Title:Nuclear Medicine Application of Pentixafor/Pentixather Targeting CXCR4
for Imaging and Therapy in Related Disease
Volume: 23
Issue: 7
Author(s): Zhenying Chen, Qianqian Xue and Shaobo Yao*
Affiliation:
- Department of Nuclear Medicine, The First Affiliated Hospital of Fujian Medical University, Fuzhou, 35005, Fujian,
P.R. China
Keywords:
CXCR4, CXCL12, pentixafor, pentixather, PET, endoradiotherapy.
Abstract:
C-X-C-motif chemokine receptor 4 (CXCR4) is a novel predictive biomarker for metastasis
and poor prognosis in individuals with malignancies. CXCL12 is the only cognate ligand of CXCR4.
CXCL12/CXCR4 signaling pathways are involved in the cross-talk among cancer cells, T cells, stromal
cells, and their microenvironments, including the regulation and direction of T cell migration
(chemotaxis), proliferation, and differentiation of immature progenitor stem cells. As CXCR4 overexpression
is related to tumor prognosis, it is essential to quantitatively evaluate CXCR4 expression
levels in vivo.
68Ga-Pentixafor, as a radiolabeled tracer, shows high specificity and affinity for CXCR4 in tumors.
Thus, CXCR4-directed imaging with 68Ga-Pentixafor has been investigated to evaluate CXCR4 expression
in patients non-invasively. In recent years, many small cohorts, including those of individuals
with hematologic malignancies, solid tumors, and cardiovascular and infectious diseases, have been
reported. So far, 68Ga-Pentixafor has been used successfully in individuals with hematologic malignancies.
In addition, Lutetium-177 (177Lu) or Yttrium-90 (90Y)-labeled Pentixather (an analog of
Pentixafor) suggested high potential applicability in tumor endoradiotherapy (ERT) with CXCR4
overexpression. Patients with advanced-stage multiple myeloma, refractory acute leukemia, and diffuse
large B-cell lymphoma received a certain amount of 177Lu-Pentixather or 90Y-Pentixather. This
review aimed to overview the current CXCR4-directed positron emission computed tomography
(PET) molecular imaging based on Pentixafor in several diseases and ERT.