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@ARTICLE{Walter:300194,
author = {J. D. Walter and M. Beffinger and P. Egloff and I.
Zimmermann and L. M. Hürlimann and F. Ackle and M. Seifert
and S. Kobold$^*$ and J. Vom Berg and M. A. Seeger},
title = {{F}lycodes enable simultaneous preclinical analysis for
dozens of antibodies in single cassette-dosed mice.},
journal = {Proceedings of the National Academy of Sciences of the
United States of America},
volume = {122},
number = {12},
issn = {0027-8424},
address = {Washington, DC},
publisher = {National Acad. of Sciences},
reportid = {DKFZ-2025-00671},
pages = {e2426481122},
year = {2025},
abstract = {Protein therapeutics such as antibodies require in-depth in
vivo characterization during development and consequently
account for a large proportion of laboratory animal
consumption in the pharmaceutical industry. Currently,
antibody candidates are exhaustively tested one-by-one in
animal models to determine pharmacokinetic and
pharmacodynamic (PK/PD) profiles. The simultaneous analysis
of antibody mixtures in single animals, called
cassette-dosing, could in principle overcome this
bottleneck, but is currently limited to small cassette
sizes. Here, we demonstrate how the use of genetically
encoded peptide tags (flycodes), designed for maximal
detectability in liquid chromatography-mass spectrometry,
can allow for the simultaneous characterization of large
pools of drug candidates, from single cassette-dosed mice.
We demonstrate the simultaneous assessment of PK parameters
for a group of >20 marketed/development-stage antibodies.
Biodistribution experiments in mice bearing EGFR-expressing
tumors correctly identified the two pool members recognizing
EGFR, while organ analysis registered liver accumulation of
an antibody targeting glucagon receptor, a protein
profoundly expressed in that organ. In analogy to an
early-phase drug development campaign, we performed
biophysical and PK analysis for a cassette of 80 unique
bispecific DARPin-sybody molecules. The data shown in this
study originate from only 18 cassette-dosed mice, thereby
demonstrating how flycode technology efficiently advances
preclinical discovery pipelines allowing a direct comparison
of drug candidates under identical experimental conditions.},
keywords = {Animals / Mice / ErbB Receptors: immunology / Humans /
Tissue Distribution / Antibodies: immunology /
Chromatography, Liquid: methods / Antibodies, Monoclonal:
pharmacokinetics / Antibodies, Monoclonal: immunology / Drug
Evaluation, Preclinical: methods / Female / antibodies
(Other) / cassette dosing (Other) / flycodes (Other) / mass
spectrometry (Other) / sybodies (Other) / ErbB Receptors
(NLM Chemicals) / Antibodies (NLM Chemicals) / Antibodies,
Monoclonal (NLM Chemicals)},
cin = {MU01},
ddc = {500},
cid = {I:(DE-He78)MU01-20160331},
pnm = {899 - ohne Topic (POF4-899)},
pid = {G:(DE-HGF)POF4-899},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:40096612},
doi = {10.1073/pnas.2426481122},
url = {https://inrepo02.dkfz.de/record/300194},
}