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Monodisperse Polysarcosine-based Highly-loaded Antibody-Drug Conjugates

preprint
revised on 17.12.2018, 07:57 and posted on 17.12.2018, 13:13 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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