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Intact plasma quantification of the large therapeutic lipopeptide bulevirtide

Bulevirtide is a first-in-class entry inhibitor of the hepatitis B and hepatitis delta virus blocking the sodium/bile acid co-transporter NTCP, and was recently approved for the treatment of hepatitis D as a priority medicine (prime) in an accelerated assessment by the European Medicines Agency. It...

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Bibliographic Details
Main Authors: Sauter, Max (Author) , Blank, Antje (Author) , Stoll, Felicitas E. (Author) , Lutz, Natalie (Author) , Haefeli, Walter E. (Author) , Burhenne, Jürgen (Author)
Format: Article (Journal)
Language:English
Published: 20 May 2021
In: Analytical and bioanalytical chemistry
Year: 2021, Volume: 413, Issue: 22, Pages: 5645-5654
ISSN:1618-2650
DOI:10.1007/s00216-021-03384-7
Online Access:Verlag, kostenfrei, Volltext: https://doi.org/10.1007/s00216-021-03384-7
Verlag, kostenfrei, Volltext: https://link.springer.com/10.1007/s00216-021-03384-7
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Author Notes:Max Sauter, Antje Blank, Felicitas Stoll, Natalie Lutz, Walter E. Haefeli, Jürgen Burhenne
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Summary:Bulevirtide is a first-in-class entry inhibitor of the hepatitis B and hepatitis delta virus blocking the sodium/bile acid co-transporter NTCP, and was recently approved for the treatment of hepatitis D as a priority medicine (prime) in an accelerated assessment by the European Medicines Agency. It is a very large lipopeptide comprising 47 amino acids in its sequence and a myristoylation at the N-terminus. For support of clinical development, we established highly sensitive plasma quantification assays using 100 μL of plasma, spanning concentrations of 0.1 to 100 ng/mL and 1 to 1000 ng/mL with the option to measure ten-fold diluted samples up to 10,000 ng/mL. Quantification was performed with UPLC-MS/MS measurements after extraction with protein precipitation. Both assays were fully validated according to the pertinent guidelines of the FDA and EMA, including incurred sample reanalyses and cross-validation using clinical study samples.
Item Description:Gesehen am 18.09.2023
Physical Description:Online Resource
ISSN:1618-2650
DOI:10.1007/s00216-021-03384-7

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