Canadian researchers have discovered an antiviral drug that blocks the SARS-CoV-2 virus from infecting lung cells. Promisingly, the small molecule drug known as N-0385 was shown to be highly effective against new emerging threats, the SARS-CoV-2 variants of concern.
“In this study, we report a novel and highly potent small-molecule drug called N-0385, that acts as the most effective entry inhibitor to date,” said lead researcher Dr. François Jean, a microbiologist at the University of British Columbia.
“We demonstrate that N-0385 is broadly protective against infection and mortality in mice, and believe N-0385 has potential as a viable early treatment option against emerging SARS-CoV-2 VOCs.”
Genetic variants of SARS-CoV-2 have begun to spread globally, with those displaying traits such as increased transmissibility, the ability to cause more severe COVID symptoms, and being able to evade vaccines and therapeutics classified as variants of concern. These include B.1.1.7 (first identified in the United Kingdom) and the B.1.351 variant (first isolated in South Africa).
In the study, uploaded onto the preprint server BioRxiv, Jean and colleagues showed that the broad spectrum antiviral N-0385 was able to stop the B.1.1.7 and B.1.351 variants from entering cultured human lung cells.
“N-0385 works by blocking TMPRSS2, an enzyme responsible for cutting and priming the viral spike protein so that it can attach and fuse with the host cell membrane, and release the virus’s genetic material,” explained Jean.
In animal studies, daily doses of N-0385 administered in the nose were shown to significantly increase the chances of survival in SARS-CoV-2-infected mice, without any detectable side effects.
“We hope that this, and related drugs, may have broader applications in combating other respiratory viruses that use the same means of entry into host cells, including established coronaviruses, influenza, and other viruses,” concludes Jean.