Literature DB >> 28798032

Improved Estrogen Receptor Assessment by PET Using the Novel Radiotracer 18F-4FMFES in Estrogen Receptor-Positive Breast Cancer Patients: An Ongoing Phase II Clinical Trial.

Michel Paquette1, Éric Lavallée1, Serge Phoenix1, René Ouellet1, Helena Senta1, Johan E van Lier1, Brigitte Guérin1, Roger Lecomte1, Éric E Turcotte2.   

Abstract

After encouraging preclinical and human dosimetry results for the novel estrogen receptor (ER) PET radiotracer 4-fluoro-11β-methoxy-16α-18F-fluoroestradiol (18F-4FMFES), a phase II clinical trial was initiated to compare the PET imaging diagnostic potential of 18F-4FMFES with that of 16α-18F-fluoroestradiol (18F-FES) in ER-positive (ER+) breast cancer patients.
Methods: Patients diagnosed with ER+ breast cancer (n = 31) were recruited for this study, including 6 who underwent mastectomy or axillary node dissection. For each patient, 18F-FES and 18F-4FMFES PET/CT scans were done sequentially (within a week) and in random order. One hour after injection of either radiotracer, a head-to-thigh static scan with a 2-min acquisition per bed position was obtained. Blood samples were taken at different times after injection to assess each tracer metabolism by reverse-phase thin-layer chromatography. The SUVmean of nonspecific tissues and the SUVmax of the tumor were evaluated for each detected lesion, and tumor-to-nonspecific organ ratios were calculated.
Results: Blood metabolite analysis 60 min after injection of the tracer showed a 2.5-fold increase in metabolic stability of 18F-4FMFES over 18F-FES. Although for most foci 18F-4FMFES PET had an SUVmax similar to that of 18F-FES PET, tumor contrast improved substantially in all cases. Lower uptake was consistently observed in nonspecific tissues for 18F-4FMFES, notably a 4-fold decrease in blood-pool activity as compared with 18F-FES. Consequently, image quality was considerably improved using 18F-4FMFES, with lower overall background activity. As a result, 18F-4FMFES successfully identified 9 more lesions than 18F-FES.
Conclusion: This phase II study with ER+ breast cancer patients showed that 18F-4FMFES PET achieves a lower nonspecific signal and better tumor contrast than 18F-FES PET, resulting in improved diagnostic confidence and lower false-negative diagnoses.
© 2018 by the Society of Nuclear Medicine and Molecular Imaging.

Entities:  

Keywords:  18F-4FMFES; 18F-FES; ER+; breast cancer; receptor PET imaging

Mesh:

Substances:

Year:  2017        PMID: 28798032      PMCID: PMC6910621          DOI: 10.2967/jnumed.117.194654

Source DB:  PubMed          Journal:  J Nucl Med        ISSN: 0161-5505            Impact factor:   10.057


  38 in total

1.  Factors influencing the uptake of 18F-fluoroestradiol in patients with estrogen receptor positive breast cancer.

Authors:  Lanell M Peterson; Brenda F Kurland; Jeanne M Link; Erin K Schubert; Svetlana Stekhova; Hannah M Linden; David A Mankoff
Journal:  Nucl Med Biol       Date:  2011-05-05       Impact factor: 2.408

2.  The 2010 Philip S. Portoghese Medicinal Chemistry Lectureship: addressing the "core issue" in the design of estrogen receptor ligands.

Authors:  John A Katzenellenbogen
Journal:  J Med Chem       Date:  2011-07-11       Impact factor: 7.446

3.  11 beta-methoxy-, 11 beta-ethyl- and 17 alpha-ethynyl-substituted 16 alpha-fluoroestradiols: receptor-based imaging agents with enhanced uptake efficiency and selectivity.

Authors:  M G Pomper; H VanBrocklin; A M Thieme; R D Thomas; D O Kiesewetter; K E Carlson; C J Mathias; M J Welch; J A Katzenellenbogen
Journal:  J Med Chem       Date:  1990-12       Impact factor: 7.446

4.  Breast cancer: PET imaging of estrogen receptors.

Authors:  M A Mintun; M J Welch; B A Siegel; C J Mathias; J W Brodack; A H McGuire; J A Katzenellenbogen
Journal:  Radiology       Date:  1988-10       Impact factor: 11.105

5.  Loss of estrogen receptor in recurrent breast cancer is associated with poor response to endocrine therapy.

Authors:  T Kuukasjärvi; J Kononen; H Helin; K Holli; J Isola
Journal:  J Clin Oncol       Date:  1996-09       Impact factor: 44.544

6.  2- and 4-fluorinated 16 alpha(-)[125I]iodoestradiol derivatives: synthesis and effect on estrogen receptor binding and receptor-mediated target tissue uptake.

Authors:  H Ali; J Rousseau; T G Gantchev; J E van Lier
Journal:  J Med Chem       Date:  1993-12-24       Impact factor: 7.446

7.  Automated synthesis of 11beta-methoxy-4,16alpha-[16alpha-(18)F]difluoroestradiol (4F-M[(18)F]FES) for estrogen receptor imaging by positron emission tomography.

Authors:  Naseem Ahmed; Rejean Langlois; Serge Rodrigue; François Bénard; Johan E van Lier
Journal:  Nucl Med Biol       Date:  2007-05       Impact factor: 2.408

8.  Synthesis of A-ring fluorinated derivatives of (17 alpha,20E/Z)-[125I]iodovinylestradiols: effect on receptor binding and receptor-mediated target tissue uptake.

Authors:  H Ali; J Rousseau; J E van Lier
Journal:  J Med Chem       Date:  1993-10-15       Impact factor: 7.446

9.  Feasibility and predictability of perioperative PET and estrogen receptor ligand in patients with invasive breast cancer.

Authors:  Mary L Gemignani; Sujata Patil; Venkatraman E Seshan; Michelle Sampson; John L Humm; Jason S Lewis; Edi Brogi; Steven M Larson; Monica Morrow; Neeta Pandit-Taskar
Journal:  J Nucl Med       Date:  2013-08-22       Impact factor: 10.057

10.  Comparison of 18F-FES, 18F-FDG, and 18F-FMISO PET Imaging Probes for Early Prediction and Monitoring of Response to Endocrine Therapy in a Mouse Xenograft Model of ER-Positive Breast Cancer.

Authors:  SiMin He; MingWei Wang; ZhongYi Yang; JianPing Zhang; YongPing Zhang; JianMin Luo; YingJian Zhang
Journal:  PLoS One       Date:  2016-07-28       Impact factor: 3.240

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  11 in total

Review 1.  Clinical Evaluation of Nuclear Imaging Agents in Breast Cancer.

Authors:  Ziqi Li; Mariam S Aboian; Xiaohua Zhu; Bernadette Marquez-Nostra
Journal:  Cancers (Basel)       Date:  2022-04-23       Impact factor: 6.575

2.  Determination of binding affinity of molecular imaging agents for steroid hormone receptors in breast cancer.

Authors:  Kelley Salem; Manoj Kumar; Kyle C Kloepping; Ciara J Michel; Yongjun Yan; Amy M Fowler
Journal:  Am J Nucl Med Mol Imaging       Date:  2018-04-25

Review 3.  Recent Advances in Imaging Steroid Hormone Receptors in Breast Cancer.

Authors:  Manoj Kumar; Kelley Salem; Amye J Tevaarwerk; Roberta M Strigel; Amy M Fowler
Journal:  J Nucl Med       Date:  2019-11-15       Impact factor: 10.057

4.  PET Imaging of Estrogen Receptors Using 18F-Based Radioligands.

Authors:  Manoj Kumar; Kelley Salem; Justin J Jeffery; Amy M Fowler
Journal:  Methods Mol Biol       Date:  2022

5.  A preclinical PET dual-tracer imaging protocol for ER and HER2 phenotyping in breast cancer xenografts.

Authors:  Michel Paquette; Serge Phoenix; Christine Lawson; Brigitte Guérin; Roger Lecomte; Lee-Hwa Tai; Éric E Turcotte; Jeffrey V Leyton
Journal:  EJNMMI Res       Date:  2020-06-26       Impact factor: 3.138

Review 6.  Insight into the Development of PET Radiopharmaceuticals for Oncology.

Authors:  Joseph Lau; Etienne Rousseau; Daniel Kwon; Kuo-Shyan Lin; François Bénard; Xiaoyuan Chen
Journal:  Cancers (Basel)       Date:  2020-05-21       Impact factor: 6.639

7.  Non-conventional and Investigational PET Radiotracers for Breast Cancer: A Systematic Review.

Authors:  Michele Balma; Virginia Liberini; Manuela Racca; Riccardo Laudicella; Matteo Bauckneht; Ambra Buschiazzo; Daniele Giovanni Nicolotti; Simona Peano; Andrea Bianchi; Giovanni Albano; Natale Quartuccio; Ronan Abgral; Silvia Daniela Morbelli; Calogero D'Alessandria; Enzo Terreno; Martin William Huellner; Alberto Papaleo; Désirée Deandreis
Journal:  Front Med (Lausanne)       Date:  2022-04-12

Review 8.  Recent Advances in Nuclear Imaging of Receptor Expression to Guide Targeted Therapies in Breast Cancer.

Authors:  Barbara Salvatore; Maria Grazia Caprio; Billy Samuel Hill; Annachiara Sarnella; Giovanni Nicola Roviello; Antonella Zannetti
Journal:  Cancers (Basel)       Date:  2019-10-22       Impact factor: 6.639

Review 9.  Development of Radiotracers for Breast Cancer-The Tumor Microenvironment as an Emerging Target.

Authors:  Amelie Heesch; Jochen Maurer; Elmar Stickeler; Mohsen Beheshti; Felix M Mottaghy; Agnieszka Morgenroth
Journal:  Cells       Date:  2020-10-21       Impact factor: 6.600

10.  ZR-75-1 breast cancer models to study the utility of 18F-FES by PET imaging.

Authors:  Ziteng Ding; Xudang Xu; Tiannv Li; Jia Wang; Jin Sun; Lijun Tang
Journal:  Transl Cancer Res       Date:  2021-03       Impact factor: 1.241

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