Comprehensive pharmacogenetic profiling of the epidermal growth factor receptor pathway for biomarkers of response to, and toxicity from, cetuximab

J Med Genet. 2017 Aug;54(8):567-571. doi: 10.1136/jmedgenet-2016-104317. Epub 2017 Mar 10.

Abstract

Background: Somatic mutations in the epidermal growth factor receptor (EGFR) intracellular signalling pathways predict non-response to cetuximab in the treatment of advanced colorectal cancer (aCRC). We hypothesised that common germline variants within these pathways may also play similar roles.

Methods: We analysed 54 potentially functional, common, inherited EGFR pathway variants in 815 patients with aCRC treated with oxaliplatin-fluoropyrimidine chemotherapy plus cetuximab. Primary endpoints were response and skin rash (SR). We had >85% power to detect ORs=1.6 for variants with minor allele frequencies >20%.

Results: We identified five potential biomarkers for response and four for SR, although none remained significant after correction for multiple testing. Our initial data supported a role for Ser313Pro in PIK3R2 in modulating response to cetuximab-in patients with KRAS wild-type CRCs, 36.4% with one allele encoding proline responded, as compared with 71.2% homozygous for allele encoding serine (OR 0.23, 95% CI 0.09 to 0.56, p=0.0014), and this association was predictive for cetuximab (pinteraction=0.017); however, independent replication failed to validate this association. No previously proposed predictive biomarkers were validated.

Conclusions: Our study highlights the need to validate potential pharmacogenetic biomarkers. We did not find strong evidence for common germline biomarkers of cetuximab response and toxicity.

Keywords: Pharmacogenetics; biomarkers.; cetuximab; colorectal cancer.

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Antineoplastic Agents / therapeutic use
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use
  • Biomarkers, Pharmacological
  • Cetuximab / therapeutic use*
  • Colorectal Neoplasms / drug therapy*
  • Colorectal Neoplasms / genetics*
  • ErbB Receptors / genetics*
  • Female
  • Gene Frequency
  • Germ-Line Mutation
  • Humans
  • Male
  • Middle Aged
  • Organoplatinum Compounds / therapeutic use*
  • Oxaliplatin
  • Pharmacogenomic Variants / genetics
  • Signal Transduction / genetics

Substances

  • Antineoplastic Agents
  • Biomarkers, Pharmacological
  • Organoplatinum Compounds
  • Oxaliplatin
  • EGFR protein, human
  • ErbB Receptors
  • Cetuximab