Repurposing of Cetuximab in antibody-directed chemotherapy-loaded nanoparticles in EGFR therapy-resistant pancreatic tumours

Nanoscale. 2019 Nov 14;11(42):20261-20273. doi: 10.1039/c9nr07257h. Epub 2019 Oct 18.

Abstract

The anti-Epidermal Growth Factor Receptor (EGFR) antibody Cetuximab (CTX) has demonstrated limited anti-cancer efficacy in cells overexpressing EGFR due to activating mutations in RAS in solid tumours, such as pancreatic cancer. The utilisation of antibodies as targeting components of antibody-drug conjugates, such as trastuzumab emtansine (Kadcyla), demonstrates that antibodies may be repurposed to direct therapeutic agents to antibody-resistant cancers. Here we investigated the use of CTX as a targeting agent for camptothecin (CPT)-loaded polymeric nanoparticles (NPs) directed against KRAS mutant CTX-resistant cancer cells. CPT was encapsulated within poly(lactic-co-glycolic acid) (PLGA) NPs using the solvent evaporation method. CTX conjugation improved NP binding and delivery of CPT to CTX-resistant cancer cell lines. CTX successfully targeted CPT-loaded NPs to mutant KRAS PANC-1 tumours in vivo and reduced tumour growth. This study highlights that CTX can be repurposed as a targeting agent against CTX-resistant cancers and that antibody repositioning may be applicable to other antibodies restricted by resistance.

MeSH terms

  • Ado-Trastuzumab Emtansine* / chemistry
  • Ado-Trastuzumab Emtansine* / pharmacology
  • Animals
  • Cetuximab* / chemistry
  • Cetuximab* / pharmacology
  • Drug Resistance, Neoplasm / drug effects*
  • ErbB Receptors / metabolism
  • Female
  • HCT116 Cells
  • Humans
  • Immunoconjugates* / chemistry
  • Immunoconjugates* / pharmacology
  • Mice
  • Mice, SCID
  • Nanoparticles* / chemistry
  • Nanoparticles* / therapeutic use
  • Neoplasm Proteins / metabolism*
  • Pancreatic Neoplasms / drug therapy
  • Pancreatic Neoplasms / metabolism
  • Pancreatic Neoplasms / pathology
  • Xenograft Model Antitumor Assays

Substances

  • Immunoconjugates
  • Neoplasm Proteins
  • EGFR protein, human
  • ErbB Receptors
  • Cetuximab
  • Ado-Trastuzumab Emtansine