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Wester, H.J.* ; Keller, U.* ; Schottelius, M.* ; Beer, A.* ; Philipp-Abbrederis, K.* ; Hoffmann, F.* ; Simecek, J.* ; Gerngross, C.* ; Lassmann, M.* ; Herrmann, K.* ; Pellegata, N.S. ; Rudelius, M.* ; Kessler, H.* ; Schwaiger, M.*

Disclosing the CXCR4 expression in lymphoproliferative diseases by targeted molecular imaging.

Theranostics 5, 618-630 (2015)

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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.

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