Table 5.
Activity of DRV against PI‐resistant HIV‐1 laboratory strains.
|
Virus |
Amino acid substitution |
EC50 [μm][a] |
|||||
|---|---|---|---|---|---|---|---|
|
SQV |
RTV |
IDV |
NFV |
APV |
DRV |
||
|
HIV‐1NL4‐3 |
wild type |
0.009 |
0.018 |
0.011 |
0.020 |
0.027 |
0.003 |
|
HIV‐1SQV 5μm |
L10I, G48V, I54V, L90M |
>1 (>111) |
>1 (>56) |
>1 (>91) |
0.30 (15) |
0.17 (6) |
0.005 (2) |
|
HIV‐1RTV 5μm |
M46I, V82F, I84V |
0.013 (1) |
>1 (>56) |
0.31 (28) |
0.24 (12) |
0.61 (23) |
0.025 (8) |
|
HIV‐1IDV5 μm |
L10F, L24I, M46I, L63P, A71V, G73S, V82T |
0.015 (2) |
>1 (>56) |
>1 (>91) |
0.74 (37) |
0.33 (12) |
0.029 (10) |
|
HIV‐1NFV 5μm |
L10F, D30N, K45I, A71V, T74S |
0.031 (3) |
0.09 (5) |
0.28 (25) |
>1 (>50) |
0.093 (3) |
0.003 (1) |
|
HIV‐1APV 5μm |
L10F, V32I, M46I, I54M, A71V, I84V |
0.020 (2) |
>1 (>56) |
0.31 (28) |
0.21 (11) |
>1 (>37) |
0.22 (73) |
[a] MT‐4 cells were exposed to each HIV‐1 strain (100×TCID50), and the inhibition of p24 Gag protein production by the drug was used as an end point. Numbers in parentheses represent the fold changes of the IC50 values for each isolate relative to that of HIV‐1NL4‐3. See reference 105.