CXCR4-targeted theranostics in oncology.

Area of Science:

• Oncology
• Nuclear Medicine
• Radiotherapy

Background:

• C-X-C motif chemokine receptor 4 (CXCR4) is frequently overexpressed across diverse cancer types.
• This overexpression makes CXCR4 a promising target for molecular imaging and targeted cancer therapies.

Purpose of the Study:

• To review current applications of CXCR4-directed molecular imaging.
• To introduce the CXCR4-targeted theranostic concept for advanced hematological malignancies.

Main Methods:

• Utilizing positron emission tomography (PET) with agents like [68Ga]PentixaFor for CXCR4 imaging.
• Applying theranostic agents such as [177Lu]/[90Y]PentixaTher for targeted radiotherapy.
• Performing pretherapeutic dosimetry to optimize treatment activity and minimize adverse events.

Main Results:

• [68Ga]PentixaFor PET is effective for assessing solid tumors (e.g., adrenocortical carcinoma, small-cell lung cancer) and hematological malignancies (e.g., multiple myeloma, lymphomas).
• PET-based quantification of CXCR4 aids in selecting patients for theranostic treatment with [177Lu]/[90Y]PentixaTher.
• The CXCR4-directed theranostic approach has shown efficacy as a conditioning regimen for stem cell transplantation and in treating radiation-sensitive hematological cancers.

Conclusions:

• CXCR4-targeted molecular imaging and theranostics offer a promising approach for managing various cancers.
• This theranostic strategy is particularly valuable for advanced hematological malignancies, enhancing treatment efficacy and safety.
• Pretherapeutic dosimetry is crucial for optimizing CXCR4-targeted radiopharmaceutical therapy.