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

Area of Science:

• Oncology
• Nuclear Medicine
• Molecular Imaging

Background:

• The chemokine receptor CXCR4 plays a critical role in cancer development, including tumor proliferation, angiogenesis, metastasis, and apoptosis.
• CXCR4 is overexpressed in various hematological malignancies and solid tumors, often correlating with a poor prognosis.
• Targeting the CXCR4/CXCL12 axis presents a promising strategy for cancer diagnosis and therapy.

Purpose of the Study:

• To review the application of chemokine receptor ligands as novel radiopharmaceuticals in oncology.
• To highlight the diagnostic and therapeutic potential of CXCR4-targeting agents.

Main Methods:

• Development of radionuclide-labeled chemokine receptor ligands (e.g., Pentixafor, Pentixather).
• Utilizing positron emission tomography (PET) imaging with 68Ga-Pentixafor for tumor visualization.
• Investigating therapeutic efficacy of 177Lu/90Y-Pentixather in radioligand therapy.

Main Results:

• 68Ga-Pentixafor enables visualization of CXCR4 expression in hemoblastosis and solid tumors.
• 177Lu/90Y-Pentixather demonstrated direct antitumor activity and a myeloablative effect in treating advanced hemoblastoses.
• These agents facilitate both diagnosis and targeted therapy for CXCR4-expressing cancers.

Conclusions:

• Chemokine receptor ligands, particularly CXCR4-targeting radiopharmaceuticals, represent a significant advancement in oncological practice.
• These agents offer a dual capability for diagnosis and therapy, especially for refractory and advanced malignancies.
• Further development of CXCR4-targeted radiopharmaceuticals is warranted for improved cancer management.