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Since the outbreak of the novel coronavirus pneumonia (COVID-19) at the end of 2019, it has continued to spread globally.
In response to COVID-19, in addition to speeding up vaccination, it is also very urgent to find safer and effective treatment options
July 20, 2021, researchers at Chicago University and other institutions of top international academic journal Sciencepublished a paper entitled: masitinib the Broad IS A coronavirus that 3CL inhibitor of SARS-CoV Blocks of Replication-2 (masitinib is a wide range of Coronavirus 3CL inhibitor can block the replication of SARS-CoV-2)
ScienceScience Masitinib is a broad coronavirus 3CL inhibitor that blocks replication of SARS-CoV-2 Masitinib is a broad coronavirus 3CL inhibitor that blocks replication of SARS-CoV-2
The research team used the strategy of "new use of old drugs" and discovered masitinib (masitinib) from among 1,900 safe-to-use drugs, which is an oral tyrosine kinase inhibitor that can competitively inhibit the new coronavirus The activity of the main protease 3CLpro, thereby inhibiting the replication of the new coronavirus
In vivo experiments in mice showed that Masitinib treatment can reduce the titers of the new coronavirus in the lungs and nose of mice to less than 1% of the original, and lung inflammation has also been reduced in just 6 days
The research team screened a library of drugs that had been safely used in 1900 and found that 20 of them could effectively inhibit the replication of the new coronavirus in in vitro experiments
Further research found that Masitinib is a competitive inhibitor of 3CLpro
In order to evaluate the therapeutic effect of Masitinib on infection with the new coronavirus, the research team infected 20 K18-hACE2 transgenic mice intranasally with 2×10E4 PFU of the new coronavirus
The experimental results showed that Masitinib quickly and effectively reduced the neo-coronavirus load in mice (reduces the viral load by more than 99% on the 6th day), with good safety, and reduced inflammation characteristics, and showed Potential benefits for survival and clinical scoring
Drugs targeting the new coronavirus 3CLpro are an attractive treatment option, partly because 3CLpro is considered to be less susceptible to new coronavirus resistance
Finally, the research team said that the research data showed that Masitinib is the most beneficial in the early stages of infection and can produce the greatest antiviral effect
In addition, Masitinib can effectively inhibit the new coronavirus and its mutant strains, and is also effective against a variety of coronaviruses and picornaviruses.
Original source:
Original source:Nir Drayman, et al.
Masitinib is a broad coronavirus 3CL inhibitor that blocks replication of SARS-CoV-2
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