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).

ParameterHumanCynomolgus MonkeyMouseRatDog
Km (μM)72.6 ± 20254 ± 0.1****138 ± 18***139 ± 7.6***157 ± 8.8****
Vmax (nmol/mg/min)4.6 ± 1.42.5 ± 0.22.4 ± 0.6*2.1 ± 0.6*3.9 ± 0.9
Vmax/Km (μl/mg/min)6310171525
Normalized Vmax/Km (μl/mg/min)&1.620.471.172.590.88
  • * P < 0.05; ***P < 0.001; ****P < 0.0001.