Antibody-drug Conjugate Targets, Drugs, and Linkers

Beverly A Teicher1, Joel Morris1

  • 1Developmental Therapeutics Program, DCTD, National Cancer Institute, Bethesda, MD 20892, USA.

Current Cancer Drug Targets
|February 25, 2022
PubMed

Insights

Antibody-drug conjugates (ADCs) precisely deliver potent drugs to tumors. This review examines 78 potential ADC targets, highlighting successful FDA-approved options and ongoing clinical research for effective cancer therapy.

Area of Science:

  • Oncology
  • Pharmacology
  • Biotechnology

Background:

  • Antibody-drug conjugates (ADCs) represent a targeted cancer therapy approach.
  • ADCs aim to deliver cytotoxic agents specifically to tumor cells, minimizing damage to healthy tissues.
  • The efficacy of ADCs relies on identifying suitable antibody targets with high tumor cell expression and low normal cell expression.

Purpose of the Study:

  • To review and analyze a comprehensive list of 78 potential antibody targets investigated for ADC applications.
  • To discuss the characteristics of potent cytotoxic drug payloads and linker technologies essential for ADC development.
  • To identify key factors contributing to the success of antibody-drug conjugate therapies.

Main Methods:

  • Literature review and analysis of 78 antibody targets explored for ADC development.
  • Discussion of cytotoxic payloads and linker chemistries used in ADCs.
  • Evaluation of clinical success and ongoing interest in various ADC targets.

Main Results:

  • A significant number of targets have been evaluated, with some abandoned and others leading to FDA-approved drugs.
  • Several targets continue to be of high interest for active clinical development.
  • The review covers various cytotoxic payloads and linker strategies employed in ADC design.

Conclusions:

  • Successful ADCs depend on the careful selection of antibody targets with specific expression profiles.
  • Potent cytotoxic payloads and appropriate linker stability are critical for ADC efficacy and safety.
  • Ongoing research and development continue to advance the field of antibody-drug conjugates for cancer treatment.

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