Bulevirtide

Source: Wikipedia, the free encyclopedia.

Bulevirtide
Clinical data
Trade namesHepcludex
Other namesMyrB, Myrcludex-B[1]
License data
Subcutaneous
ATC code
Legal status
Legal status
Identifiers
JSmol)
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  • Key:WQNDXLHKAMIGEX-WOAPPVHJSA-N

Bulevirtide, sold under the brand name Hepcludex, is an antiviral medication for the treatment of chronic hepatitis D (in the presence of hepatitis B).[3]

The most common side effects include raised levels of bile salts in the blood and reactions at the site of injection.[3]

Bulevirtide works by attaching to and blocking a receptor (target) through which the hepatitis delta and hepatitis B viruses enter liver cells.[3] 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.[3]

Bulevirtide was approved for medical use in the European Union in July 2020.[3]

Structural formula

Bulevirtide is a 47-amino acid peptide with the following sequence:[5]

Asp-His-Gln-Leu-Asp-Pro-Ala-Phe-Gly-Ala-Asn-Ser-Asn-Asn-Pro-Asp-Trp-Asp-Phe-Asn-Pro-Asn-Lys-Asp-His-Trp-Pro-Glu-Ala-Asn-Lys-Val-Gly-NH2
(C13H27CO-GTNLSVPNPLGFFPDHQLDPAFGANSNNPDWDFNPNKDHWPEANKVG-NH2)

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.[3][6]

Pharmacology

Mechanism of action

Bulevirtide binds and inactivates the sodium/bile acid cotransporter, blocking both HBV and HDV viruses from entering hepatocytes.[7]

The

acylated pre-S1[8][9] that can also dock to NTCP, blocking the virus's entry mechanism.[10]

The drug is also effective against hepatitis D because the hepatitis D virus uses the same entry receptor as HBV and is only effective in the presence of a hepatitis B virus infection.[10]

Pre-clinical data in mice suggests that pharmacological inhibition of NTCP-mediated bile salt uptake may also be effective to lower hepatic bile salt accumulation in cholestatic conditions. This reduces hepatocellular damage.[11] An increased ratio of phospholipid to bile salts seen in bile upon NTCP inhibition may further contribute to the protective effect as bile salts are less toxic in presence of phospholipids.[12]

References

  1. S2CID 202674681
    .
  2. ^ "Hepcludex 2 mg powder for solution for injection - Summary of Product Characteristics (SmPC)". (emc). 30 March 2022. Retrieved 1 July 2022.
  3. ^ a b c d e f g "Hepcludex EPAR". European Medicines Agency (EMA). 26 May 2020. Retrieved 12 August 2020. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  4. ^ "Hepcludex Product information". Union Register of medicinal products. Retrieved 3 March 2023.
  5. PMID 34018034
    .
  6. ^ "Summary of opinion: Hepcludex" (PDF). European Medicines Agency. 28 May 2020.
  7. ^ Francisco EM (29 May 2020). "Hepcludex". European Medicines Agency. Archived from the original on 15 June 2020. Retrieved 6 August 2020.
  8. PMID 23246506
    .
  9. PMID 26327754
    .
  10. ^ a b Spreitzer H (14 September 2015). "Neue Wirkstoffe – Myrcludex B". Österreichische Apothekerzeitung (in German) (19/2015): 12.
  11. ^ Na+ -taurocholate cotransporting polypeptide inhibition has hepatoprotective effects in cholestasis in mice. Slijepcevic D, Roscam Abbing RLP, Fuchs CD, Haazen LCM, Beuers U, Trauner M, Oude Elferink RPJ, van de Graaf SFJ. Hepatology. 2018 Sep;68(3):1057-1069. doi: 10.1002/hep.29888
  12. PMID 31136002
    .

External links

  • "Bulevirtide". Drug Information Portal. U.S. National Library of Medicine.
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