Linker and Conjugation Site Synergy in Antibody-Drug Conjugates: Impacts on Biological Activity.

ABSTRACT: Antibody-drug conjugates (ADCs) produced using general conjugation methods yield heterogeneous products containing mixtures of species with different numbers of payloads per antibody (drug-antibody ratios) conjugated at multiple sites. This heterogeneity affects the stability, efficacy, and safety of ADCs. Thus, various site-specific conjugation methods have been developed to achieve homogeneity in ADCs. It was reported that linker structures and conjugation sites generally affected the characteristics of site-specific ADCs such as stability, efficacy, and safety. However, the combined effects of conjugation sites and linker structures on the physicochemical and biological characteristics of site-specific ADCs have remained unclear. In this study, we generated 30 homogeneous site-specific

SUBMITTER: Aoyama M 

PROVIDER: S-EPMC11488503 | biostudies-literature | 2024 Oct

REPOSITORIES: biostudies-literature