Targeted delivery of interleukin-10 to chronic cardiac allograft rejection using a human antibody specific to the extra domain A of fibronectin

Int J Cardiol. 2015 Sep 15:195:311-22. doi: 10.1016/j.ijcard.2015.05.144. Epub 2015 May 29.

Abstract

Background and aims: Management of chronic rejection is challenging since there are not sufficient preventive or therapeutic strategies. The rejection process leads to overexpression of ED-A(+) fibronectin (ED-A(+) Fn). The human antibody F8, specific to ED-A(+) Fn, may serve as a vehicle for targeted delivery of bioactive payloads, e.g. interleukin 10 (IL-10). The aim of this study was to investigate the therapeutic effects of the fusion protein F8-interleukin-10 (F8-IL10) in the process of chronic rejection development.

Methods: A heterotopic rat heart transplantation model was used to induce chronic rejection. For therapeutic interventions, the immunocytokines F8-humanIL10 (DEKAVIL), F8-ratIL10 as well as KSF-humanIL10 (irrelevant antigen-specificity) were used. Treatment was performed weekly for 10 weeks starting at day 7 after transplantation (1mg/animal).

Results: In the cardiac allografts, treatment with F8-huIL10 or F8-ratIL10 was associated with increased heart weights, a higher grade of chronic rejection, increased CIF, higher protein expression levels of alpha-smooth muscle actin (α-SMA), an augmented infiltration with inflammatory cells (CD4+, CD8+ and CD68+ cells) and higher serum levels of brain natriuretic peptide (BNP) compared to the control groups.

Conclusions: All observed treatment effects are transplantation-specific since the F8 antibody is specific to ED-A(+) Fn that is not expressed in healthy hearts. A clear targeting effect of F8-huIL10 as well as F8-ratIL10 could be proven. Against that background, a further study is needed to address the question, if F8-IL10 treatment is capable to reduce CAV and CIF starting at a time point when chronic rejection has fully developed (therapeutic approach).

Keywords: Antibody; Cardiac allograft rejection; Cardiac allograft vasculopathy; Cardiac remodelling; ED-A domain containing fibronectin; Interleukin-10; Interstitial fibrosis; Targeted therapy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antibodies, Monoclonal* / immunology
  • Antibodies, Monoclonal* / pharmacology
  • Antibodies, Monoclonal, Humanized
  • Chronic Disease
  • Disease Models, Animal
  • Drug Monitoring / methods
  • Fibronectins / immunology
  • Fluorescent Antibody Technique
  • Graft Rejection* / drug therapy
  • Graft Rejection* / immunology
  • Graft Rejection* / pathology
  • Humans
  • Interleukin-10 / immunology*
  • Models, Cardiovascular
  • Molecular Targeted Therapy
  • Rats
  • Recombinant Fusion Proteins* / immunology
  • Recombinant Fusion Proteins* / pharmacology
  • Treatment Outcome

Substances

  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Humanized
  • F8 monoclonal antibody
  • Fibronectins
  • IL10 protein, human
  • Recombinant Fusion Proteins
  • Interleukin-10