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Mol Imaging Biol. 2012 Feb;14(1):106-14. doi: 10.1007/s11307-010-0466-y.

Positron emission tomography imaging of tumors expressing the human chemokine receptor CXCR4 in mice with the use of 64Cu-AMD3100.

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  • 1Laboratory of Molecular Immunology, National Institute of Allergy and Infectious Diseases, 10 Center Drive, Room 11N111, Bethesda, MD 20892, USA.

Abstract

PURPOSE:

Expression of CXCR4 in cancers has been correlated with poor prognosis and increased metastasis. Quantifying CXCR4 expression non-invasively might aid in prognostication and monitoring therapy. We evaluated a radiolabeled antagonist of CXCR4, ⁶⁴Cu-AMD3100, as a positron-emitting imaging agent.

PROCEDURES:

CXCR4-transfected or non-transfected cell lines were injected into mice to form xenografts. Accumulation of ⁶⁴Cu-AMD3100 in tumors was analyzed by small-animal PET and biodistribution assays.

RESULTS:

⁶⁴Cu-AMD3100 accumulated in CXCR4-expressing, but not CXCR4-negative, tumors. For CXCR4-expressing tumors, tumor-to-blood and tumor-to-muscle ratios were 23-41 and 50-59, respectively, depending on tumor type. Excess of unlabeled Cu-AMD3100 or AMD3100 significantly reduced ⁶⁴Cu-AMD3100 accumulation in CXCR4-expressing tumors. Human-absorbed dose calculations predicted a dose limit of 444 MBq.

CONCLUSIONS:

CXCR4 can be imaged in tumors using ⁶⁴Cu-AMD3100. Dosimetry studies suggest that imaging in humans is feasible. We conclude that ⁶⁴Cu-AMD3100 should be investigated as a potential agent for imaging and quantifying CXCR4 in tumors.

PMID:
21347799
[PubMed - indexed for MEDLINE]
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