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Low Selectivity Indices of Ivermectin and Macrocyclic Lactones on SARS-CoV-2 Replication In Vitro

1
Centre d’Etude des Maladies Infectieuses et Pharmacologie Anti-Infectieuse (CEMIPAI), CNRS UAR 3725, Université de Montpellier, 1919 Route de Mende, CEDEX 05, 34293 Montpellier, France
2
TransVIHMI, Institut de Recherche pour le Développement (IRD), Unité Mixte Internationale 233, INSERM Unité 1175, Université de Montpellier, 34293 Montpellier, France
3
Infectious Disease Department, University Hospital of Montpellier, 34293 Montpellier, France
4
Institute of Research in Infectiology of Montpellier (IRIM), University of Montpellier, UMR9004 CNRS, 34293 Montpellier, France
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editor: Tohru Suzuki
COVID 2022, 2(1), 60-75; https://doi.org/10.3390/covid2010005
Received: 20 November 2021 / Revised: 17 December 2021 / Accepted: 5 January 2022 / Published: 12 January 2022
Ivermectin was first approved for human use as an endectocide in the 1980s. It remains one of the most important global health medicines in history and has recently been shown to exert in vitro activity against SARS-CoV-2. However, the macrocyclic lactone family of compounds has not previously been evaluated for activity against SARS-CoV-2. The present study aims at comparing their anti-viral activity in relevant human pulmonary cell lines in vitro. Here, in vitro antiviral activity of the avermectins (ivermectin and selamectin) and milbemycins (moxidectin and milbemycin oxime) were assessed against a clinical isolate from a CHU Montpellier patient infected with SARS-CoV-2 in 2020. Ivermectin, like the other macrocyclic lactones moxidectin, milbemycin oxime and selamectin, reduced SARS-CoV-2 replication in vitro (EC50 of 2–5 μM). Immunofluorescence assays with ivermectin and moxidectin showed a reduction in the number of infected and polynuclear cells, suggesting a drug action on viral cell fusion. However, cellular toxicity of the avermectins and milbemycins during infection showed a very low selectivity index of <10. Thus, none of these agents appears suitable for human use for its anti-SARS-CoV-2 activity per se, due to low selectivity index. View Full-Text
Keywords: SARS-CoV-2; in vitro drug screening; ivermectin; anti-parasite drugs; antiviral specificity index SARS-CoV-2; in vitro drug screening; ivermectin; anti-parasite drugs; antiviral specificity index
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MDPI and ACS Style

Chable-Bessia, C.; Boullé, C.; Neyret, A.; Swain, J.; Hénaut, M.; Merida, P.; Gros, N.; Makinson, A.; Lyonnais, S.; Chesnais, C.; Muriaux, D. Low Selectivity Indices of Ivermectin and Macrocyclic Lactones on SARS-CoV-2 Replication In Vitro. COVID 2022, 2, 60-75. https://doi.org/10.3390/covid2010005

AMA Style

Chable-Bessia C, Boullé C, Neyret A, Swain J, Hénaut M, Merida P, Gros N, Makinson A, Lyonnais S, Chesnais C, Muriaux D. Low Selectivity Indices of Ivermectin and Macrocyclic Lactones on SARS-CoV-2 Replication In Vitro. COVID. 2022; 2(1):60-75. https://doi.org/10.3390/covid2010005

Chicago/Turabian Style

Chable-Bessia, Christine, Charlotte Boullé, Aymeric Neyret, Jitendriya Swain, Mathilde Hénaut, Peggy Merida, Nathalie Gros, Alain Makinson, Sébastien Lyonnais, Cédric Chesnais, and Delphine Muriaux. 2022. "Low Selectivity Indices of Ivermectin and Macrocyclic Lactones on SARS-CoV-2 Replication In Vitro" COVID 2, no. 1: 60-75. https://doi.org/10.3390/covid2010005

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