Table 2.
HIV drugs against SARS-CoV-2-Nluc.
| Inhibitor class | Compound name | EC50 (µM)a | CC50 (µM)a | SIb | Exposure (µM)c | Plasma protein binding (%)d | Reference |
|---|---|---|---|---|---|---|---|
| HIV protease (aspartyl) | Lopinavir | 9.00 ± 0.42 | 31.5 ± 2.5 | 3.5 | 15.6/8.8 | 98–99 | 51,52 |
| Amprenavir | >10 | >50 | – | – | 90 | 53 | |
| Nelfinavir | 0.77 ± 0.32 | 12.0 ± 1.3 | 15.7 | 8.3/2.6 | >98 | 54e | |
| Ritonavir | >10 | 36.9 ± 1.7 | – | – | 98–99 | 55,56 | |
| Indinavir | >10 | >50 | – | – | 61 | 57,58 | |
| Saquinavir | 8.95 ± 0.31 | 35.1 ± 11.7 | 3.9 | 3.7/0.65 | 98 | 59e | |
| Darunavir | >10 | >50 | – | – | 95 | 60e | |
| Atazanavir | >10 | >50 | – | – | 86 | 52 | |
| Tipranavir | 8.65 ± 0.16 | 28.4 ± 0.5 | 3.3 | 130/30.8 | 99.9 | 61 | |
| HIV NRTI | Emtricitabine (FTC) | >10 | >50 | – | Cmax 7.9 | 4 | 62e |
| Tenofovir alafenamide (TAF) | >10 | >50 | – | Cmax 0.4 | 80 | 63,64 | |
| Rovafovir (GS-9131) | >10 | >50 | – | – | – | 65 | |
| HIV NNRTI | Rilpivirine | 7.80 ± 1.04 | 14.6 ± 1.6 | 1.9 | 0.83/0.30 | 99.7 | 66e |
| Efavirenz | >9.6 | 37.6 ± 10.7 | <3.9 | 12.9/5.6 | 99.5–99.8 | 67 | |
| HIV integrase | Bictegravir | >10 | >50 | – | – | >99 | 68 |
aValues are mean ± standard deviation of two independent replicates in A549-hACE2 cells.
bSI = CC50/EC50.
cValues represent Cmax/Cmin for human exposures in the clinic based on approved dosing schedules.
dData from literature as cited.
eInformation from product description.