ± 1.4 |
| CLR (liters/h) | 7.6 ± 2.9 | 5.0 ± 1.2 | 2.6 ± 1.2 | 0.7 ± 0.4 | 13.3 ± 2.5c | NA |
| Ae (% of dose) | 31.5 ± 8.5 | 23.6 ± 8.3 | 19.8 ± 11.9 | 8.0 ± 5.3 | NA | NA |
a
Subjects with normal renal function and those with mild renal impairment received a single dose of 600 mg, and subjects with moderate or severe renal impairment received a single dose of 400 or 200 mg, respectively. Unless indicated otherwise, values are means ± standard deviations. NA, not applicable.
b
Tmax values are medians (ranges).
c
Dialytic clearance.