AB Science announces the signing of an exclusive licensing agreement with the University of Chicago to conduct research for the prevention and treatment of Covid-19 - Seite 3

Masitinib in COVID-19

Research led by the University of Chicago [1] have shown that masitinib inhibits 3CLpro, a SARS-CoV-2 protease that is crucial for virus infection and reproduction, by directly binding to the protease catalytic site.

• Key points from this research article include:
  • The study objective was to identify safe-in-human drugs with potential anti-coronavirus properties from an initial library of 1,900 compounds, either approved for human use or with extensive safety data in humans (Phase 2 or 3 clinical trials).
  • Masitinib significantly inhibited SARS-CoV-2 replication in human lung cells.
  • Notably, masitinib completely inhibited 3CLpro activity. 3CLpro is the SARS-CoV-2 main protease, necessary for its viral replication cycle.
  • X-ray crystallography revealed that masitinib directly binds to the active site of 3CLpro, thereby having a direct antiviral activity by blocking its enzymatic activity.
  • Masitinib was also effective in blocking the replication of multiple picornaviruses (human pathogens that cause a range of diseases including meningitis, hepatitis, and poliomyelitis).
  • Overall, masitinib was shown to have broad anti-coronavirus and anti-picornavirus activity.

A Phase 2 study is on-going to evaluate masitinib in combination with isoquercetin for the treatment of COVID-19. This study (AB20001) is a randomized (1:1), double-blind, placebo-controlled Phase 2 clinical trial to evaluate the safety and efficacy of masitinib combined with isoquercetin in hospitalized patients with moderate and severe COVID-19. The study will enroll 200 patients (age ≥18 without an upper age limit) at medical centers in France and other countries. The primary objective is to improve the clinical status of patients after 15 days of treatment.

[1] Drayman N, Jones KA, Azizi S-A, et al. Drug repurposing screen identifies masitinib as a 3CLpro inhibitor that blocks replication of SARS-CoV-2 in vitro. bioRxiv 2020.08.31.274639; doi: https://doi.org/10.1101/2020.08.31.274639

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