2. Academic Validation
  3. CXCR4-targeted theranostics in oncology

CXCR4-targeted theranostics in oncology

  • Eur J Nucl Med Mol Imaging. 2022 Oct;49(12):4133-4144. doi: 10.1007/s00259-022-05849-y.
Andreas K Buck 1,  Sebastian E Serfling 2,  Thomas Lindner 2,  Heribert Hänscheid 2,  Andreas Schirbel 2,  Stefanie Hahner 3,  Martin Fassnacht 3,  Hermann Einsele 4,  Rudolf A Werner 2 5
Affiliations

Affiliations

  • 1 Department of Nuclear Medicine, University Hospital Würzburg, Oberdürrbacher Str. 6, 97080, Wurzburg, Germany. [email protected].
  • 2 Department of Nuclear Medicine, University Hospital Würzburg, Oberdürrbacher Str. 6, 97080, Wurzburg, Germany.
  • 3 Division of Endocrinology and Diabetes, Department of Medicine I, University Hospital, University of Würzburg, Wurzburg, Germany.
  • 4 Department of Internal Medicine II, Hematology and Oncology, University Hospital Würzburg, Wurzburg, Germany.
  • 5 Division of Nuclear Medicine and Molecular Imaging, The Russell H Morgan Department of Radiology and Radiological Sciences, The Johns Hopkins School of Medicine, Baltimore, MD, USA.
PMID: 35674738 DOI: 10.1007/s00259-022-05849-y
Abstract

A growing body of literature reports on the upregulation of C-X-C motif Chemokine Receptor 4 (CXCR4) in a variety of Cancer entities, rendering this receptor as suitable target for molecular imaging and endoradiotherapy in a theranostic setting. For instance, the CXCR4-targeting positron emission tomography (PET) agent [68 Ga]PentixaFor has been proven useful for a comprehensive assessment of the current status quo of solid tumors, including adrenocortical carcinoma or small-cell lung Cancer. In addition, [68 Ga]PentixaFor has also provided an excellent readout for hematological malignancies, such as multiple myeloma, marginal zone lymphoma, or mantle cell lymphoma. PET-based quantification of the CXCR4 capacities in vivo allows for selecting candidates that would be suitable for treatment using the theranostic equivalent [177Lu]/[90Y]PentixaTher. This CXCR4-directed theranostic concept has been used as a conditioning regimen prior to hematopoietic stem cell transplantation and to achieve sufficient anti-lymphoma/-tumor activity in particular for malignant tissues that are highly sensitive to radiation, such as the hematological system. Increasing the safety margin, pretherapeutic dosimetry is routinely performed to determine the optimal activity to enhance therapeutic efficacy and to reduce off-target adverse events. The present review will provide an overview of current applications for CXCR4-directed molecular imaging and will introduce the CXCR4-targeted theranostic concept for advanced hematological malignancies.

Keywords

Adrenocortical carcinoma; C-X-C motif chemokine receptor 4; CXCR4; Endoradiotherapy; Multiple myeloma; Theranostics; [177Lu]PentixaTher; [68Ga]PentixaFor; [90Y]PentixaTher.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-153549
    99.20%, CXCR4 Targeting Peptide