Pharmacokinetic and pharmacodynamic study of a clinically effective anti-CD2 monoclonal antibody

Scand J Immunol. 2020 Jan;91(1):e12839. doi: 10.1111/sji.12839. Epub 2019 Nov 10.

Abstract

The humanized IgG1κ monoclonal antibody siplizumab and its rat parent monoclonal IgG2b antibody BTI-322 are directed against the CD2 antigen. Siplizumab is species-specific, reacting with human and chimpanzee cells but not with cells from any other species, including other non-human primates. Because siplizumab treatment has recently shown great potential in clinical transplantation, we now present the results of our previous pharmacokinetic, pharmacodynamic and safety studies of both antibodies. Fourteen chimpanzees received 1-3 doses of 0.143 to 5.0 mg/kg iv The effects were followed with flow cytometry on peripheral lymphocytes and staining of lymph nodes. Side effects were recorded. Serum antibody concentrations were followed. Across the doses, a rapid, transient depletion of CD2, CD3, CD4 and CD8 lymphocytes and NK cells was observed for both antibodies. Immune reconstitution was more rapid for BTI-322 compared to siplizumab. Paracortical lymph node T cell depletion was moderate, estimated at 45% with doses of >0.6 mg/kg. Restoration of lymph node architecture was seen after two weeks to two months for all animals. All four subjects receiving BTI-322 experienced AEs on the first dosing day, while the eight subjects dosed with siplizumab experienced few mild, transient AEs. Infusion with siplizumab and BTI-322 resulted in rapid depletion of CD2+ cells in circulation and tissue. Siplizumab had a longer t1/2 and fewer AEs compared to BTI-322.

Keywords: antibodies/immunoglobulins; experimental animals; molecules; processes; solid organ transplantation; subject; transplantation.

MeSH terms

  • Animals
  • Antibodies, Monoclonal / pharmacokinetics*
  • Antibodies, Monoclonal / therapeutic use
  • Antibodies, Monoclonal, Humanized / pharmacokinetics
  • Antibodies, Monoclonal, Humanized / therapeutic use
  • Biomarkers
  • Biopsy
  • CD2 Antigens / antagonists & inhibitors*
  • Cytokines / blood
  • Female
  • Immunoglobulin G / administration & dosage
  • Immunoglobulin G / pharmacology
  • Immunophenotyping
  • Killer Cells, Natural / immunology
  • Killer Cells, Natural / metabolism
  • Lymphocyte Depletion
  • Lymphocytes / immunology
  • Lymphocytes / metabolism
  • Male
  • Pan troglodytes
  • Rats

Substances

  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Humanized
  • Biomarkers
  • CD2 Antigens
  • Cytokines
  • Immunoglobulin G