1. Academic Validation
  2. Payload diversification: a key step in the development of antibody-drug conjugates

Payload diversification: a key step in the development of antibody-drug conjugates

  • J Hematol Oncol. 2023 Jan 17;16(1):3. doi: 10.1186/s13045-022-01397-y.
Louise Conilh 1 2 Lenka Sadilkova 3 Warren Viricel 3 Charles Dumontet 4 5
Affiliations

Affiliations

  • 1 Cancer Research Center of Lyon, UMR INSERM 1052; CNRS 5286, University of Lyon, Lyon, France. l.conilh@mablink.com.
  • 2 Mablink Bioscience, Lyon, France. l.conilh@mablink.com.
  • 3 Mablink Bioscience, Lyon, France.
  • 4 Cancer Research Center of Lyon, UMR INSERM 1052; CNRS 5286, University of Lyon, Lyon, France.
  • 5 Hospices Civils de Lyon, Lyon, France.
Abstract

Antibody-drug conjugates (ADCs) is a fast moving class of targeted biotherapeutics that currently combines the selectivity of monoclonal Antibodies with the potency of a payload consisting of cytotoxic agents. For many years microtubule targeting and DNA-intercalating agents were at the forefront of ADC development. The recent approval and clinical success of trastuzumab deruxtecan (Enhertu®) and sacituzumab govitecan (Trodelvy®), two Topoisomerase 1 inhibitor-based ADCs, has shown the potential of conjugating unconventional payloads with differentiated mechanisms of action. Among future developments in the ADC field, payload diversification is expected to play a key role as illustrated by a growing number of preclinical and clinical stage unconventional payload-conjugated ADCs. This review presents a comprehensive overview of validated, forgotten and newly developed payloads with different mechanisms of action.

Keywords

Antibody–drug conjugates; Cytotoxic molecule; Payload; Topoisomerase 1 inhibitor.

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