Methods to Design and Synthesize Antibody-Drug Conjugates (ADCs)

Int J Mol Sci. 2016 Feb 2;17(2):194. doi: 10.3390/ijms17020194.

Abstract

Antibody-drug conjugates (ADCs) have become a promising targeted therapy strategy that combines the specificity, favorable pharmacokinetics and biodistributions of antibodies with the destructive potential of highly potent drugs. One of the biggest challenges in the development of ADCs is the application of suitable linkers for conjugating drugs to antibodies. Recently, the design and synthesis of linkers are making great progress. In this review, we present the methods that are currently used to synthesize antibody-drug conjugates by using thiols, amines, alcohols, aldehydes and azides.

Keywords: antibody-drug conjugates (ADCs); drugs; linkers; monoclonal antibodies (mAbs); targeted therapy.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antibodies, Monoclonal / chemistry*
  • Antineoplastic Agents / chemistry*
  • Cross-Linking Reagents / chemistry
  • Drug Design*
  • Humans
  • Immunoconjugates / chemistry*

Substances

  • Antibodies, Monoclonal
  • Antineoplastic Agents
  • Cross-Linking Reagents
  • Immunoconjugates