Disclosing the CXCR4 expression in lymphoproliferative diseases by targeted molecular imaging

Theranostics. 2015 Mar 1;5(6):618-30. doi: 10.7150/thno.11251. eCollection 2015.


Chemokine ligand-receptor interactions play a pivotal role in cell attraction and cellular trafficking, both in normal tissue homeostasis and in disease. In cancer, chemokine receptor-4 (CXCR4) expression is an adverse prognostic factor. Early clinical studies suggest that targeting CXCR4 with suitable high-affinity antagonists might be a novel means for therapy. In addition to the preclinical evaluation of [(68)Ga]Pentixafor in mice bearing human lymphoma xenografts as an exemplary CXCR4-expressing tumor entity, we report on the first clinical applications of [(68)Ga]Pentixafor-Positron Emission Tomography as a powerful method for CXCR4 imaging in cancer patients. [(68)Ga]Pentixafor binds with high affinity and selectivity to human CXCR4 and exhibits a favorable dosimetry. [(68)Ga]Pentixafor-PET provides images with excellent specificity and contrast. This non-invasive imaging technology for quantitative assessment of CXCR4 expression allows to further elucidate the role of CXCR4/CXCL12 ligand interaction in the pathogenesis and treatment of cancer, cardiovascular diseases and autoimmune and inflammatory disorders.

Keywords: CXCR4; chemokine receptor; lymphoma, in vivo imaging; positron emission tomography.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Coordination Complexes / chemical synthesis
  • Coordination Complexes / pharmacokinetics*
  • Coordination Complexes / pharmacology
  • Female
  • Humans
  • Jurkat Cells
  • Lymphoma, Large B-Cell, Diffuse / diagnostic imaging*
  • Male
  • Mice
  • Mice, SCID
  • Peptides, Cyclic / chemical synthesis
  • Peptides, Cyclic / pharmacokinetics*
  • Peptides, Cyclic / pharmacology
  • Positron-Emission Tomography*
  • Protein Binding
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / pharmacokinetics*
  • Radiopharmaceuticals / pharmacology
  • Receptors, CXCR4 / antagonists & inhibitors
  • Receptors, CXCR4 / metabolism*
  • Tissue Distribution


  • 68Ga-pentixafor
  • Coordination Complexes
  • Peptides, Cyclic
  • Radiopharmaceuticals
  • Receptors, CXCR4