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Baloxavir Marboxil: A Review in Acute Uncomplicated Influenza

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Abstract

Baloxavir marboxil (Xofluza®; hereafter referred to as baloxavir), the prodrug of baloxavir acid, is a first-in-class, small molecule inhibitor of the polymerase acidic (PA) protein subunit of the influenza virus polymerase complex. Baloxavir (after conversion to baloxavir acid) acts to block influenza virus replication by inhibiting the cap-dependent endonuclease activity of the PA protein. Taken orally as a single dose, baloxavir is approved in the USA for the treatment of acute uncomplicated influenza in patients ≥ 12 years of age who have been symptomatic for ≤ 48 h. Data from randomized, double-blind, placebo- and oseltamivir-controlled phase III trials have shown that baloxavir is efficacious in improving influenza symptoms both in otherwise healthy adolescents and adults and in those at high risk of influenza complications, displaying similar efficacy to that of oseltamivir. Furthermore, there is evidence that baloxavir can reduce influenza viral load more rapidly than oseltamivir. Baloxavir has activity against influenza A and B viruses (including strains resistant to neuraminidase inhibitors) and is well tolerated. Evidence of the emergence and likely human-to-human transmission of variant viruses with reduced susceptibility to baloxavir highlights the importance of monitoring and surveillance for changes in influenza virus drug susceptibility patterns. However, currently available evidence suggests that baloxavir, with the benefits of a single oral dose regimen, provides a useful alternative to neuraminidase inhibitors for the treatment of acute uncomplicated influenza in adolescents and adults.

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Acknowledgements

During the peer review process, the manufacturer of baloxavir marboxil was also offered an opportunity to review this article. Changes resulting from comments received were made on the basis of scientific and editorial merit.

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    Matt Shirley

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Correspondence to Matt Shirley.

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The preparation of this review was not supported by any external funding.

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Matt Shirley is a salaried employee of Adis International Ltd/Springer Nature, is responsible for the article content and declares no relevant conflicts of interest.

Additional information

Additional information for this Adis Drug Evaluation can be found at https://doi.org/10.6084/m9.figshare.11929797.

The manuscript was reviewed by: S. Gravenstein, Department of Health Services, Policy & Practice School of Public Health and the Alpert Medical School Department of Medicine, Brown University, and Providence Veterans Administration Medical Center, Providence, RI, USA; L. Naesens, Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, KU Leuven, Leuven, Belgium.

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Shirley, M. Baloxavir Marboxil: A Review in Acute Uncomplicated Influenza. Drugs 80, 1109–1118 (2020). https://doi.org/10.1007/s40265-020-01350-8

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