tetano
Editor, Senior Moderator
Int J Antimicrob Agents
. 2021 Dec 17;106499.
doi: 10.1016/j.ijantimicag.2021.106499. Online ahead of print.
Effects of simeprevir on the replication of SARS-CoV-2 in vitro and in transgenic hACE2 mice
Elishiba Muturi[SUP] 1 [/SUP], Wei Hong[SUP] 1 [/SUP], Junhua Li[SUP] 2 [/SUP], Wan Yang[SUP] 3 [/SUP], Jin He[SUP] 3 [/SUP], Hongping Wei[SUP] 4 [/SUP], Hang Yang[SUP] 5 [/SUP]
Affiliations
Abstract
In a bid to contain the current COVID-19 (coronavirus disease 2019) pandemic, various countermeasures have been applied. To date, however, there is a lack of an effective drug for the treatment of COVID-19. Through molecular modelling studies, simeprevir, a protease inhibitor approved for the management of hepatitis C virus infection, has been predicted as a potential antiviral against SARS-CoV-2 (severe acute respiratory syndrome coronavirus 2), the causative agent of COVID-19. Here we assessed the efficacy of simeprevir against SARS-CoV-2 both in vitro in Vero E6 cells and in vivo in a human angiotensin-converting enzyme 2 (hACE2) transgenic mouse model. The results showed that simeprevir could inhibit SARS-CoV-2 replication in Vero E6 cells with a half-maximal effective concentration (EC[SUB]50[/SUB]) of 1.41 ± 0.12 μM. In a transgenic hACE2 mouse model of SARS-CoV-2 infection, intraperitoneal administration of simeprevir at 10 mg/kg/day for 3 consecutive days failed to suppress viral replication. These findings collectively imply that simeprevir does not inhibit SARS-CoV-2 in vivo and therefore do not support its application as a treatment against COVID-19 at a dosage of 10 mg/kg/day.
Keywords: Antiviral efficacy; COVID-19; SARS-CoV-2; Simeprevir.
. 2021 Dec 17;106499.
doi: 10.1016/j.ijantimicag.2021.106499. Online ahead of print.
Effects of simeprevir on the replication of SARS-CoV-2 in vitro and in transgenic hACE2 mice
Elishiba Muturi[SUP] 1 [/SUP], Wei Hong[SUP] 1 [/SUP], Junhua Li[SUP] 2 [/SUP], Wan Yang[SUP] 3 [/SUP], Jin He[SUP] 3 [/SUP], Hongping Wei[SUP] 4 [/SUP], Hang Yang[SUP] 5 [/SUP]
Affiliations
- PMID: 34929295
- DOI: 10.1016/j.ijantimicag.2021.106499
Abstract
In a bid to contain the current COVID-19 (coronavirus disease 2019) pandemic, various countermeasures have been applied. To date, however, there is a lack of an effective drug for the treatment of COVID-19. Through molecular modelling studies, simeprevir, a protease inhibitor approved for the management of hepatitis C virus infection, has been predicted as a potential antiviral against SARS-CoV-2 (severe acute respiratory syndrome coronavirus 2), the causative agent of COVID-19. Here we assessed the efficacy of simeprevir against SARS-CoV-2 both in vitro in Vero E6 cells and in vivo in a human angiotensin-converting enzyme 2 (hACE2) transgenic mouse model. The results showed that simeprevir could inhibit SARS-CoV-2 replication in Vero E6 cells with a half-maximal effective concentration (EC[SUB]50[/SUB]) of 1.41 ± 0.12 μM. In a transgenic hACE2 mouse model of SARS-CoV-2 infection, intraperitoneal administration of simeprevir at 10 mg/kg/day for 3 consecutive days failed to suppress viral replication. These findings collectively imply that simeprevir does not inhibit SARS-CoV-2 in vivo and therefore do not support its application as a treatment against COVID-19 at a dosage of 10 mg/kg/day.
Keywords: Antiviral efficacy; COVID-19; SARS-CoV-2; Simeprevir.