Reducing hydrophobicity of homogeneous antibody-drug conjugates improves pharmacokinetics and therapeutic index
Abstract
The in vitro potency of antibody-drug conjugates (ADCs) increases with the drug-to-antibody ratio (DAR); however, ADC plasma clearance also increases with DAR, reducing exposure and in vivo efficacy. Here we show that accelerated clearance arises from ADC hydrophobicity, which can be modulated through drug-linker design. We exemplify this using hydrophilic auristatin drug linkers and PEGylated ADCs that yield uniform, high-DAR ADCs with superior...
Paper Details
Title
Reducing hydrophobicity of homogeneous antibody-drug conjugates improves pharmacokinetics and therapeutic index
Published Date
Jun 15, 2015
Journal
Volume
33
Issue
7
Pages
733 - 735
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