CXCR4 Theranostics: A Potential Game Changer in Solid Tumors and Hematological Malignancies

An overexpression of CXCR4 receptors is reported in at least 30 different human solid tumors and hematological malignancies. This overexpression is often associated with tumor aggressiveness, increased risk of metastasis, and a higher probability of recurrence, which in turn leads to a poor prognosis. No in vivo method suitable for whole-body CXCR4 disease quantification has been described and this unmet clinical need or the scientific question has been reported recently. 68Ga-Pentixafor which is a CXCR4 targeting high-affinity PET imaging probe and the tracer has been evaluated in multiple myeloma, lymphoproliferative disorders, and in lung carcinoma, and the imaging results are extremely promising. Human dosimetry studies demonstrated excellent pharmacokinetics and low radiation burden to patients. The clinical applications of 68Ga-Pentixafor/177Lu/213Bi-Pentixather as a “theranostics pair” for the diagnosis and treatment of CXCR4-expressing cancers are emerging. CXCR4-based theranostics, which had not been investigated in clinical practice till now (except few preliminary proof-of-concept studies), may be a potential game changer both in the diagnosis and treatment of CXCR4 overexpressing solid tumors and hematological malignancies in which all other available treatment options have eventually failed.