Fc Effector Function Contributes to the Activity of Human Anti-CTLA-4 Antibodies

Cancer Cell. 2018 Apr 9;33(4):649-663.e4. doi: 10.1016/j.ccell.2018.02.010. Epub 2018 Mar 22.

Abstract

With the use of a mouse model expressing human Fc-gamma receptors (FcγRs), we demonstrated that antibodies with isotypes equivalent to ipilimumab and tremelimumab mediate intra-tumoral regulatory T (Treg) cell depletion in vivo, increasing the CD8+ to Treg cell ratio and promoting tumor rejection. Antibodies with improved FcγR binding profiles drove superior anti-tumor responses and survival. In patients with advanced melanoma, response to ipilimumab was associated with the CD16a-V158F high affinity polymorphism. Such activity only appeared relevant in the context of inflamed tumors, explaining the modest response rates observed in the clinical setting. Our data suggest that the activity of anti-CTLA-4 in inflamed tumors may be improved through enhancement of FcγR binding, whereas poorly infiltrated tumors will likely require combination approaches.

Keywords: CTLA-4; Fc-gamma receptors; IgG subclass; antibody-dependent cell-mediated cytotoxicity; immune checkpoints; immune regulatory antibodies; ipilimumab; regulatory T cell depletion; tremelimumab; tumor immunotherapy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antibodies, Monoclonal / administration & dosage
  • Antibodies, Monoclonal / pharmacology
  • Antibodies, Monoclonal, Humanized
  • Antineoplastic Agents, Immunological / administration & dosage*
  • Antineoplastic Agents, Immunological / pharmacology
  • CTLA-4 Antigen / antagonists & inhibitors
  • Cell Line, Tumor
  • Female
  • Humans
  • Ipilimumab / administration & dosage
  • Ipilimumab / pharmacology
  • Melanoma / drug therapy*
  • Melanoma / genetics
  • Melanoma / immunology
  • Mice
  • Polymorphism, Single Nucleotide*
  • Receptors, IgG / genetics*
  • Receptors, IgG / metabolism
  • T-Lymphocytes, Regulatory / immunology*
  • Treatment Outcome
  • Xenograft Model Antitumor Assays

Substances

  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Humanized
  • Antineoplastic Agents, Immunological
  • CTLA-4 Antigen
  • CTLA4 protein, human
  • FCGR3A protein, human
  • Ipilimumab
  • Receptors, IgG
  • tremelimumab