TABLE 1.
Relative potencies of HBV NRTIs
| Drug | Culture EC50 (nM) (mean ± SD)a | Difference (fold) from ETV EC50 | Enzyme IC50 (nM) (mean ± SD)a,b | Difference (fold) from ETV IC50b | Ki (nM)b | Km (nM)b,c | Ki/Kmb |
|---|---|---|---|---|---|---|---|
| ETV | 5.3 ± 2.5 | 1.0 | 0.5 ± 0.1 | 1 | 0.4 | 5.0 | 0.08 |
| LVD | 1,491 ± 1,033 | 281 | 6.2 ± 4.4d | 12.4 | 4.4 | 2.0 | 2.2 |
| ADV | 2,636 ± 1,549 | 497 | 31 ± 2.7 | 62 | 22.2 | 5.7 | 3.9 |
| LdT | 8,950 ± 4,803 | 1,689 | 243 ± 9 | 486 | — | — | — |
| TFV | 2,482 ± 1,938 | 468 | — | — | — | — | — |
a
Values represent three or more independent experiments.
b
—, not tested.
c
Km values were determined with dGTP for ETV, dCTP for LVD, and dATP for ADV.
d
LVD-TP values for this table were obtained from the work of Levine et al. (28).