Doxorubicin overcomes resistance to drozitumab by antagonizing Inhibitor of Apoptosis Proteins (IAPs)

Anticancer Res. 2014 Dec;34(12):7007-20.

Abstract

Background/aim: Drozitumab is a fully human agonistic monoclonal antibody that binds to death receptor DR5 and induces apoptosis. However, drozitumab resistance is a major obstacle limiting anticancer efficacy.

Materials and methods: We examined the potential for the chemotherapeutic agent doxorubicin to overcome resistance against drozitumab-resistant breast cancer cells both in vitro and in vivo.

Results: Treatment with doxorubicin increased cell surface expression of DR5, reduced levels of Inhibitors of Apoptosis Proteins (cIAPs) and re-sensitised cells to drozitumab-induced apoptosis. Animals implanted with resistant breast cancer cells into the mammary fat pad and treated with a combination of drozitumab and doxorubicin showed inhibition of tumor growth and a substantial delay in tumor progression compared to untreated controls and mice treated with each agent alone.

Conclusion: These results suggest that combination of drozitumab with chemotherapy and agents that modulate IAP levels could potentially be a useful strategy in the treatment of breast cancer.

Keywords: Apo2L/TRAIL; Apoptosis; breast cancer; chemotherapy; drozitumab; drug resistance.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antibiotics, Antineoplastic / therapeutic use*
  • Antibodies, Monoclonal / therapeutic use*
  • Antibodies, Monoclonal, Humanized
  • Apoptosis / drug effects
  • Breast Neoplasms / drug therapy*
  • Cell Line, Tumor
  • Doxorubicin / therapeutic use*
  • Drug Resistance, Neoplasm / drug effects*
  • Drug Synergism
  • Female
  • Humans
  • Inhibitor of Apoptosis Proteins / antagonists & inhibitors*
  • Mice
  • Mice, Nude
  • Receptors, TNF-Related Apoptosis-Inducing Ligand / biosynthesis*
  • Xenograft Model Antitumor Assays

Substances

  • Antibiotics, Antineoplastic
  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Humanized
  • Inhibitor of Apoptosis Proteins
  • Receptors, TNF-Related Apoptosis-Inducing Ligand
  • Doxorubicin
  • drozitumab