Baloxavir marboxil

Baloxavir marboxil, sold under the brand name Xofluza, is an antiviral medication for treatment of influenza A and influenza B. It is taken as a single dose by mouth. It may reduce the duration of flu symptoms by about a day.

Baloxavir marboxil
Clinical data
Trade namesXofluza
Other namesS-033188/S-033447
AHFS/Drugs.comMonograph
MedlinePlusa618062
License data
Pregnancy
category
    Routes of
    administration
    By mouth
    ATC code
    Legal status
    Legal status
    Identifiers
    CAS Number
    PubChem CID
    UNII
    KEGG
    Chemical and physical data
    FormulaC27H23F2N3O7S
    Molar mass571.55 g·mol−1
    3D model (JSmol)

    It was approved for medical use in the United States in 2018. It was developed by Shionogi Co., a Japanese pharmaceutical company, and Roche AG.[1]

    Medical use

    As of 2019, in the only published phase III RCT of otherwise healthy outpatients, baloxavir reduced the duration of symptoms by about one day compared to placebo, which was the same as oseltamivir. On the first day after baloxavir was started the viral load decreased more than with either placebo or oseltamivir. However, after five days of oseltamivir the effect of a single dose of baloxavir was indistinguishable.[2]

    Resistance

    In 2.2% of baloxavir recipients in the phase II trial and in about 10% of baloxavir recipients in the phase III trial the influenza strain became resistant. This was due to polymerase acidic protein variants with I38T/M/F substitutions.[2]

    Side effects

    Common side effects are diarrhea and bronchitis.[3] Adverse events were reported in 21% of people who received baloxavir, 25% of those receiving placebo, and 25% of oseltamivir.[2]

    Mechanism of action

    Baloxavir marboxil is an influenza therapeutic agent (cap-dependent endonuclease inhibitor), characterized by taking a single dose by mouth. The pharmacodynamics of baloxavir marboxil are such that it inhibits the cap-dependent endonuclease activity of the influenza polymerase. It inhibits the process known as cap snatching, which is a mechanism exploited by viruses to hijack the host mRNA transcription system to allow synthesis of viral RNAs. It acts unlike neuraminidase inhibitors such as oseltamivir and zanamivir which inhibit the liberation of viruses from the infected cell surface.[4]

    Approval

    Baloxavir marboxil was approved for sale in Japan in February 2018.[5] On October 24, 2018, the U.S. Food and Drug Administration (FDA) approved it for the treatment of acute uncomplicated influenza in people 12 years of age and older who have been symptomatic for no more than 48 hours.[3] In October 2019, the FDA approved the use of Xofluza for people at high risk of developing influenza-related complications.[6]

    References

    1. Branswell, Helen (27 June 2018). "A flu drug — shown to reduce the duration of symptoms — could upend treatment in U.S." STAT.
    2. Hayden FG, Sugaya N, Hirotsu N, et al. (September 2018). "Baloxavir Marboxil for Uncomplicated Influenza in Adults and Adolescents". N. Engl. J. Med. 379 (10): 913–923. doi:10.1056/NEJMoa1716197. PMID 30184455.
    3. "FDA approves new drug to treat influenza". U.S. Food and Drug Administration (FDA) (Press release). 24 October 2018. Archived from the original on 24 October 2019. Retrieved 23 October 2019.
    4. Dias A, Bouvier D, Crépin T, et al. (April 2009). "The cap-snatching endonuclease of influenza virus polymerase resides in the PA subunit". Nature. 458 (7240): 914–8. Bibcode:2009Natur.458..914D. doi:10.1038/nature07745. PMID 19194459.
    5. "Xofluza (Baloxavir Marboxil) Tablets 10mg/20mg Approved For The Treatment Of Influenza Types A And B In Japan" (Press release). Shionogi & Co., Ltd. 23 February 2018 via www.publicnow.com.
    6. "Genentech Announces FDA Approval of Xofluza (Baloxavir Marboxil) for People at High Risk of Developing Influenza-Related Complications" (Press release). Genentech. 17 October 2019. Archived from the original on 24 October 2019. Retrieved 23 October 2019 via Business Wire.
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