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Monodisperse Polysarcosine-Based Antibody-Drug Conjugates

28 November 2018, Version 1
Working Paper
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

We report the on-resin synthesis of monodisperse (i.e. discrete) polysarcosine compounds and their use as an hydrophobicity masking entity for the construction of highly-loaded homogeneous antibody-drug conjugates (ADC). The polysarcosine-based drug-linker platform described herein improves drug-loading, physicochemical properties, pharmacokinetics and shows excellent potency in vivo.

Keywords

Antibody-drug conjugates
ADC
Bioconjugation
Antibody
Polysarcosine
Cancer
Drug Delivery

Supplementary materials

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Version History

Nov 28, 2018 Version 1

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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.v1
D O I: 10.26434/chemrxiv.7388162.v1 [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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