Baloxavir Marboxil

- Overview
  - Baloxavir Marboxil is a synthetic antiviral compound. It has activity against viruses causing influenza A and influenza B. It originated by Shionogi (Japan).
    It is a small molecule inhibitor of cap-dependent endonuclease found in of influenza A and B viruses. It is a pro-drug that is converted via hydrolysis to its active form, Baloxavir Acid.
    Baloxavir Marboxil is soluble in DMSO.
    
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    Background
    
    Baloxavir Marboxil has a unique mechanism of action as a cap-dependent endonuclease inhibitor. It inhibits the process called cap snatching, which is a mechanism used by viruses to hijack the host’s mRNA transcription system and synthesize their own viral RNAs.
- Properties
  - CAS Number
    
    1985606-14-1
    
    Molecular Formula
    
    C27H23F2N3O7S
    
    Molecular Weight
    
    571.55
    
    Appearance
    
    White or off-white powder
    
    Other Properties
    
    Source: Synthetic
    
    Storage
    
    -20°C
    
    * For research use only
- Applications
  - Application Description
    
    Spectrum: Effective against viruses causing influenza A and influenza B, including strains resistant to current antiviral agents.
    
    Microbiology Applications: Viruses have been detected that are resistant to Baloxavir Marboxil owing to an I38 mutation of cap-dependent endonuclease (CEN)(Yoshino et al, 2019).
    While it is being studied for COVID-19 no published evidence supports its use to date.
    
    Eukaryotic Cell Culture Applications: Baloxavir Acid was assayed along with a different class of antivirals, the neuraminidase inhibitors (oseltamivir acid, zanamivir hydrate, laninamivir, peramivir trihydrate) to evaluate its effectiveness in combination. Madin-Darby Canine Kidney (MDCK) cells were used in cell viability assays infected with influenza virus A/PR/8/34 strain. Results indicated that Baloxavir Acid (tested at 1.25 – 80 nmol/L) had a synergistic effect in vitro. There was no evidence of cytotoxicity for Baloxavir Acid alone or in combination (Fukao et al, 2019).