Table 2.
Mean plasma PK parameters after IV administration (bolus) of RDV, MeRDV, IsoRDV, and Nuc in Ces1c−/− mice
| Parameters | RDV | MeRDV | IsoRDV | Nuc |
|---|---|---|---|---|
| AUC0-∞ (h⋅nM) | 1,576.2 ± 948 | 2,382.6 ± 1,154.5 | 4,950.3 ± 628.2 | 26,312.3 ± 839.4 |
| AUC0-t (h⋅nM) | 1,570.2 ± 947.8 | 2,370.4 ± 1,152.0 | 4,941.6 ± 626.4 | 25,123.2 ± 285.4 |
| CL/F (L⋅h−1) | 1.06 ± 0.44 | 0.79 ± 0.62 | 0.28 ± 0.03 | 0.052 ± 0.002 |
| Cmax (nM) | 1,371.7 ± 515.1 | 2,268.9 ± 949.5 | 5,888.3 ± 587.8 | 18,132.7 ± 2,656.8 |
| t1/2 (h) | 1.25 ± 0.39 | 0.92 ± 0.22 | 1.04 ± 0.33 | 6.34 ± 4.01 |
| Vd (L) | 1.91 ± 0.94 | 0.93 ± 0.48 | 0.42 ± 0.17 | 0.47 ± 0.29 |
| Nuc from RDV | Nuc from MeRDV | Nuc from IsoRDV | - | |
| AUC0-t (h⋅nM) | 10,345 ± 1,469.1 | 7,868.6 ± 2,237.1 | 8,561.4 ± 3,657.8 | - |
| Cmax (nM) | 1,859.5 ± 523.4 | 2,183.7 ± 947.4 | 1,810.6 ± 776.0 | - |
| Ala from RDV | Ala from MeRDV | Ala from IsoRDV | - | |
| AUC0-t (h⋅nM) | 5,059 ± 1,151.1 | 5,329.7 ± 1,920.3 | 4,237.6 ± 2,453.1 | - |
| Cmax (nM) | 8,632.1 ± 1,809.2 | 8,627.9 ± 3,318.5 | 8,262.1 ± 4,594.9 | - |
Data are shown as mean ± S.D. from three to four mice for each time point.