Hans Jürgen Wester, Ulrich Keller, Margret Schottelius, Ambros Beer, Kathrin Philipp-Abbrederis, Frauke Hoffmann, Jakub Šimeček, Carlos Gerngross, Michael Lassmann, Ken Herrmann, Natalia Pellegata, Martina Rudelius, Horst Kessler, Markus Schwaiger. (06-03-2015).

Theranostics 2015; 5(6):618-630, 2015, doi:10.7150/thno.11251

Department: 

Research Area C

Abstract: 

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 [68Ga]Pentixafor in mice bearing human lymphoma xenografts as an exemplary CXCR4-expressing tumor entity, we report on the first clinical applications of [68Ga]Pentixafor-Positron Emission Tomography as a powerful method for CXCR4 imaging in cancer patients. [68Ga]Pentixafor binds with high affinity and selectivity to human CXCR4 and exhibits a favorable dosimetry. [68Ga]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.