Current Status and Future Perspectives of CXCR4-based Radio-theranostics in Human Cancers

Among the class of chemokine receptors, the G-protein coupled CXCR4 receptors are overexpressed in more than 30 human cancers. These receptors have been recognized as potential disease targets both for imaging and therapy. CXCR4 receptors are associated with tumor aggressiveness, increased risk of metastasis, and a higher probability of recurrence, which in turn leads to a poor prognosis. Ga-68 Pentixafor PET/CT has been reported to have a high affinity for CXCR4 receptors and offers efficient in vivo imaging suitable for the whole body CXCR4 disease mapping. Ga-68 Pentixafor, as a high throughput PET probe targeting CXCR4 receptors, has provided important diagnostic and prognostic information in human cancers. This PET radioligand provides favorable radiolabelling efficiency, stability, and safety profiling data. This review article discusses the Ga-68 Pentixafor PET/CT and Lu-177/Y-90 Pentixather as “theranostics pair” and their potential applications in hematological and solid cancers.