CD206+ macrophages are relevant non-invasive imaging biomarkers and therapeutic targets in experimental lung fibrosis

Thorax. 2024 Nov 14;79(12):1124-1135. doi: 10.1136/thorax-2023-221168.

Abstract

Background: Interstitial lung diseases (ILDs) include a large number of diseases associated with progressive pulmonary fibrosis (PPF), including idiopathic pulmonary fibrosis (IPF). Despite the rarity of each of the fibrotic ILDs individually, they cumulatively affect a considerable number of patients. PPF is characterised by an excessive collagen deposition leading to functional decline.

Objectives: Therapeutic options are limited to nintedanib and pirfenidone which are only able to reduce fibrosis progression. CD206-expressing M2 macrophages are involved in fibrosis progression, and whether they may be relevant therapeutic targets or biomarkers remains an open question.

Results: In our study, CD206+ lung macrophages were monitored in bleomycin-induced lung fibrosis in mice by combining flow cytometry, scRNAseq and in vivo molecular imaging using a single photon emission computed tomography (SPECT) radiopharmaceutical, 99mTc-tilmanocept. The antifibrotic effect of the inhibition of M2 macrophage polarisation with a JAK inhibitor, tofacitinib, was assessed in vivo. We demonstrate that CD206-targeted in vivo SPECT imaging with 99mTc-tilmanocept was able to accurately detect and quantify the increase in CD206+ macrophages from early to advanced stages of experimental fibrosis and ex vivo in lung biopsies from patients with IPF. CD206-targeted imaging also specifically detected a decrease in CD206+ lung macrophages on nintedanib and tofacitinib treatment. Importantly, early in vivo imaging of CD206+ macrophages allowed the prediction of experimental lung fibrosis progression as well as nintedanib and tofacitinib efficacy.

Conclusions: These findings indicate that M2 macrophages may be relevant theranostic targets for personalised medicine for patients with PPF.

Keywords: Idiopathic pulmonary fibrosis; Imaging/CT MRI etc; Interstitial Fibrosis; Macrophage Biology.

MeSH terms

  • Animals
  • Biomarkers* / metabolism
  • Bleomycin
  • Disease Models, Animal
  • Flow Cytometry
  • Humans
  • Indoles
  • Macrophages / drug effects
  • Macrophages / metabolism
  • Mannose Receptor*
  • Mannose-Binding Lectins / metabolism
  • Mice
  • Mice, Inbred C57BL
  • Piperidines* / pharmacology
  • Piperidines* / therapeutic use
  • Pulmonary Fibrosis / diagnostic imaging
  • Pulmonary Fibrosis / drug therapy
  • Pyrimidines* / pharmacology
  • Pyrimidines* / therapeutic use
  • Pyrroles* / pharmacology
  • Pyrroles* / therapeutic use
  • Radiopharmaceuticals
  • Receptors, Cell Surface / metabolism
  • Tomography, Emission-Computed, Single-Photon* / methods

Substances

  • Piperidines
  • Biomarkers
  • Pyrimidines
  • Pyrroles
  • Mannose Receptor
  • tofacitinib
  • Receptors, Cell Surface
  • Bleomycin
  • Mannose-Binding Lectins
  • Radiopharmaceuticals
  • nintedanib
  • Indoles