A Monoclonal Antibody to ADAM17 Inhibits Tumor Growth by Inhibiting EGFR and Non-EGFR-Mediated Pathways

Mol Cancer Ther. 2015 Jul;14(7):1637-49. doi: 10.1158/1535-7163.MCT-14-1040. Epub 2015 May 6.

Abstract

ADAM17 is the primary sheddase for HER pathway ligands. We report the discovery of a potent and specific ADAM17 inhibitory antibody, MEDI3622, which induces tumor regression or stasis in many EGFR-dependent tumor models. The inhibitory activity of MEDI3622 correlated with EGFR activity both in a series of tumor models across several indications as well in as a focused set of head and neck patient-derived xenograft models. The antitumor activity of MEDI3622 was superior to that of EGFR/HER pathway inhibitors in the OE21 esophageal model and the COLO205 colorectal model suggesting additional activity outside of the EGFR pathway. Combination of MEDI3622 and cetuximab in the OE21 model was additive and eradicated tumors. Proteomics analysis revealed novel ADAM17 substrates that function outside of the HER pathways and may contribute toward the antitumor activity of the monoclonal antibody.

MeSH terms

  • ADAM Proteins / antagonists & inhibitors*
  • ADAM Proteins / immunology
  • ADAM Proteins / metabolism
  • ADAM17 Protein
  • Animals
  • Antibodies, Monoclonal / administration & dosage
  • Antibodies, Monoclonal / pharmacokinetics
  • Antibodies, Monoclonal / pharmacology*
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology
  • Blotting, Western
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cetuximab / administration & dosage
  • Cetuximab / pharmacology
  • Dose-Response Relationship, Drug
  • Drug Synergism
  • ErbB Receptors / antagonists & inhibitors*
  • ErbB Receptors / metabolism
  • Female
  • HCT116 Cells
  • HT29 Cells
  • Humans
  • Mice, Inbred DBA
  • Mice, Nude
  • Neoplasms / drug therapy*
  • Neoplasms / immunology
  • Neoplasms / metabolism
  • Signal Transduction / drug effects*
  • Treatment Outcome
  • Xenograft Model Antitumor Assays*

Substances

  • Antibodies, Monoclonal
  • ErbB Receptors
  • ADAM Proteins
  • ADAM17 Protein
  • ADAM17 protein, human
  • Adam17 protein, mouse
  • Cetuximab