Baloxavir marboxil
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Baloxavir marboxil is a polymerase acidic endonuclease inhibitor used to treat uncomplicated influenza.
Baloxavir marboxil is a polymerase acidic endonuclease inhibitor used to treat uncomplicated influenza.
The influenza virus RNA polymerase complex is a heterotrimer made up of three protein subunits - polymerase basic protein 1 (PB1), polymerase basic protein 2 (PB2), and polymerase acidic protein (PA). This polymerase complex is an influenza virus-specific enzyme essential for viral gene transcription and replication, with its subunits playing different roles in viral mRNA synthesis. The PB2 subunit binds to the cap of host cellular pre-messenger RNA, allowing the PA protein - a cap-dependent endonuclease - to cleave the capped pre-messenger RNA. This initial step of mRNA synthesis by the PA protein, also known as the "cap-snatching process," provides an RNA primer for the PB1 subunit, which carries out its RNA-dependent RNA polymerase function to proceed with viral mRNA transcription. After administration, the prodrug baloxavir marboxil is almost completely hydrolyzed by esterases in the gastrointestinal lumen, intestinal epithelium, liver and blood to its active metabolite, baloxavir. Baloxavir selectively inhibits the PA protein, blocking the initiation of mRNA synthesis and ultimately influenza virus proliferation. Cap-dependent endonuclease is a highly conserved region across influenza strains; however, baloxavir is still vulnerable to resistance because amino acid substitutions in the PA protein can lead to reduced viral susceptibility to baloxavir.
Baloxavir marboxil is an influenza virus polymerase acidic (PA) endonuclease inhibitor indicated for the treatment of acute uncomplicated influenza in patients who have been symptomatic for no more than 48 hours and who are otherwise healthy adults and pediatric patients five years of age and older, or patients 12 years of age and older who are at high risk of developing influenza-related complications. The drug is also indicated for post-exposure prophylaxis of influenza in patients five years of age and older following contact with an individual who has influenza. In Europe, it is approved for use in patients aged one year and above for these indications. Baloxavir marboxil is associated with a risk for loss of efficacy due to changes in influenza virus such as changes in virus subtypes, emergence of virus resistance, and changes in viral virulence; therefore, the drug should be used after considering available information on drug susceptibility patterns for circulating influenza virus strains.
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