1. Pharmaceutical Radiochemistry, Technische Universität München, Garching, Germany
2. III. Medical Department, Technische Universität München, Munich, Germany
3. Department of Nuclear Medicine, Technische Universität München, Munich, Germany
4. Department of Nuclear Medicine, University Hospital Würzburg, Würzburg, Germany
5. Institute of Pathology, Helmholtz Zentrum München, Munich, Germany
6. Institute of Pathology, Universität Würzburg, Comprehensive Cancer Center Mainfranken, Würzburg, Germany
7. Institute for Advanced Study, Department of Chemistry, Technische Universität München, Garching, Germany
8. Chemistry Department, Faculty of Science, King Abdulaziz University, Jeddah, Saudi Arabia
# Current address: Ulm University, Department of Nuclear Medicine; Ulm, Germany.
* Current address: Scintomics GmbH, Fuerstenfeldbruck, Germany.
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.
Keywords: CXCR4, chemokine receptor, positron emission tomography, lymphoma, in vivo imaging