TABLE 7.
Susceptibilities of lersivirine-resistant HIV-1 isolates to lersivirine, efavirenz, and etravirinea
Virus backboneb | Experimental condition | RT mutation(s) | Fold change in EC50 from that for wt virus of indicated drugc |
||
---|---|---|---|---|---|
Lersivirine | EFV | ETV | |||
wt | Virus after passage through lersivirine | V108I | 5.5 | 1.5 | 0.9 |
K103N | Input virus | K103N | 2.7 | 35.5 | 1.4 |
Virus after passage through lersivirine | K103N, V108V/I | 5.0 | 54.8 | 1.1 | |
Y181C | Input virus | Y181C | 1.8 | 1.9 | 4.4 |
Virus after passage through lersivirine | Y181C, V179V/D | 11.1 | 9.5 | 13.0 | |
Virus after passage through lersivirine | Y181C, V108V/I, V179V/D | 8.0 | 7.2 | 9.4 |
Mutations were identified in the GeneSeq HIV assay at Monogram Biosciences. Susceptibilities to lersivirine, efavirenz (EFV), and etravirine (ETV) were determined in Monogram Biosciences's PhenoSense assay.
Serial passage of wt virus or K103N or Y181C site-directed mutants in fixed concentrations of lersivirine. The wt and K103N and Y181C mutant viruses were passaged at 17 days, 10 days, and 17 days, respectively.
The drug-sensitive virus CNDO was used as the reference virus for estimation of fold change in EC50 in the PhenoSense assay; this value was then used to determine the EC50 fold change from that for the wt virus.