Mechanisms of resistance to anti-EGFR therapy in colorectal cancer

Oncotarget. 2017 Jan 17;8(3):3980-4000. doi: 10.18632/oncotarget.14012.

Abstract

Targeting the epidermal growth factor receptor (EGFR) either alone or in combination with chemotherapy is effective for patients with RAS wild type metastatic colorectal cancer (mCRC). However, only a small percentage of mCRC patients are sensitive to anti-EGFR therapy and even the best cases finally become refractory to this therapy. It has become apparent that the RAS mutations correlate with resistance to anti-EGFR therapy. However, these resistance mechanisms only account for nearly 35% to 50% of nonresponsive patients, suggesting that there might be additional mechanisms. In fact, several novel pathways leading to escape from anti-EGFR therapy have been reported in recent years. In this review, we provide an overview of known and novel mechanisms that contribute to both primary and acquired anti-EGFR therapy resistance, and enlist possible treatment strategies to overcome or reverse this resistance.

Keywords: acquired resistance; colorectal cancer; epidermal growth factor receptor; primary resistance; targeted drug.

Publication types

  • Review

MeSH terms

  • Antibodies, Monoclonal / pharmacology
  • Antibodies, Monoclonal / therapeutic use
  • Cetuximab / pharmacology
  • Cetuximab / therapeutic use
  • Colorectal Neoplasms / drug therapy
  • Colorectal Neoplasms / genetics*
  • Drug Resistance, Neoplasm*
  • ErbB Receptors / genetics
  • Gene Expression Regulation, Neoplastic / drug effects
  • Gene Regulatory Networks / drug effects*
  • Humans
  • Mutation
  • Neoplasm Metastasis
  • Panitumumab
  • Protein Kinase Inhibitors / pharmacology*
  • Protein Kinase Inhibitors / therapeutic use
  • Signal Transduction
  • ras Proteins / genetics

Substances

  • Antibodies, Monoclonal
  • Protein Kinase Inhibitors
  • Panitumumab
  • EGFR protein, human
  • ErbB Receptors
  • ras Proteins
  • Cetuximab