Advancing antibody drug conjugation: from the laboratory to a clinically approved anticancer drug

Hematol Oncol Clin North Am. 2014 Feb;28(1):13-25. doi: 10.1016/j.hoc.2013.10.009.


The concept of using monoclonal antibodies for delivering drugs to cancer cells has been explored for decades, with early work surrounding nonspecific targets and drugs with low potencies. These studies underscored the importance of critical parameters, such as antigen and tumor target selection, linker stability, drug potency, pharmacokinetics, and conjugation methodology, in developing effective antibody drug conjugates with acceptable safety profiles. Brentuximab vedotin represents the culmination of much research and development activities in which many of these parameters were addressed. This article provides an overview of many studies that led to the development of this highly active antibody drug conjugate.

Keywords: Chemotherapeutic; Drug delivery; Immunotherapy; Monoclonal antibody; Targeting; Tumor.

Publication types

  • Review

MeSH terms

  • Animals
  • Antibodies, Monoclonal / pharmacology
  • Antibodies, Monoclonal / therapeutic use*
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Brentuximab Vedotin
  • Clinical Trials as Topic
  • Drug Evaluation, Preclinical
  • Humans
  • Immunoconjugates / pharmacology
  • Immunoconjugates / therapeutic use*
  • Ki-1 Antigen / antagonists & inhibitors
  • Treatment Outcome


  • Antibodies, Monoclonal
  • Antineoplastic Agents
  • Immunoconjugates
  • Ki-1 Antigen
  • Brentuximab Vedotin