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Monodisperse Polysarcosine-based Highly-loaded Antibody-Drug Conjugates

17 December 2018, Version 2
Working Paper
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

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.

Keywords

Antibody-drug conjugates
ADC
Bioconjugation
Antibody
Polysarcosine
Cancer
Drug Delivery

Supplementary materials

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Now Published

Monodisperse polysarcosine-based highly-loaded antibody-drug conjugates [opens in a new tab]
Warren Viricel, Guy Fournet, Sabine Beaumel, Emeline Perrial, Sébastien Papot, Charles Dumontet, Benoît Joseph journal article
Chemical Science , Volume 10, Issue 14
Online publication date: 2019

Version History

Dec 17, 2018 Version 2

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The content is available under CC BY NC ND 4.0 [opens in a new tab]

DOI

10.26434/chemrxiv.7388162.v2
D O I: 10.26434/chemrxiv.7388162.v2 [opens in a new tab]

Funding

Mablink Bioscience SA
Banque Publique d'Investissement (BPI France)
Cancéropôle Lyon Auvergne Rhône-Alpes (CLARA)

Author’s competing interest statement

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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