Table 8.
Antiviral activity of macrocyclic inhibitors against multidrug‐resistant clinical isolates in PHA‐PBMCs.
|
Virus[a] |
IC50 value [μm] |
||||||
|---|---|---|---|---|---|---|---|
|
SQV |
IDV |
APV |
LPV |
DRV |
21 |
20 |
|
|
HIV‐1ERS104pre (WT X4) |
0.008 |
0.043 |
0.030 |
0.034 |
0.003 |
0.007 |
0.005 |
|
HIV‐1MDR/B (X4) |
0.27 (34) |
>1 (>23) |
>1 (>33) |
>1 (>29) |
0.019 (6) |
0.089 (13) |
0.037 (7) |
|
HIV‐1MDR/C (X4) |
0.032 (11) |
>1 (>23) |
0.37 (12) |
>1 (>29) |
0.008 (3) |
0.029 (4) |
0.044 (9) |
|
HIV‐1MDR/G (X4) |
0.030 (4) |
0.34 (5) |
0.43 (14) |
0.26 (8) |
0.023 (5) |
0.028 (4) |
0.057 (11) |
|
HIV‐1MDR/TM (X4) |
0.26 (33) |
>1 (>23) |
0.32 (11) |
>1 (>29) |
0.004 (1) |
0.072 (10) |
0.027 (6) |
|
HIV‐1MDR/MM (R5) |
0.19 (24) |
>1 (>23) |
0.21 (7) |
>1 (>29) |
0.011 (4) |
0.055 (8) |
0.033 (7) |
|
HIV‐1MDR/JSL (R5) |
0.30 (37) |
>1 (>23) |
0.62 (21) |
>1 (>29) |
0.027 (9) |
0.21 (30) |
0.073 (15) |
[a] The amino acid substitutions identified in the protease‐encoding region compared to the consensus type B sequence cited from the Los Alamos database. See reference 95 for details.