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    Bulevirtide

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    Bulevirtide
    Names
    Trade namesHepcludex
    Other namesMyrB, Myrcludex-B[1]
    Clinical data
    Routes of
    use    		Subcutaneous injection
    Legal
    License data
    Legal status
    • EU: Rx-only [2]
    Chemical and physical data
    FormulaC248H355N65O72
    Molar mass5398.951 g·mol−1


    Bulevirtide, sold under the brand name Hepcludex, is an antiviral medication for the treatment of hepatitis D.[2]

    The most common side effects include raised levels of bile salts in the blood and reactions at the site of injection.[2]

    Bulevirtide works by attaching to and blocking a receptor (target) through which the hepatitis delta and hepatitis B viruses enter liver cells.[2] By blocking the entry of the virus into the cells, it limits the ability of HDV to replicate and its effects in the body, reducing symptoms of the disease.[2]

    Bulevirtide was approved for medical use in the European Union in July 2020.[2]

    Medical uses[edit | edit source]

    Bulevirtide is indicated for the treatment of chronic hepatitis delta virus (HDV) infection in plasma (or serum) HDV-RNA positive adult patients with compensated liver disease.[2][3]

    Pharmacology[edit | edit source]

    Mechanism of action involves binding to and inactivating NTCP receptor[4][5]

    Mechanism of action[edit | edit source]

    Bulevirtide binds and inactivates the sodium/bile acid cotransporter, blocking both viruses from entering hepatocytes.[6]

    The hepatitis B virus uses its surface lipopeptide pre-S1 for docking to mature liver cells via their sodium/bile acid cotransporter (NTCP) and subsequently entering the cells. Myrcludex B is a synthetic N-acylated pre-S1[7][8] that can also dock to NTCP, blocking the virus's entry mechanism.[9]

    The drug is also effective against hepatitis D because the hepatitis D virus is only infective in the presence of a hepatitis B virus infection.[9]

    References[edit | edit source]

    1. ↑ Deterding, K.; Wedemeyer, H. (2019). "Beyond Pegylated Interferon-Alpha: New Treatments for Hepatitis Delta". AIDS Reviews. 21 (3): 126–134. doi:10.24875/AIDSRev.19000080. PMID 31532397.
    2. ↑ 2.0 2.1 2.2 2.3 2.4 2.5 2.6 "Hepcludex EPAR". European Medicines Agency (EMA). 26 May 2020. Archived from the original on 12 December 2021. Retrieved 12 August 2020. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
    3. ↑ "Summary of opinion: Hepcludex" (PDF). European Medicines Agency. 28 May 2020. Archived (PDF) from the original on 22 July 2021. Retrieved 21 April 2021.
    4. ↑ Liu, Hongtao; Zakrzewicz, Dariusz; Nosol, Kamil; Irobalieva, Rossitza N.; Mukherjee, Somnath; Bang-Sørensen, Rose; Goldmann, Nora; Kunz, Sebastian; Rossi, Lorenzo; Kossiakoff, Anthony A.; Urban, Stephan; Glebe, Dieter; Geyer, Joachim; Locher, Kaspar P. (20 March 2024). "Structure of antiviral drug bulevirtide bound to hepatitis B and D virus receptor protein NTCP". Nature Communications. 15 (1). doi:10.1038/s41467-024-46706-w.
    5. ↑ Sandmann, Lisa; Cornberg, Markus (16 April 2021). "Experimental Drugs for the Treatment of Hepatitis D". Journal of Experimental Pharmacology. 13: 461–468. doi:10.2147/JEP.S235550.
    6. ↑ Francisco, Estela Miranda (29 May 2020). "Hepcludex". European Medicines Agency. Archived from the original on 15 June 2020. Retrieved 6 August 2020.
    7. ↑ Volz T, Allweiss L, Ben MBarek M, Warlich M, Lohse AW, Pollok JM, et al. (May 2013). "The entry inhibitor Myrcludex-B efficiently blocks intrahepatic virus spreading in humanized mice previously infected with hepatitis B virus". Journal of Hepatology. 58 (5): 861–7. doi:10.1016/j.jhep.2012.12.008. PMID 23246506.
    8. ↑ Abbas Z, Abbas M (August 2015). "Management of hepatitis delta: Need for novel therapeutic options". World Journal of Gastroenterology. 21 (32): 9461–5. doi:10.3748/wjg.v21.i32.9461. PMC 4548107. PMID 26327754.
    9. ↑ 9.0 9.1 Spreitzer H (14 September 2015). "Neue Wirkstoffe – Myrcludex B". Österreichische Apothekerzeitung (in German) (19/2015): 12.{{cite journal}}: CS1 maint: unrecognized language (link)

    External links[edit | edit source]

    Identifiers:
    • "Bulevirtide". Drug Information Portal. U.S. National Library of Medicine. Archived from the original on 23 April 2021. Retrieved 21 April 2021.


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