Table 1.
Anti-HIV-1 activity, anti-HBV activity, and cytotoxicity of NRTIs
| Drug | IC50 (μM) against
|
CC50 (μM) in
|
S.I. with
|
|||
|---|---|---|---|---|---|---|
| Anti-HIV-1 | Anti-HBV | MT-4 | HepG2 2.2.15 | Anti-HIV-1 | Anti-HBV | |
| ETV | 1.0 ± 0.4 | 0.0007 ± 0.0002 | 39.1 ± 8.7 | > 100 | 38 | > 140,000 |
| ddI | 1.1 ± 0.04 | 3.7 ± 0.7 | > 100 | > 100 | > 89 | > 27 |
| 3TC | 0.29 ± 0.08 | 0.03 ± 0.01 | > 100 | > 100 | > 340 | > 3,300 |
| FTC | 0.23 ± 0.10 | 0.02 ± 0.01 | > 100 | > 100 | > 430 | > 5,000 |
| TDF | 0.58 ± 0.39 | 0.04 ± 0.01 | 40.4 ± 11.3 | > 100 | 70 | > 2,500 |
| ADV | 0.24 ± 0.12 | 0.20 ± 0.08 | 5.1 ± 1.0 | > 100 | 21 | > 500 |
| ABC | 0.58 ± 0.03 | 3.9 ± 1.0 | > 100 | > 100 | > 170 | > 26 |
| d4T | 0.65 ± 0.03 | > 100 | > 100 | > 100 | > 150 | N.D. |
| Ed4T | 0.26 ± 0.01 | > 100 | > 100 | > 100 | > 380 | N.D. |
| ddC | 0.33 ± 0.13 | 0.75 ± 0.12 | > 100 | > 100 | > 300 | > 130 |
| AZT | 0.03 ± 0.01 | > 100 | 30.5 ± 3.1 | > 100 | 1,020 | N.D. |
| EFdA | 0.0003 ± 0.0001 | 0.16 ± 0.03 | 19.2 ± 5.9 | > 100 | 64,000 | > 630 |
| LdT | > 100 | 0.007 ± 0.001 | > 100 | > 100 | N.D. | > 14,000 |
| CAdA | 0.0004 ± 0.0001 | 0.0004 ± 0.0002 | 3.5 ± 1.2 | 3.8 ± 1.0 | 8,750 | 9,500 |
| CdG | 0.0004 ± 0.0001 | 0.0004 ± 0.0001 | 2.8 ± 0.9 | 3.2 ± 0.7 | 7,000 | 8,000 |
Abbreviations: IC50: 50% inhibitory concentration, CC50: 50% cytotoxic concentration, S.I.: selectivity index. (CC50/IC50), N.D.: not determined
Anti-HIV-1 activity was determined using MT-4 cells, while anti-HBV activity was determined using HepG2 2.2.15 cells. Each assay was conducted in duplicate or triplicate. The values represent mean values (± 1 S.D.) out of two or three independent experiments.