Antibody-drug conjugates (ADCs) take the advantage of antigen specificity of monoclonal
antibodies to deliver highly potent cytotoxic drugs selectively to antigen-expressing tumor cells. The
recent approval of Adcetris™ and Kadcyla™ as well as emerging data from numerous ongoing
clinical trials underscore the role of ADCs as a new therapeutic option for cancer patients. However,
conventional conjugation methods generally result in a heterogeneous mixture of ADCs, which can
result in significant therapeutic liabilities and can lead to complicated manufacturing processes. The
increased understanding from the clinical investigation of current ADCs and site-specific bioconjugation
technologies has enabled scientists to accelerate the discovery and development of the next generation ADCs
with defined and homogeneous composition. The present manuscript reviews the recent advances and trends in the
research and development of novel ADCs obtained by site-specific conjugation method.
Keywords: Antibody-drug conjugates, ADCs, conjugation site, DAR, homogeneous ADCs, site specific conjugation.
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