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Masitinib, a potential wonder drug for COVID-19

2021-07-26

Since the outbreak of COVID-19 at the end of 2019, the epidemic is still spreading around the world. Up to now, more than 190 million confirmed cases of COVID-19 have been reported and more than 4.11 million deaths have been reported, causing a huge disaster for all mankind.

In addition to accelerating vaccination efforts for COVID-19, there is also an urgent need to find safer and more effective treatments. Review the flu (1918-2020), one hundred - year history, what really makes the human society from the impact of influenza is "flu vaccine + oral specific" "+ prevention" combination, especially oral anti-flu drugs (oseltamivir, etc.), let people after the flu virus, only need to medicine, simple protection can maintain the normal social activities.


For the prevention and control of COVID-19, "COVID-19 vaccine + oral anti-COVID-19 drug" is also a better choice, which is more convenient and has lower social cost. At present, there are a number of small molecule antiviral drug candidates in clinical research stage around the world. Recently, two more drugs have made new progress, bringing hope for victory in the fight against the epidemic.


Masitinib is a new drug

Masitinib is an oral tyrosine kinase inhibitor that competitively inhibits the activity of 3CLpro, the main protease of the Novel Coronavirus, and thus inhibits replication of the novel Coronavirus.


In vivo tests in mice showed that masitinib treatment reduced the Novel coronavirin titers in the lungs and nose of mice to less than 1% of their original level and reduced lung inflammation in just six days. In addition, Masitinib was also effective against α, β and γ mutant strains of COVID-19 in vitro.


The Masitinib study used an "old drug, new drug" strategy -- scientists first sifted through 1,900 drugs already in clinical use, looking for drugs that could inhibit common coronavirus infections.


A total of 108 drugs emerged from the study and were further tested for inhibition of the Novel coronavirus. Eventually, the researchers began to evaluate whether the 20 drugs they identified would inhibit the key target of 3CLpro, the most potent of which was a molecule called Masitinib.


The researchers actually evaluated masitinib's anti-CORONAVIRUS effect in animal models. They used 20 mice expressing the human ACE2 receptor and infected them with the Novel coronavirus through the nose. The mice were then divided into two groups, one to receive masitinib (25 mg/kg twice daily) and the other to receive a placebo as a control.

On the sixth day of treatment, the researchers began to analyze the effects of the treatment and found that Masitinib significantly reduced virus titers in the lungs and nose of the mice and improved lung pathology. Survival, weight loss, and clinical scores also improved.


Taken together, the researchers showed that Masitinib reduced viral load by more than 99 percent by the sixth day of treatment. At the end of the paper, the researchers concluded that Masitinib showed a good antiviral effect and reduced lung inflammation and enhanced lung function. The efficacy of this therapy in COVID-19 patients should be evaluated. Mechanistically, masitinib's best window for treatment is early in the infection, because it is expected to significantly inhibit viral replication and control the disease in the first place. The nature of oral administration also makes it easier to use.


In addition, masitinib is effective against multiple coronaviruses and small RNA viruses in addition to the Novel Coronavirus and its mutant strains, and has the potential to treat other viral infections as a broad-spectrum antiviral.