Abstract

Recently,
Antibody-Drug Conjugates (ADCs) have been investigated as potential treatments for both liquid and
solid tumours. Indeed, the combination of a potent cytotoxic small
molecule payload linked to antibody targeted selectivity has many advantages. Therefore, three
conjugation methods to link these two entities were explored using active
payloads. Two different variations of MTGase conjugation were optimised to
provide the best conditions for obtaining homogenous and pure conjugates. Given
that all the methods used involve significant structural modifications to the antibody,
stability studies were carried out on the ADCs to examine the influence of the
DAR and conjugation method on stability, deconjugation and binding.