Table 1.
Potency of currently approved antiretroviral therapy in macrophages versus PBMCs
| Compound | Acute infection in macrophages EC50, nM |
Chronic infection in macrophages EC50, nM |
Acute infection in PBMCs EC50, nM |
|---|---|---|---|
| Entry inhibitors | |||
| Maraviroc | 0.5 | NA | 0.2–2.9 |
| Enfuvirtide | 20 | NA | NA |
| NNRTI | |||
| Delavirdine | 10 | NE | 6 |
| Efavirenz | 10 | NE | 10 |
| Etravirine | NA | NA | NA |
| Nevirapine | 50 | NE. | 40 |
| NRTI | |||
| Abacavir sulfate | 300 | NE | NA |
| Didanosine | 50 | NE | 500 |
| Lamivudine | 20 | NE | 40 |
| Stavudine | 240 | NE | 800 |
| Tenofovir disoproxil fumarate | 20 | NE | 370 |
| Zalcitabine | 3 | NE | 40 |
| Zidovudine | 20 | NE | 200 |
| Protease inhibitors | |||
| Amprenavir | 10 | 720 | NA |
| Atazanavir | NA | NA | NA |
| Darunavir | NA | NA | NA |
| Fosamprenavir | NA | NA | NA |
| Indinavir | 60 | 400 | 50 |
| Nelfinavir | 80 | 1.4×103 | 40 |
| Ritonavir | 120 | 3.3×103 | 20 |
| Saquinavir | 50 | 500 | 10 |
| Tipranavir | NA | NA | NA |
The 50% effective concentration (EC50) of US Federal Drug Administration-approved HIV type-1 antiretroviral therapy in acute versus chronically infected macrophages [14-17,22,29,35,45-47,52,119].
NA, not available; NE, not effective; NNRTI, non-nucleoside reverse transcriptase inhibitor; NRTI, nucleoside reverse transcriptase inhibitor; PBMCs, peripheral blood mononuclear cells.