TABLE 5.
CIsa of combinations of NNRTIs in two-compound combinations against HIV-1 RT activity and the replication of HIV-1 (RF)
| Compound tested with efavirenz | Ratiob | CI against HIV replication at:
|
CI against RT activity at:
|
||||
|---|---|---|---|---|---|---|---|
| IC50 | IC75 | IC90 | IC50 | IC75 | IC90 | ||
| DPC082 | 1:3 | 1.90 | 2.18 | 2.53 | 1.90 | 2.22 | 2.60 |
| 1:1 | 1.09 | 1.17 | 1.28 | 1.45 | 1.68 | 1.96 | |
| 3:1 | 1.36 | 1.10 | 0.90 | 1.26 | 1.33 | 1.43 | |
| DPC083 | 1:3 | 3.55 | 3.38 | 3.44 | 0.81 | 0.92 | 1.08 |
| 1:1 | 2.47 | 2.39 | 2.35 | 1.12 | 1.18 | 1.28 | |
| 3:1 | 4.07 | 3.16 | 2.47 | 0.88 | 1.02 | 1.23 | |
| DPC961 | 1:3 | 4.03 | 2.69 | 2.06 | 1.07 | 0.98 | 0.90 |
| 1:1 | 3.39 | 3.57 | 4.47 | 1.12 | 1.16 | 1.21 | |
| 3:1 | 3.96 | 2.31 | 1.56 | 1.10 | 1.20 | 1.31 | |
| DPC963 | 1:3 | 4.74 | 2.49 | 1.69 | 1.05 | 0.95 | 0.86 |
| 1:1 | 4.44 | 2.88 | 2.17 | 1.14 | 1.13 | 1.13 | |
| 3:1 | 4.78 | 2.85 | 1.97 | 1.45 | 1.15 | 0.91 | |
| NVP | 1:3 | 1.28 | 2.83 | 6.92 | 1.50 | 1.89 | 2.52 |
| 1:1 | 1.24 | 2.25 | 4.26 | 1.51 | 1.60 | 2.67 | |
| 3:1 | 3.17 | 2.76 | 2.42 | 1.62 | 1.89 | 2.52 | |
a
CIs were calculated by using the model of Chou and Talalay (5) for drug combinations and the CalcuSyn software package (BioSoft). CIs <0.8, >0.8 but <1.2, and >1.2 indicate synergy, additivity, and antagonism, respectively.
b
The ratio represents the biologically relevant IC50 ratio in which the two compounds were combined according to their individual IC50s determined by the HIV-1 RT and yield reduction assays.