Monodisperse Polysarcosine-based Highly-loaded Antibody-Drug Conjugates

17 December 2018, Version 2
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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