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. 2020 Jul 10;181:104866. doi: 10.1016/j.antiviral.2020.104866

Table 2.

Available EC50 against SARS-CoV-2 and corresponding total plasma concentrations obtained in human.

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.