TABLE 2.
Kinetic parameters of the tenofovir uptake by OAT1 species orthologs from human, cynomolgus monkey, mouse, rat, and dog
Statistical analyses were performed by one-way analysis of variance followed by Dunnett’s multiple comparisons test. N ≥ 2; &, tenofovir transport efficiency for OAT1 from each species was normalized to the corresponding membrane-bound OAT1 quantity (Supplemental Table 3).
| Parameter | Human | Cynomolgus Monkey | Mouse | Rat | Dog |
|---|---|---|---|---|---|
| Km (μM) | 72.6 ± 20 | 254 ± 0.1**** | 138 ± 18*** | 139 ± 7.6*** | 157 ± 8.8**** |
| Vmax (nmol/mg/min) | 4.6 ± 1.4 | 2.5 ± 0.2 | 2.4 ± 0.6* | 2.1 ± 0.6* | 3.9 ± 0.9 |
| Vmax/Km (μl/mg/min) | 63 | 10 | 17 | 15 | 25 |
| Normalized Vmax/Km (μl/mg/min)& | 1.62 | 0.47 | 1.17 | 2.59 | 0.88 |
*
P < 0.05; ***P < 0.001; ****P < 0.0001.