Table 1 Comparison of NNRTI efficacies in various assay systems
Inhibition of HIV replication in vitroEC50[nM] | Enhancement of Gag processing (Fig. 2) | Cytotoxicity on MT4-CMV-EGFP control cells CC50[μM] | Cytotoxicity on MT4-LTR-EGFP-IIIB HIV-1 producing cells CC50[μM] | Ctotoxicity on MT4-LTR-EGFP-IIIB cells in presence of 0.1 μM DRV CC50[μM] | Enhancement of RT-Dimerization EC50[μM] | |
|---|---|---|---|---|---|---|
IDX-12899 | 1.9 ± 1.3 | ++ | > 10 | 0.29 ± 0.21 | > 10 | 0.0046 |
GW-678248 | 0.84 ± 0.25 | ++ | > 10 | 0.63 ± 0.29 | > 10 | 0.0032 |
VRX-480773 | 1.6 ± 0.81 | ++ | 5.82 ± 1.44 | 0.68 ± 0.34 | 6.33 ± 0.08 | 0.0040 |
EFV | 1.9 ± 0.9 | + | > 10 | 1.71 ± 0.43 | > 10 | 0.020 |
ETV | 3.2 ± 5 | + | > 10 | > 10 | > 10 | 0.27 |
UK-453061 | 7.5 ± 1.4 | - | > 10 | > 10 | > 10 | 0.15 |
NVP | 42 ± 20 | - | > 10 | > 10 | >10 | 18 |
TMC-120 | 1.7 ± 1.4 | - | 3.02 ± 0.90 | 2.56 ± 0.74 | 4.33 ± 0.81 | ND |