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Synonyms: BLV | formerly Myrcludex B | Hepcludex®
bulevirtide is an approved drug (EMA (2020), UK HMRA (2021))
Compound class:
Peptide or derivative
Comment: Bulevirtide is a lipopeptide antiviral agent. It blocks entry of the hepatitis-causing viruses HBV and HDV into hepatocytes [1]. The peptide structure of bulevirtide is derived from the pre-S1 domain of the large envelope protein of HBV surface antigen (HBsAg) [4], that binds to the heoatocyte expressed surface protein sodium/bile acid and sulphated solute cotransporter 1 (NTCP; SLC10A1) to mediate viral entry into host cells. Bulevirtide functionally blocks this entry process [3].
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| References |
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1. Blank A, Markert C, Hohmann N, Carls A, Mikus G, Lehr T, Alexandrov A, Haag M, Schwab M, Urban S et al.. (2016)
First-in-human application of the novel hepatitis B and hepatitis D virus entry inhibitor myrcludex B. J Hepatol, 65 (3): 483-9. [PMID:27132172] |
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2. Kang C, Syed YY. (2020)
Bulevirtide: First Approval. Drugs, 80 (15): 1601-1605. [PMID:32926353] |
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3. Petersen J, Dandri M, Mier W, Lütgehetmann M, Volz T, von Weizsäcker F, Haberkorn U, Fischer L, Pollok JM, Erbes B et al.. (2008)
Prevention of hepatitis B virus infection in vivo by entry inhibitors derived from the large envelope protein. Nat Biotechnol, 26 (3): 335-41. [PMID:18297057] |
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4. Schulze A, Schieck A, Ni Y, Mier W, Urban S. (2010)
Fine mapping of pre-S sequence requirements for hepatitis B virus large envelope protein-mediated receptor interaction. J Virol, 84 (4): 1989-2000. [PMID:20007265] |
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5. Wedemeyer H, Aleman S, Brunetto MR, Blank A, Andreone P, Bogomolov P, Chulanov V, Mamonova N, Geyvandova N, Morozov V et al.. (2023)
A Phase 3, Randomized Trial of Bulevirtide in Chronic Hepatitis D. N Engl J Med, 389 (1): 22-32. [PMID:37345876] |
