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Nelfinavir inhibits replication of severe acute respiratory syndrome coronavirus 2 in vitro

Norio Yamamoto, Shutoku Matsuyama, Tyuji Hoshino, Naoki Yamamoto
doi: https://doi.org/10.1101/2020.04.06.026476
Norio Yamamoto
1Department of Virology, Division of Host Defense Mechanism, Tokai University School of Medicine, 143 Shimokasuya, Isehara, Kanagawa 259-1193, Japan
2Department of Microbiology, Juntendo University School of Medicine, 2-1-1 Hongo, Bunkyo-ku, Tokyo 113-8421, Japan
3Influenza Virus Research Center, National Institute of Infectious Diseases, 4-7-1 Gakuen, Musashi-murayama, Tokyo 208-0011, Japan
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  • For correspondence: n-yamamoto@tsc.u-tokai.ac.jp nyamamo@juntendo.ac.jp
Shutoku Matsuyama
4Department of Virology III, National Institute of Infectious Diseases, 4-7-1 Gakuen, Musashi-murayama, Tokyo 208-0011, Japan
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Tyuji Hoshino
5Graduate School of Pharmaceutical Sciences, Chiba University, 1-8-1 Inohana, Chuo-ku, Chiba 260-8675, Japan
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Naoki Yamamoto
6Department of Molecular Virology, Graduate School of Medicine, Tokyo Medical and Dental University, 1-5-45, Yushima, Bunkyo-ku, Tokyo 113-8519, Japan
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Abstract

In December 2019, severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) emerged in Wuhan, Hubei Province, China. No specific treatment has been established against coronavirus disease-2019 (COVID-19) so far. Therefore, it is urgently needed to identify effective antiviral agents for the treatment of this disease, and several approved drugs such as lopinavir have been evaluated. Here, we report that nelfinavir, an HIV-1 protease inhibitor, potently inhibits replication of SARS-CoV-2. The effective concentrations for 50% and 90% inhibition (EC50 and EC90) of nelfinavir were 1.13 µM and 1.76 µM respectively, the lowest of the nine HIV-1 protease inhibitors including lopinavir. The trough and peak serum concentrations of nelfinavir were three to six times higher than EC50 of this drug. These results suggest that nelfinavir is a potential candidate drug for the treatment of COVID-19 and should be assessed in patients with COVID-19.

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The copyright holder for this preprint is the author/funder, who has granted bioRxiv a license to display the preprint in perpetuity. All rights reserved. No reuse allowed without permission.
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Posted April 08, 2020.
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Nelfinavir inhibits replication of severe acute respiratory syndrome coronavirus 2 in vitro
Norio Yamamoto, Shutoku Matsuyama, Tyuji Hoshino, Naoki Yamamoto
bioRxiv 2020.04.06.026476; doi: https://doi.org/10.1101/2020.04.06.026476
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Nelfinavir inhibits replication of severe acute respiratory syndrome coronavirus 2 in vitro
Norio Yamamoto, Shutoku Matsuyama, Tyuji Hoshino, Naoki Yamamoto
bioRxiv 2020.04.06.026476; doi: https://doi.org/10.1101/2020.04.06.026476

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