Pharmaceutical Research

, Volume 32, Issue 11, pp 3577–3583 | Cite as

Internalization, Trafficking, Intracellular Processing and Actions of Antibody-Drug Conjugates

Expert Review



This review discusses the molecular mechanism involved in the targeting and delivery of antibody-drug conjugates (ADCs), the new class of biopharmaceuticals mainly designed for targeted cancer therapy.


this review goes over major progress in preclinical and clinical studies of ADCs, in the past 5 years.


The pharmacokinetics and pharmacodynamics of ADCs involve multiple mechanisms, including internalization of ADCs by target cells, intracellular trafficking, release of conjugated drugs, and payload.


These mechanisms actually jointly determine the efficacy of ADCs. Therefore, the optimization of ADCs should take them as necessary rationales.


Antibody drug conjugate Internalization Recycling Trafficking Linker 



Antibody-drug conjugates


Antibody-dependent cellular cytotoxicity


Complement-dependent cytotoxicity


N(2′)-deacetyl-N(2′)-(3-mercapto-1-oxopropyl)- maytansine


Epidermal growth factor receptor


Neonatal Fc receptor


Monomethyl auristatin E


Maximum tolerated doses


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Copyright information

© Springer Science+Business Media New York 2015

Authors and Affiliations

  1. 1.Scientific Development Manager, Discovery BiologyGenScript USA Inc.PiscatawayUSA

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