Elsevier

Drug Discovery Today

Volume 25, Issue 10, October 2020, Pages 1786-1792
Drug Discovery Today

Feature
Repositioning chloroquine as antiviral prophylaxis against COVID-19: potential and challenges

https://doi.org/10.1016/j.drudis.2020.06.030Get rights and content

Highlights

  • Chloroquine (CQ) has in vitro evidence of potential efficacy against SARS-CoV-2 (virus causing COVID-19) and particularly effective at early stages of infection when viral load is low.

  • CQ can achieve micromolar concentrations required for antiviral efficacy in short-term use at conventional doses but special attention to cardiac risk with COVID-19 is needed.

  • CQ could be particularly suited as a prophylactic in COVID-19 but futher research and confirmatory trials to establish its risk profile and efficacy is needed.

The Coronavirus Disease 2019 (COVID-19) pandemic is advancing globally, and pharmaceutical prophylaxis is one solution. Here, we propose repositioning chloroquine (CQ) as prophylaxis against COVID-19. CQ blocks viral attachment and entry to host cells and demonstrates efficacy against a variety of viruses, including severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the causative agent of COVID-19. Furthermore, CQ is safe, inexpensive, and available. Here, we review the antiviral mechanisms of CQ, its in vitro activity against coronaviruses, its pharmacokinetics (PK) and adverse effects, and why it could be more efficacious as a prophylactic rather than as a therapeutic, given the infection dynamics of SARS-CoV-2. We propose two prophylactic regimens based on efficacy and risk considerations. Although it is largely preclinical data that suggest the potential of CQ, properly planned prophylactic trials and further research are urgently needed.

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