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Monodisperse Polysarcosine-based Highly-loaded Antibody-Drug Conjugates

preprint
revised on 17.12.2018 and posted on 17.12.2018 by Warren Viricel, Guy Fournet, Sabine Beaumel, Emeline Perrial, Sébastien Papot, Charles Dumontet, Benoît Joseph

We report the synthesis of monodisperse (i.e. discrete) polysarcosine compounds and their use as a hydrophobicity masking entity for the construction of highly-loaded homogeneous β- glucuronidase-responsive antibody-drug conjugates (ADCs). The highly hydrophilic drug-linker platform described herein improves drug-loading, physicochemical properties, pharmacokinetics and in vivo antitumor efficacy of the resulting conjugates.

Funding

Mablink Bioscience SA

Banque Publique d'Investissement (BPI France)

Cancéropôle Lyon Auvergne Rhône-Alpes (CLARA)

History

Email Address of Submitting Author

w.viricel@mablink.com

Institution

Mablink Bioscience SA

Country

France

ORCID For Submitting Author

0000-0001-8929-1497

Declaration of Conflict of Interest

Some authors are co-inventors on a PCT patent application related to this work and are shareholders of Mablink Bioscience SA.

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