Table 2.
Relative activities of capsid assembly inhibitors against drug-resistant viruses
| Inhibitor | EC50 (nM) for the WT | Fold change from the EC50 for the isogenic WT virusa with the following mutation (resistance class)b: |
||||||
|---|---|---|---|---|---|---|---|---|
| Y188L (NNRTI) | V106A (NNRTI) | K65R (NRTI) | M184V (NRTI) | V32I I47V (PI) | L33F I54L (PI) | G140S Q148H (INSTI) | ||
| BD 1 | 70 | 1.1 | 0.9 | 0.8 | 0.9 | 1.5 | 0.9 | 1.2 |
| BM 2 | 284 | 1.0 | 0.7 | 1.0 | 0.6 | 1.1 | 1.3 | 1.2 |
| BM 3 | 112 | 1.2 | 0.9 | 0.7 | 1.0 | 0.7 | 0.6 | 0.8 |
| Nevirapine | 18 | >83 | 130b | 0.3 | 0.5 | 1.4 | 1.4 | 1.3 |
| Lamivudine | 89 | 1.3 | 0.9 | 26.4 | >96 | 0.9 | 1.2 | 1.2 |
| Amprenavir | 35 | 0.6 | 0.8 | 1.2 | 0.5 | 6.9 | 8.3 | 1.3 |
| Raltegravir | 1.5 | 2.8b | 0.4 | 1.0 | 0.6 | 0.7 | 1.8 | 227 |
a
All values are averages for two independent experiments except for the values for V106A with nevirapine and Y188L with raltegravir, for which experiments were performed once. Significant fold change values are in boldface.
b
Resistance targets were RT for Y188L, V106A, K65R, and M184V; PR for V32I I47V and L33F I54L; and IN for G140S Q148H.