Evaluation of Xa inhibitors as potential inhibitors of the SARS-CoV-2 Mpro protease

Based on previous large-scale in silico screening several factor Xa inhibitors were proposed to potentially inhibit SARS-CoV-2 M-pro. In addition to their known anticoagulants activity this potential inhibition could have an additional therapeutic effect on patients with COVID-19 disease. In this study we examined the binding of the Apixaban, Betrixaban and Rivaroxaban to the SARS-CoV-2 M-pro with the use of the MicroScale Thermophoresis technique. Our results indicate that the experimentally measured binding affinity is weak and the therapeutic effect due to the SARS-CoV-2 M-pro inhibition is rather negligible.

Automated summary

Based on in silico screening, factor Xa inhibitors were suggested to potentially inhibit SARS-CoV-2 M-pro. However, our study found that the binding affinity of Apixaban, Betrixaban, and Rivaroxaban to SARS-CoV-2 M-pro was weak, indicating a negligible therapeutic effect.