ArticleClinical cancer research : an official journal of the American Association for Cancer Research2015
Pharmacodynamic imaging guides dosing of a selective estrogen receptor degrader.
Article in Clinical cancer research : an official journal of the American Association for Cancer Research, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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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
21 citing papers in PubMed, 35 citations in OpenAlex.
- Utility ofEuropean journal of nuclear medicine and molecular imaging · 2017Trial
- HER3 PET Imaging Predicts Response to Pan Receptor Tyrosine Kinase Inhibition Therapy in Gastric Cancer.Molecular imaging and biology · 2023Article
- Hyperpolarized [1-Molecular imaging and biology · 2022Article
- PET Imaging of Estrogen Receptors UsingMethods in molecular biology (Clifton, N.J.) · 2022Article
- The quest for improving the management of breast cancer by functional imaging: The discovery and development of 16α-[Nuclear medicine and biology · 2021Review
- The Predictive Value of Early Changes inThe oncologist · 2020Article
- Review
- Translational strategy using multiple nuclear imaging biomarkers to evaluate target engagement and early therapeutic efficacy of SAR439859, a novel selective estrogen receptor degrader.EJNMMI research · 2020Article
- G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer.Breast cancer research and treatment · 2020Article
- Recent Advances in Imaging Steroid Hormone Receptors in Breast Cancer.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2020Review
- Imaging of Preclinical Endometrial Cancer Models for Monitoring Tumor Progression and Response to Targeted Therapy.Cancers · 2019Review
- Heterogeneity in Metastatic Breast CancerJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2018Article
- Receptor Occupancy Imaging Studies in Oncology Drug Development.The AAPS journal · 2018Review
- Article
- Somatostatin receptor type 2 as a radiotheranostic PET reporter gene for oncologic interventions.Theranostics · 2018Article
- Determination of binding affinity of molecular imaging agents for steroid hormone receptors in breast cancer.American journal of nuclear medicine and molecular imaging · 2018Article
- Clinical cancer research : an official journal of the American Association for Cancer Research · 2017Article
- Estrogen Receptor Binding (18F-FES PET) and Glycolytic Activity (18F-FDG PET) Predict Progression-Free Survival on Endocrine Therapy in Patients with ER+ Breast Cancer.Clinical cancer research : an official journal of the American Association for Cancer Research · 2017Article
- Design, construction and testing of a low-cost automated (68)Gallium-labeling synthesis unit for clinical use.American journal of nuclear medicine and molecular imaging · 2016Article
- Article
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
purposeEstrogen receptor (ER) targeting is key in management of receptor-positive breast cancer. Currently, there are no methods to optimize anti-ER therapy dosing. This study assesses the use of 16α-(18)F-fluoroestradiol ((18)F-FES) PET for fulvestrant dose optimization in a preclinical ER(+) breast cancer model. EXPERIMENTAL
designIn vitro, (18)F-FES retention was compared with ERα protein expression (ELISA) and ESR1 mRNA transcription (qPCR) in MCF7 cells (ER(+)) after treatment with different fulvestrant doses. MCF7 xenografts were grown in ovariectomized nude mice and assigned to vehicle, low- (0.05 mg), medium- (0.5 mg), or high-dose (5 mg) fulvestrant treatment groups (5-7 per group). Two and 3 days after fulvestrant treatment, PET/CT was performed using (18)F-FES and (18)F-FDG, respectively. ER expression was assessed by immunohistochemistry, ELISA, and qPCR on xenografts. Tumor proliferation was assessed using Ki67 immunohistochemistry.
resultsIn vitro, we observed a parallel graded reduction in (18)F-FES uptake and ER expression with increased fulvestrant doses, despite enhancement of ER mRNA transcription. In xenografts, ER expression significantly decreased with increased fulvestrant dose, despite similar mRNA expression and Ki67 staining among the treatment groups. We observed a significant dose-dependent reduction of (18)F-FES PET mean standardized uptake value (SUV(mean)) with fulvestrant treatment but no significant difference among the treatment groups in (18)F-FDG PET SUV(mean).
conclusionsWe demonstrated that (18)F-FES uptake mirrors the dose-dependent changes in functional ER expression with fulvestrant resulting in ER degradation and/or blockade; these precede changes in tumor metabolism and proliferation. Quantitative (18)F-FES PET may be useful for tracking early efficacy of ER blockade/degradation and guiding ER-targeted therapy dosing in patients with breast cancer.
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