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]
Identifiers
CAS Number
  • 2012558-47-1
DrugBank
UNII
KEGG
ChEMBL
ATC code
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

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

Mechanism of action

Bulevirtide binds and inactivates the sodium/bile acid cotransporter, blocking both viruses from entering hepatocytes.[4]

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[5][6] that can also dock to NTCP, blocking the virus's entry mechanism.[7]

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.[7]

References

  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. Francisco, Estela Miranda (29 May 2020). "Hepcludex". European Medicines Agency. Archived from the original on 15 June 2020. Retrieved 6 August 2020.
  5. 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.
  6. 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.
  7. 7.0 7.1 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

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