Cysteine-based coupling: challenges and solutions

J You, J Zhang, J Wang, M Jin - Bioconjugate Chemistry, 2021 - ACS Publications
J You, J Zhang, J Wang, M Jin
Bioconjugate Chemistry, 2021ACS Publications
Antibody–drug conjugates (ADCs) have attracted great attention in recent years in the wake
of an accelerated FDA approval rate and several large-scale acquisitions. To date, there are
ten ADC drugs on the market and more than 70 in various stages of clinical trials. Yet, due to
the complicated nature of ADC molecules, considerations need to cover many aspects for
the success of ADCs, including target specificity, linker–payload stability, tumor permeability,
and clearance rate. This topical review summarizes and discusses current methods used to …
Antibody–drug conjugates (ADCs) have attracted great attention in recent years in the wake of an accelerated FDA approval rate and several large-scale acquisitions. To date, there are ten ADC drugs on the market and more than 70 in various stages of clinical trials. Yet, due to the complicated nature of ADC molecules, considerations need to cover many aspects for the success of ADCs, including target specificity, linker–payload stability, tumor permeability, and clearance rate. This topical review summarizes and discusses current methods used to increase stability and homogeneity of ADCs of cysteine conjugation. We believe that they will lead to improvement of efficacy and pharmacokinetics (PK) of ADC drugs.
ACS Publications