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Masitinib: Just 6 days to reduce 99% of the COVID-19 virus load. Since the outbreak of the novel coronavirus pneumonia (COVID-19) at the end of 2019, it has continued to spread globally. As of now, more than 190 million confirmed cases of COVID-19 have been reported globally, and more than 4.11 million patients have died. Caused a huge disaster.
In response to COVID-19, in addition to speeding up vaccination, it is also very urgent to find safer and effective treatment options. Due to the urgency of the epidemic, it is a good choice to screen drugs that are already on the market for the treatment and prevention of COVID-19.
On July 20, 2021, researchers from the University of Chicago and other institutions published a titled Masitinib is a broad coronavirus 3CL inhibitor that blocks replication of SARS-CoV-2 in the top international academic journal Science. Coronavirus 3CL inhibitor can block the 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-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 in just 6 days, and lung inflammation has also been reduced. In addition, Masitinib is equally effective against COVID-19 α, β, and γ mutants in in vitro experiments.
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. Among them, 8 drugs can effectively inhibit the activity of 3CLpro, the main protease of the new coronavirus. The most effective is a drug called masitinib, which is an oral tyrosine kinase inhibitor.
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. One half was treated with PBS as a control group, and the other half was treated with Masitinib (25 mg/kg) twice a day, starting 12 hours after infection for 10 days.
The experimental results showed that Masitinib quickly and effectively reduced the neo-coronavirus load in mice (reduced more than 99% of the viral load on the 6th day), with good safety, and reduced inflammation characteristics, and showed Potential benefits for survival and clinical scoring. It is worth noting that in vitro experiments have shown that Masitinib is equally effective on the COVID-19 α, β, and γ mutant strains.
Drugs targeting the new coronavirus 3CLpro are an attractive treatment option, partly because 3CLpro is considered to be less susceptible to drug resistance to the new coronavirus. Masitinib is a competitive inhibitor of 3CLpro. This direct-acting antiviral mechanism of action distinguishes Masitinib from many other COVID-19 treatment drugs (including polymerase inhibitors or monoclonal antibodies).
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. Oral Masitinib is a potential strategy for early treatment. The future development of masitinib analogs with lower anti-tyrosine kinase activity will help reduce its reported side effects.
In addition, Masitinib can effectively inhibit the new coronavirus and its mutant strains, and is also effective against a variety of coronaviruses and picornaviruses. It has the potential to treat other viral infections and can be used as a broad-spectrum antiviral drug.
(source:internet, reference only)