Baloxavir marboxil is a prodrug of S-033447. S-033447 is a small molecule inhibitor of the cap-dependent endonuclease of influenza A and B viruses, which developed by Shionogi & Roche.
Indication: Influenza
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Patent from Shionogi & Roche, expiry date(The U.S):Sep.21, 2031.
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Baloxavir marboxil, chemically designated as (1R,2S)-3-[4-amino-6-oxo-1-(2,2,2-trifluoroethyl)-5-(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-7-yl]-2-hydroxy-3-(4-methoxyphenyl)propanoic acid 2,2,2-trifluoroethyl ester, is a novel antiviral medication developed specifically for the treatment of influenza. Its molecular formula is C20H18F6N4O4, and it carries the CAS registry number 1976597-89-1. This compound functions as a prodrug, meaning it is biologically inactive in its administered form but is rapidly converted into its active metabolite, baloxavir, upon oral ingestion by hydrolysis within the body.
The primary therapeutic utility of baloxavir marboxil lies in its ability to inhibit the influenza A and B viruses. Unlike traditional neuraminidase inhibitors such as oseltamivir, which target the viral surface enzyme responsible for releasing new virions from infected cells, baloxavir targets the cap-dependent endonuclease activity of the viral polymerase complex PA subunit. By blocking this essential step in the viral replication cycle, the drug effectively halts the synthesis of viral RNA, thereby preventing the virus from multiplying and spreading within the host. Clinical studies have demonstrated that a single-dose regimen of baloxavir marboxil can significantly shorten the duration of influenza symptoms when administered within 48 hours of symptom onset. It is particularly advantageous for patients who cannot tolerate other antiviral therapies or require a convenient once-daily dosing schedule. Approved by regulatory agencies including the US FDA and the European Medicines Agency, it represents a significant advancement in influenza management, offering a distinct mechanism of action that helps combat potential resistance issues associated with existing treatments. While generally well-tolerated, common side effects may include diarrhea and bronchitis, though serious adverse events are rare. As a first-in-class inhibitor of the influenza polymerase, baloxavir marboxil provides clinicians with a powerful tool to mitigate the global burden of seasonal flu outbreaks.