Problems of Radiation Medicine and Radiobiology

D. O. Dzhuzha

Nonprofit Organization «National Cancer Institute of Ministry of Health of Ukraine»,
33/43 Julia Zdanovska Str., Kyiv, 03022, Ukraine

RADIOPHARMACEUTICALS BASED ON ANTAGONISTS OF CHEMOCINE RECEPTOR CXCR4 IN DIAGNOSTICS AND TREATMENT OF ONCOLOGICAL DISEASES

The review is devoted to the use of a new class of radiopharmaceuticals (RPs) – chemokine receptor ligands – in oncological practice. The chemokine receptor CXCR4 is of particular interest as a molecular target in the diagnosis and treatment of malignant tumors, as it plays an important role in carcinogenesis. By interacting with the chemokine CCXL12, it activates cell signaling pathways that affect tumor cell proliferation, angiogenesis, metastasis growth, and apoptosis inhibition. The CXCR4 receptor is overexpressed on the cell surfaces of many hematological malignancies and solid tumors; the expression is correlated with poor prognosis. Numerous inhibitors of the CXCR4/CXCL12 axis and their radionuclide-labeled analogues have been developed, which allow visualization of CXCR4 and radioligand therapy. The possibilities of using RP ⁶⁸Ga-Pentixafor for the diagnosis of hemoblastosis and solid tumors are shown. The therapeutic RP ¹⁷⁷Lu/⁹⁰Y-Pentixather was tested in the complex treatment of spread hemoblastoses and showed the direct antitumor activity and the desired myeloablative effect. Taking into account the results already obtained and the importance of new therapeutic approaches, especially in the field of refractory spread malignancies, it is obvious that these studies will be further developed.
Key words: chemokine receptor CXCR4; ⁶⁸Ga-Pentixafor; ¹⁷⁷Lu/⁹⁰Y-Pentixather; CXCR4-directed radionuclide diagnostics; radioligand therapy of hematological malignances.

Problems of Radiation Medicine and Radiobiology.
2024;29:19-33. doi: 10.33145/2304-8336-2024-29-19-33

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