ArticleJournal of nuclear medicine : official publication, Society of Nuclear Medicine2013
Assessment of cellular proliferation in tumors by PET using 18F-ISO-1.
Article in Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 42 papers, 1 of them a synthesis that pooled it.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
42 citing papers in PubMed, 1 synthesis or guideline pooled it, 82 citations in OpenAlex.
- Non-conventional and Investigational PET Radiotracers for Breast Cancer: A Systematic Review.Frontiers in medicine · 2022Pooled it
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- Radiation dosimetry and fasting-dependent hepatobiliary clearance of the VAChT-specific PET radioligandEJNMMI research · 2025Article
- Recent Advances in the Development of Sigma Receptor (Radio)Ligands and Their Application in Tumors.ACS pharmacology & translational science · 2025Review
- Ternary Complex Components Responsible for Rapid LDL Internalization as Biomarkers for Breast Cancer Associated with Proliferation and Early Recurrence.Cancer research communications · 2025Article
- Radiopharmaceuticals and their applications in medicine.Signal transduction and targeted therapy · 2025Review
- Exploring Tetrahydroisoquinoline (THIQ) Scaffold as Therapeutic Modulators of Sigma Receptors.Mini reviews in medicinal chemistry · 2025Review
- The Sigma Receptors in Alzheimer's Disease: New Potential Targets for Diagnosis and Therapy.International journal of molecular sciences · 2023Review
- Novel applications of molecular imaging to guide breast cancer therapy.Cancer imaging : the official publication of the International Cancer Imaging Society · 2022Review
- Screening of σJournal of medicinal chemistry · 2022Article
- Discovery and development of brain-penetrantActa pharmaceutica Sinica. B · 2022Article
- Novel Sigma-2 receptor ligand A011 overcomes MDR in adriamycin-resistant human breast cancer cells by modulating ABCB1 and ABCG2 transporter function.Frontiers in pharmacology · 2022Article
- QSAR-Based Computational Approaches to Accelerate the Discovery of Sigma-2 Receptor (S2R) Ligands as Therapeutic Drugs.Molecules (Basel, Switzerland) · 2021Article
- Recent Advances in the Development of Sigma Receptor Ligands as Cytotoxic Agents: A Medicinal Chemistry Perspective.Journal of medicinal chemistry · 2021Review
- Design, Radiosynthesis and Preliminary Biological Evaluation in Mice of a Brain-PenetrantInternational journal of molecular sciences · 2021Article
- Sigma-2 Receptor-A Potential Target for Cancer/Alzheimer's Disease Treatment via Its Regulation of Cholesterol Homeostasis.Molecules (Basel, Switzerland) · 2020Review
- The Biological Function of Sigma-2 Receptor/TMEM97 and Its Utility in PET Imaging Studies in Cancer.Cancers · 2020Review
- Breast CancerJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2020Article
- Approaches to PET Imaging of Glioblastoma.Molecules (Basel, Switzerland) · 2020Review
- Advances in PET Diagnostics for Guiding Targeted Cancer Therapy and Studying In Vivo Cancer Biology.Current pathobiology reports · 2019Article
Corrections and comments
- Erratum issuedWagner-Johnson, Nina [corrected to Wagner-Johnston, Nina]
Authors and funding
12 authors at 3 institutions in 1 country.
Funding
Abstract
unlabelledThis first study in humans was designed to evaluate the safety and dosimetry of a cellular proliferative marker, N-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-2-(2-(18)F-fluoroethoxy)-5-methylbenzamide ((18)F-ISO-1), and evaluate the feasibility of imaging tumor proliferation by PET in patients with newly diagnosed malignant neoplasms.
methodsPatients with biopsy-proven lymphoma, breast cancer, or head and neck cancer underwent (18)F-ISO-1 PET. Tumor (18)F-ISO-1 uptake was assessed semiquantitatively by maximum standardized uptake value, ratios of tumor to normal tissue and tumor to muscle, and relative distribution volume ratio. The PET results were correlated with tumor Ki-67 and mitotic index, from in vitro assays of the tumor tissue. The biodistribution of (18)F-ISO-1 and human dosimetry were evaluated.
resultsThirty patients with primary breast cancer (n = 13), head and neck cancer (n = 10), and lymphoma (n = 7) were evaluated. In the entire group, tumor maximum standardized uptake value and tumor-to-muscle ratio correlated significantly with Ki-67 (τ = 0.27, P = 0.04, and τ = 0.38, P = 0.003, respectively), but no significant correlation was observed between Ki-67 and tumor-to-normal-tissue ratio (τ = 0.07, P = 0.56) or distribution volume ratio (τ = 0.26, P = 0.14). On the basis of whole-body PET data, the gallbladder is the dose-limiting organ, with an average radiation dose of 0.091 mGy/MBq. The whole-body and effective doses were 0.012 mGy/MBq and 0.016 mSv/MBq, respectively. No adverse effects of (18)F-ISO-1 were encountered.
conclusionThe presence of a significant correlation between (18)F-ISO-1 and Ki-67 makes this agent promising for evaluation of the proliferative status of solid tumors. The relatively small absorbed doses to normal organs allow for the safe administration of up to 550 MBq, which is sufficient for PET imaging in clinical trials.
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