Potent antitumour activity of interleukin-2-Fc fusion proteins requires Fc-mediated depletion of regulatory T-cells

Nat Commun. 2017 May 12:8:15373. doi: 10.1038/ncomms15373.

Abstract

Interleukin-2 (IL-2) is an established therapeutic agent used for cancer immunotherapy. Since treatment efficacy is mediated by CD8+ and NK cell activity at the tumour site, considerable efforts have focused on generating variants that expand these subsets systemically, as exemplified by IL-2/antibody complexes and 'superkines'. Here we describe a novel determinant of antitumour activity using fusion proteins consisting of IL-2 and the antibody fragment crystallizable (Fc) region. Generation of long-lived IL-2-Fc variants in which CD25 binding is abolished through mutation effectively prevents unwanted activation of CD25+ regulatory T-cells (Tregs) and results in strong expansion of CD25- cytotoxic subsets. Surprisingly, however, such variants are less effective than wild-type IL-2-Fc in mediating tumour rejection. Instead, we report that efficacy is crucially dependent on depletion of Tregs through Fc-mediated immune effector functions. Our results underpin an unexpected mechanism of action and provide important guidance for the development of next generation IL-2 therapeutics.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antibodies, Monoclonal / immunology
  • Antineoplastic Agents / pharmacology*
  • CD8-Positive T-Lymphocytes / immunology
  • Cytokines / metabolism
  • Female
  • Immunoglobulin Fragments / immunology*
  • Immunoglobulin G / immunology
  • Immunologic Memory
  • Immunotherapy*
  • Interleukin-2 / pharmacology
  • Interleukin-2 Receptor alpha Subunit / metabolism
  • Killer Cells, Natural / immunology
  • Leukocytes, Mononuclear / cytology
  • Lymphocyte Activation*
  • Lymphocyte Subsets / immunology
  • Melanoma, Experimental
  • Mice
  • Mice, Inbred BALB C
  • Mice, Inbred C57BL
  • Mutagenesis
  • Neoplasms / immunology*
  • Neoplasms / therapy
  • Recombinant Proteins / metabolism
  • Spleen / cytology
  • Spleen / metabolism
  • T-Lymphocytes, Regulatory / immunology*

Substances

  • Antibodies, Monoclonal
  • Antineoplastic Agents
  • Cytokines
  • IL2RA protein, human
  • Immunoglobulin Fragments
  • Immunoglobulin G
  • Interleukin-2
  • Interleukin-2 Receptor alpha Subunit
  • Recombinant Proteins