Table 9.
Assay and clone | BMS-626529 |
MVC |
||
---|---|---|---|---|
Mean EC50 (nM) ± SD | Mean MPI ± SD | Mean EC50 (nM) ± SD | Mean MPI ± SD | |
PhenoSense Entry assay | ||||
MVC res 2 | >5,000 | NA | NA | <66 |
MVC res 3 | 6.7 | 100 | NA | <33 |
Cell fusion assay | ||||
S1 | 3.5 ± 0.3 | 100 ± 0.1 | 1.3 ± 0.1 | 100 ± 0.1 |
S2 | 9.6 ± 0.6 | 100 ± 0.1 | 3.2 ± 0.2 | 100 ± 0.1 |
R3 | 5.0 ± 1.8 | 100 ± 0.2 | 11 ± 2.2 | 56 ± 2.2 |
R4 | 101 ± 31 | 93 ± 7.1 | >3,335 | 39 ± 18 |
Post 5.1 | 209 ± 5.1 | 98 ± 1.7 | >5,000 | 15 ± 19 |
Resistance to either BMS-626529 or MVC is indicated by boldface type. S1 and S2 (isolated pretreatment) and R3 and R4 (isolated on day 224) cloned envelopes were isolated from a patient who experienced virologic failure on MVC treatment (33). The Post 5.1 envelope was isolated from a patient who was treated with the CCR5 antagonist aplaviroc and was resistant to both aplaviroc and MVC (50). Data are the mean values of two independent experiments. NA, not applicable because inhibition did not reach high enough levels.