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.
|Mechanism of Action||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.|
|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).|
Dias A et al (2009) The cap-snatching endonuclease of influenza virus polymerase residues in the PA subunit. Nature 458:914-918 PMID 19194459
Dong LH and Cao XR (2018) Studies of the interaction of influenza virus RNA polymerase PAN with endonuclease inhibitors. Interdiscip. Sci. 10(2):430-437 PMID 28631174
Hayden FG (2018) Baloxavir Marboxil for uncomplicated influenza in adults and adolescents. N. Eng. J Med. 379(10):913-923 PMID 30184455
Yoshino R, Yasuo N, Sekijima M (2019) Molecular dynamics simulation reveals the mechanism by which the influenza cap-dependent endonuclease acquires resistance against Baloxavir Marboxil. Sci.Rep. 29(1):17464 PMID 31767949