ArticleEJNMMI research2016
Preclinical evaluation of [(68)Ga]NOTA-pentixafor for PET imaging of CXCR4 expression in vivo - a comparison to [(68)Ga]pentixafor.
Article in EJNMMI research, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 26 citations in OpenAlex.
- CXCR4-targeted PET imaging of glioblastoma using [EJNMMI radiopharmacy and chemistry · 2026Article
- The CXCR4-targeted theranostics era: a comprehensive review of a decade of progress (2015-2025).Theranostics · 2026Review
- Radiosynthesis and preclinical evaluation of aEJNMMI radiopharmacy and chemistry · 2024Article
- Development of a New Class of CXCR4-Targeting Radioligands Based on the Endogenous Antagonist EPI-X4 for Oncological Applications.Journal of medicinal chemistry · 2023Article
- Modern Developments in Bifunctional Chelator Design for Gallium Radiopharmaceuticals.Molecules (Basel, Switzerland) · 2022Review
- Synthesis, validation and quality controls of [68Ga]-DOTA-Pentixafor for PET imaging of chemokine receptor CXCR4 expression.Acta bio-medica : Atenei Parmensis · 2020Article
- Assessment of Chemotherapy-Induced Organ Damage with Ga-68 Labeled Duramycin.Molecular imaging and biology · 2020Article
- Noninvasive Classification of Human Triple Negative Breast Cancer by PET Imaging with GRP78-Targeted Molecular Probe [Molecular imaging and biology · 2020Article
- A benzenesulfonamide derivative as a novel PET radioligand for CXCR4.Bioorganic & medicinal chemistry · 2020Article
- Noninvasive PET Imaging of a Ga-68-Radiolabeled RRL-Derived Peptide in Hepatocarcinoma Murine Models.Molecular imaging and biology · 2019Article
- CXCR4-directed theranostics in oncology and inflammation.Annals of nuclear medicine · 2018Review
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4 authors at 2 institutions in 1 country.
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Abstract
backgroundDue to its overexpression in a variety of tumor types, the chemokine receptor 4 (CXCR4) represents a highly relevant diagnostic and therapeutic target in nuclear oncology. Recently, [(68)Ga]pentixafor has emerged as an excellent imaging agent for positron emission tomography (PET) of CXCR4 expression in vivo. In this study, the corresponding [(68)Ga]-1,4,7-triazacyclononane-triacetic acid (NOTA) analog was preclinically evaluated and compared to the 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) parent compound [(68)Ga]pentixafor.
methodsNOTA-pentixafor was synthesized by combining solid and solution-phase peptide synthesis. The CXCR4 receptor affinities of [(68)Ga]pentixafor and [(68)Ga]NOTA-pentixafor were determined in competitive binding assays using the leukemic CXCR4-expressing Jurkat T-cell line and [(125)I]FC131 as the radioligand. Internalization and cell efflux assays were performed using CXCR4-transfected Chem-1 cells. Small-animal PET and biodistribution studies were carried out using Daudi-tumor bearing SCID mice.
results[(68)Ga]NOTA-pentixafor showed a 1.4-fold improved affinity towards CXCR4 (IC50). However, internalization efficiency into CXCR4(+)-Chem-1 cells was substantially decreased compared to [(68)Ga]pentixafor. Accordingly, small-animal PET imaging and biodistribution studies revealed a 9.5-fold decreased uptake of [(68)Ga]NOTA-pentixafor in Daudi lymphoma xenografts (1.7 ± 0.4 % vs 16.2 ± 3.8 % ID/g at 90 min p.i.) and higher levels of non-specific accumulation, primarily in the excretory organs such as the liver, intestines, and kidneys (2.3 ± 0.9 % vs 2.0 ± 0.3 % ID/g, 1.9 ± 0.8 % vs 0.7 ± 0.2 % ID/g, and 2.7 ± 1.1 % vs 1.7 ± 0.9 % ID/g, respectively).
conclusionsDespite enhanced CXCR4-affinity in vitro, the [(68)Ga]NOTA-analog of pentixafor showed reduced CXCR4 targeting efficiency in vivo. In combination with enhanced background accumulation, this resulted in significantly inferior PET imaging contrast, and thus, [(68)Ga]NOTA-pentixafor offers no advantages over [(68)Ga]pentixafor.
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