TABLE 4.
Activity of AB-423 against nucleoside-resistant variants of HBVa
| HBV variant | Avg EC50 ± SD (μM)b |
||
|---|---|---|---|
| AB-423 | ETV | LAM | |
| rtM204I | 0.226 ± 0.031 | ND | >100 |
| rtM204I + V173L | 0.149 ± 0.004 | ND | >100 |
| rtM204I + S202G | 0.223 ± 0.032 | 10.236 ± 1.172 | ND |
| rtM204V + L180M | 0.197 ± 0.019 | ND | >100 |
| rtM204I + S202G + M250V | 0.239 ± 0.006 | 13.940 ± 4.493 | ND |
| U95551c | 0.168 ± 0.054 | 0.002 ± 0.0002 | 0.079 ± 0.056 |
a
ETV, entecavir; ND, not determined; LAM, lamivudine; rt, reverse transcriptase (HBV polymerase). This evaluation was performed using the HepG2 cell transient-transfection cell culture system, as described in the Materials and Methods section.
b
Average EC50s and standard deviations from 3 independent determinations are shown.
c
U95551 is the wild-type genotype D strain used as the vector background for all variants.