June 27, 2022

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Small molecule TMPRSS2 inhibitor as nasal spray to prevent and treat COVID-19

Small molecule TMPRSS2 inhibitor as nasal spray to prevent and treat COVID-19



 

Small molecule TMPRSS2 inhibitor as nasal spray to prevent and treat COVID-19. 


In a new study in mice, researchers from Cornell University, Sherbrooke University, and the University of British Columbia have found that a small molecule may be able to be sprayed into people’s noses to prevent pre-exposure COVID-19 disease, if treated shortly after infection with the coronavirus SARS-CoV-2, may provide early treatment.

The relevant research results were published online in the journal Nature on March 28, 2022, with the title “A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic”.

 

The authors used experimental mice genetically engineered to express a human receptor on the cell surface that binds SARS-CoV-2 and found that the small molecule, called N-0385, inhibited the entry of the coronavirus into mice. cell. They demonstrated that as a TMPRSS2 inhibitor, N-0385 protected mice from infection prior to exposure, while delivering effective treatment within 12 hours of exposure.

 

Small molecule TMPRSS2 inhibitor as nasal spray to prevent and treat COVID-19

Ketobenzothiazole-based peptidomimetics are potent TMPRSS2 inhibitors. Image via Nature, 2022, doi:10.1038/s41586-022-04661-w.

 

This broad-spectrum therapy was tested in mice exposed to the first SARS-CoV-2 strain detected in Washington state in 2020, as well as the Delta strain, but not the Omicron variant, although These authors are optimistic that it will continue to work.

 

The authors delivered the small molecule intranasally into mice before, during, and/or after infection with SARS-CoV-2. They tracked the mice’s weight — because weight loss is a signal of infection and a good indicator of disease — and other clinical and pathological markers, such as temperature and mortality, and performed tissue analyses of the mice , to see how they respond.

The therapy prevented the mice from losing weight before they were exposed to the coronavirus, and also prevented death after infection.

Even within 12 hours of infection, the therapy showed very good efficacy, Aguilar-Carreno said.

 

 

 

 

 

 

 

 

 

References:

Tirosh Shapira et al. A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic. Nature, 2022, doi:10.1038/s41586-022-04661-w.

Small molecule TMPRSS2 inhibitor as nasal spray to prevent and treat COVID-19

(source:internet, reference only)


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