Linkers having a crucial role in antibody–drug conjugates

Jun Lu, Feng Jiang, Aiping Lyu, Ge Zhang*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

196 Citations (Scopus)
246 Downloads (Pure)


Antibody–drug conjugates (ADCs) comprised of a desirable monoclonal antibody, an active cytotoxic drug and an appropriate linker are considered to be an innovative therapeutic approach for targeted treatment of various types of tumors and cancers, enhancing the therapeutic parameter of the cytotoxic drug and reducing the possibility of systemic cytotoxicity. An appropriate linker between the antibody and the cytotoxic drug provides a specific bridge, and thus helps the antibody to selectively deliver the cytotoxic drug to tumor cells and accurately releases the cytotoxic drug at tumor sites. In addition to conjugation, the linkers maintain ADCs’ stability during the preparation and storage stages of the ADCs and during the systemic circulation period. The design of linkers for ADCs is a challenge in terms of extracellular stability and intracellular release, and intracellular circumstances, such as the acid environment, the reducing environment and cathepsin, are considered as the catalysts to activate the triggers for initiating the cleavage of ADCs. This review discusses the linkers used in the clinical and marketing stages for ADCs and details the fracture modes of the linkers for the further development of ADCs.

Original languageEnglish
Article number561
Number of pages22
JournalInternational Journal of Molecular Sciences
Issue number4
Publication statusPublished - 14 Apr 2016

Scopus Subject Areas

  • Catalysis
  • Molecular Biology
  • Spectroscopy
  • Computer Science Applications
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Inorganic Chemistry

User-Defined Keywords

  • Antibody–drug conjugates
  • Attachment site
  • Cytotoxic drug
  • Linker
  • Monoclonal antibody
  • Tumor


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