TABLE 2.
Fold changes in EC50 against molecular clones with IN substitutions identified in resistance selection study with DTG
| Virus substitution(s) | Mean fold change in EC50a: |
|||
|---|---|---|---|---|
| Dolutegravir | Raltegravir | Elvitegravir | Efavirenz | |
| NL432 (wild type) | 1.0 | 1.0 | 1.0 | 1.0 |
| E92Q | 1.6 (0.12) | 3.5 (1.4) | 19 (8.1) | 1.2 (0.22) |
| G193E | 1.3 (0.25) | 1.3 (0.35) | 1.3 (0.40) | 1.1 (0.032) |
| Q148K | 1.1 (0.19) | 83 (6.6) | >1,700 | 2.1 (0.26) |
| E138K/Q148K | 19 (8.0) | 330 (75) | 370b | 1.2b |
| Q148R | 1.2 (0.21) | 47 (9.3) | 240 (91) | 1.9 (0.21) |
| E138K/Q148R | 4.0 (1.1) | 110 (37) | 460 (230) | 1.0 (0.31) |
| G140S/Q148R | 8.4 (4.0) | 200 (5.3) | 270b | 1.5b |
| E138K/G140S/Q148R | 8.3 (1.1) | >660 | 190 (43) | 1.0 (0.10) |
| G140S/Q148R/V201I | 10 (3.0) | >660 | 420 (80) | 1.9 (0.28) |
| Q148H | 0.97 (0.67) | 13 (5.0) | 7.3 (2.3) | 1.4 (0.83) |
| G140S/Q148H | 2.6 (1.4) | >130 | >890 | 1.7 (0.99) |
| T97A/G140S/Q148H | 13 (2.1) | >660 | 3,900 (630) | 1.3 (0.046) |
| E138K/G140S/Q148H | 4.5 (1.1) | 500 (210) | 1,600 (370) | 0.92 (0.026) |
| E138K/G140S/Q148H/M154I | 8.4 (1.5) | >660 | 2,400 (670) | 0.87 (0.099) |
| V75I/E138K/G140S/Q148H/M154I | 21 (6.6) | >660 | 2,600 (450) | 1.2 (0.16) |
a
Each value represents the mean FC. The standard deviations from 3 to 5 independent experiments are shown in parentheses. Each data point was calculated from duplicate experiments. FC values of >10 are shown in bold type.
b
Data from one or two experiments.