Table 2.
Repurposed drug | In vitro antiviral activity against SARS-CoV-2 | Plasma total concentrations in human (SARS-CoV-2 infected patients) | Plasma total concentrations in human (others populations) |
---|---|---|---|
Lopinavir | EC50 = 26.63 μM (16.75 μg/mL) (Choy et al., 2020) EC50 = 15.27 μM (9.60 μg/mL) (Jeon et al., 2020) |
400/100 mg BID: Ctrough [11.4–30.8 μg/mL] 400/100 mg QD: Ctrough [8.7–18.3 μg/mL](Gregoire et al., 2020) |
|
Remdesivir | EC50 = 0.77 μM (0.46 μg/mL) (Wang et al., 2020) EC50 = 23.15 μM (13.95 μg/mL) (Choy et al., 2020) EC50 = 8.24 μM (4.97 μg/mL) (Jeon et al., 2020) EC50 = 165 ± 0.79 μM (99.43 μg/mL) (Touret et al., 2020) |
Healthy subjects 100 mg QD for 5–10 days: Mean (SD) GS-443902 C24 in PBMCs = 10.2 (5.5) μM (Day 5) (European Medicines Agency. Summary on remdesivir compassionate use. April 2020) |
|
Hydroxychloroquine | EC50 = 0.72 μM (0.24 μg/mL) (Yao et al., 2020) EC50 = 4.51 μM (1.47 μg/mL) (Liu et al., 2020) EC50 = 4.17 μM (1.35 μg/mL) (Touret et al., 2020) |
200 mg TID MD without LD: Ctrough = 0.09 ± 0.01 (H8 on day 2) to 0.19 ± 0.06 (H8 on day 6) μg/mL 400mgx2 LD on day 1 followed by 400 × 1 MD: Ctrough = 0.09 ± 0.12 (H12 on day 2) to 0.13 ± 0.14 (H12 on day 6) μg/mL (Martin-Blondel et al., n.d.) |
|
Favipiravir | EC50 = 9.4 μg/mL EC50 = 40–80 μg/mL (Eloy et al., 2020) EC50 > 100 μM (>15.71 μg/mL) (Choy et al., 2020) EC50 > 500 μM (>78.55 μg/mL) (Jeon et al., 2020) |
Ebola patients 6000 mg on day 0 followed by 1200 mg BID for 9 days: Median (range) Ctrough = 46.1 (2.3–106.9) μg/mL on day 2 and 25.9 (0–173.2) μg/mL on day 4 (Nguyen et al., 2017) |
|
Ivermectin | EC50 = 2 μM (1750 ng/mL) (Caly et al., 2020) |
Onchocerciacis patients Single dose of 150 μg/kg PO: Cmax = 38.2 ± 5.8 ng/mL (Okonkwo et al., 1993) |
*Remdesivir is a prodrug rapidly converted to a circulating monophosphate nucleoside analog (GS-441524) which inside cells undergoes rapid conversion to the pharmacologically active analog of adenosine triphosphate (GS-443902) that inhibits viral RNA polymerases. LD = loading dose, MD = maintenance dose.