Table 2.
Half maximal effective concentration of HIV PI drugs in human and fission yeast cells.
| HIV-1 Protease Inhibitor Drug | EC50 in Human Cell (nM) 1 | EC50 in Fission Yeast /Pure Compound (μM) 2 |
EC50 in Fission Yeast /Drug Formulation (μM) 3 |
Reference |
|---|---|---|---|---|
| First-generation single-agent drug | ||||
| Saquinavir (SQV) | 5–25 | 9.88 ± 0.25 | nd | [61] |
| Indinavir (IDV) | 5–30 | 48.64 ± 2.51 | nd | [62] |
| Ritonavir (RTV) | 40–100 | 115.2 ± 3.2 | 70.39 ± 2.25 | [53,63] |
| Nelfinavir (NFV) | 3–40 | 9.7 ± 0.34 | nd | [53,63] |
| Amprenavir (APV) | 15–60 | 55.41 ± 3.18 | nd | [18] |
| Fosamprenavir (FPV) * | cnd | na | cnd | [18] |
| Lopinavir (LPV) | 4–11 | 4.59 ± 0.06 | nd | [64] |
| Second-generation single-agent drug | ||||
| Atazanavir (ATV) | 2–5 | 21.08 ± 0.07 | 16.33 ± 0.95 | [65] |
| Tipranavir (TPV) | 30–70 | 7.86 ± 0.32 | nd | [66] |
| Darunavir (DRV) | 1–10 | 2.53 ± 0.08 | 1.81 ± 0.08 | [54] |
| Fixed dose combination drug | ||||
| Lopinavir/Ritonavir (LPV/r) |
na | na | 4.03 ± 0.74 | [67] |
| Atazanavir/ Cobicistat (ATV/co) |
na | na | 17.04 ± 0.95 | [68] |
| Darunavir/Cobicistat (DRV/co) | 1–2 | na | 2.02 ± 0.15 * | [68] |
Note: *, FPV is prodrug of APV; 1, from [53,63]; 2, pure compounds; 3, compounds in drug pill forms; EC50, mean 50% effective concentration; na, not available; nd, not determined; cnd, cannot be determined. LPV/r, LPV, and RTV combination. Cobicistat, an inhibitor of human CYP3A proteins (under the brand name Tybost). It is used to boost the PI effect.