Antitumor activity of an anti-CD98 antibody

Int J Cancer. 2015 Aug 1;137(3):710-20. doi: 10.1002/ijc.29415. Epub 2015 Jan 14.

Abstract

CD98 is expressed on several tissue types and specifically upregulated on fast-cycling cells undergoing clonal expansion. Various solid (e.g., nonsmall cell lung carcinoma) as well as hematological malignancies (e.g., acute myeloid leukemia) overexpress CD98. We have identified a CD98-specific mouse monoclonal antibody that exhibits potent preclinical antitumor activity against established lymphoma tumor xenografts. Additionally, the humanized antibody designated IGN523 demonstrated robust tumor growth inhibition in leukemic cell-line derived xenograft models and was as efficacious as standard of care carboplatin in patient-derived nonsmall lung cancer xenografts. In vitro studies revealed that IGN523 elicited strong ADCC activity, induced lysosomal membrane permeabilization and inhibited essential amino acid transport function, ultimately resulting in caspase-3 and -7-mediated apoptosis of tumor cells. IGN523 is currently being evaluated in a Phase I clinical trial for acute myeloid leukemia (NCT02040506). Furthermore, preclinical data support the therapeutic potential of IGN523 in solid tumors.

Keywords: acute myeloid leukemia; anti-CD98 monoclonal antibody; multiple mechanism of action; non-small cell lung cancer; phenotypic screening.

MeSH terms

  • Amino Acids / metabolism
  • Animals
  • Antibodies, Monoclonal / administration & dosage
  • Antibodies, Monoclonal / immunology
  • Antibodies, Monoclonal / pharmacology*
  • Antibodies, Monoclonal, Humanized / administration & dosage
  • Antibodies, Monoclonal, Humanized / immunology
  • Antibodies, Monoclonal, Humanized / pharmacology
  • Antibody-Dependent Cell Cytotoxicity / immunology
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / pharmacology*
  • Biological Transport
  • Caspases / metabolism
  • Cell Line, Tumor
  • Cell Membrane Permeability
  • Complement System Proteins / immunology
  • Cytotoxicity, Immunologic
  • Disease Models, Animal
  • Drug Evaluation, Preclinical
  • Female
  • Fusion Regulatory Protein-1 / antagonists & inhibitors*
  • Humans
  • Lysosomes / metabolism
  • Mice
  • Models, Biological
  • Protein Binding
  • Tumor Burden / drug effects
  • Xenograft Model Antitumor Assays

Substances

  • Amino Acids
  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Humanized
  • Antineoplastic Agents
  • Fusion Regulatory Protein-1
  • Complement System Proteins
  • Caspases