Literature DB >> 24973039

[¹⁸F]fluciclatide in the in vivo evaluation of human melanoma and renal tumors expressing αvβ 3 and α vβ 5 integrins.

Esther Mena1, Rikard Owenius, Baris Turkbey, Richard Sherry, Gennady Bratslavsky, Sven Macholl, Matthew P Miller, Ed J Somer, Liza Lindenberg, Stephen Adler, Joanna Shih, Peter Choyke, Karen Kurdziel.   

Abstract

PURPOSE: [(18)F]Fluciclatide is an integrin-targeted PET radiopharmaceutical. αvβ3 and αvβ5 are upregulated in tumor angiogenesis as well as on some tumor cell surfaces. Our aim was to use [(18)F]fluciclatide (formerly known as [(18)F]AH111585) for PET imaging of angiogenesis in melanoma and renal tumors and compare with tumor integrin expression.
METHODS: Eighteen evaluable patients with solid tumors ≥2.0 cm underwent [(18)F]fluciclatide PET/CT. All patients underwent surgery and tumor tissue samples were obtained. Immunohistochemical (IHC) staining with mouse monoclonal antibodies and diaminobenzidine (DAB) was applied to snap-frozen tumor specimens, and additional IHC was done on formalin-fixed paraffin-embedded samples. DAB optical density (OD) data from digitized whole-tissue sections were compared with PET SUV80% max, and Patlak influx rate constant (K i) data, tumor by tumor.
RESULTS: Tumors from all 18 patients demonstrated measurable [(18)F]fluciclatide uptake. At the final dynamic time-point (55 min after injection), renal malignancies (in 11 patients) demonstrated an average SUV80% max of 6.4 ± 2.0 (range 3.8 - 10.0), while the average SUV80% max for metastatic melanoma lesions (in 6 patients) was 3.0 ± 2.0 (range 0.7 - 6.5). There was a statistically significant difference in [(18)F]fluciclatide uptake between chromophobe and nonchromophobe renal cell carcinoma (RCCs, with SUV80% max of 8.2 ± 1.8 and 5.4 ± 1.4 (P = 0.020) and tumor-to-normal kidney (T/N) ratios of 1.5 ± 0.4 and 0.9 ± 0.2, respectively (P = 0.029). The highest Pearson's correlation coefficients were obtained when comparing Patlak K i and αvβ5 OD when segregating the patient population between melanoma and RCC (r = 0.83 for K i vs. melanoma and r = 0.91 for K i vs. RCC). SUV80% max showed a moderate correlation with αvβ5 and αvβ3 OD.
CONCLUSION: [(18)F]Fluciclatide PET imaging was well tolerated and demonstrated favorable characteristics for imaging αvβ3 and αvβ5 expression in melanoma and RCC. Higher uptake was observed in chromophobe than in nonchromophobe RCC. [(18)F]Fluciclatide may be a useful radiotracer to improve knowledge of integrin expression.

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Year:  2014        PMID: 24973039      PMCID: PMC6336392          DOI: 10.1007/s00259-014-2791-x

Source DB:  PubMed          Journal:  Eur J Nucl Med Mol Imaging        ISSN: 1619-7070            Impact factor:   9.236


  34 in total

1.  A randomized phase II study of cilengitide (EMD 121974) in patients with metastatic melanoma.

Authors:  Kevin B Kim; Victor Prieto; Richard W Joseph; Abdul H Diwan; Gary E Gallick; Nicholas E Papadopoulos; Agop Y Bedikian; Luis H Camacho; Patrick Hwu; Chaan S Ng; Wei Wei; Marcella M Johnson; Sabine M Wittemer; Anna Vardeleon; Aaron Reckeweg; A Dimitrios Colevas
Journal:  Melanoma Res       Date:  2012-08       Impact factor: 3.599

2.  Quantitative PET imaging of tumor integrin alphavbeta3 expression with 18F-FRGD2.

Authors:  Xianzhong Zhang; Zhengming Xiong; Yun Wu; Weibo Cai; Jeffery R Tseng; Sanjiv S Gambhir; Xiaoyuan Chen
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Review 3.  Radiolabelled RGD peptides for imaging and therapy.

Authors:  F C Gaertner; H Kessler; H-J Wester; M Schwaiger; A J Beer
Journal:  Eur J Nucl Med Mol Imaging       Date:  2012-02       Impact factor: 9.236

4.  Alpha v integrins as receptors for tumor targeting by circulating ligands.

Authors:  R Pasqualini; E Koivunen; E Ruoslahti
Journal:  Nat Biotechnol       Date:  1997-06       Impact factor: 54.908

5.  Graphical evaluation of blood-to-brain transfer constants from multiple-time uptake data. Generalizations.

Authors:  C S Patlak; R G Blasberg
Journal:  J Cereb Blood Flow Metab       Date:  1985-12       Impact factor: 6.200

6.  Monitoring tumor response to antiangiogenic sunitinib therapy with 18F-fluciclatide, an 18F-labeled αVbeta3-integrin and αV beta5-integrin imaging agent.

Authors:  Mark R Battle; Julian L Goggi; Lucy Allen; Jon Barnett; Matthew S Morrison
Journal:  J Nucl Med       Date:  2011-02-14       Impact factor: 10.057

7.  Use of a novel Arg-Gly-Asp radioligand, 18F-AH111585, to determine changes in tumor vascularity after antitumor therapy.

Authors:  Matthew S Morrison; Sally-Ann Ricketts; Jon Barnett; Alan Cuthbertson; Jean Tessier; Stephen R Wedge
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Review 8.  Radiolabeled tracers for imaging of tumor angiogenesis and evaluation of anti-angiogenic therapies.

Authors:  Roland Haubner; Hans-Jürgen Wester
Journal:  Curr Pharm Des       Date:  2004       Impact factor: 3.116

9.  Quantification of receptor-ligand binding with [¹⁸F]fluciclatide in metastatic breast cancer patients.

Authors:  Giampaolo Tomasi; Laura Kenny; Francesco Mauri; Federico Turkheimer; Eric O Aboagye
Journal:  Eur J Nucl Med Mol Imaging       Date:  2011-09-03       Impact factor: 9.236

10.  Noninvasive visualization of the activated alphavbeta3 integrin in cancer patients by positron emission tomography and [18F]Galacto-RGD.

Authors:  Roland Haubner; Wolfgang A Weber; Ambros J Beer; Eugenija Vabuliene; Daniel Reim; Mario Sarbia; Karl-Friedrich Becker; Michael Goebel; Rüdiger Hein; Hans-Jürgen Wester; Horst Kessler; Markus Schwaiger
Journal:  PLoS Med       Date:  2005-03-29       Impact factor: 11.069

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  16 in total

Review 1.  PET and SPECT imaging of melanoma: the state of the art.

Authors:  Weijun Wei; Emily B Ehlerding; Xiaoli Lan; Quanyong Luo; Weibo Cai
Journal:  Eur J Nucl Med Mol Imaging       Date:  2017-10-30       Impact factor: 9.236

2.  Systemic Delivery of Tumor-Targeted Bax-Derived Membrane-Active Peptides for the Treatment of Melanoma Tumors in a Humanized SCID Mouse Model.

Authors:  Anastassia Karageorgis; Michaël Claron; Romain Jugé; Caroline Aspord; Fabien Thoreau; Claire Leloup; Jérôme Kucharczak; Joël Plumas; Maxime Henry; Amandine Hurbin; Pascal Verdié; Jean Martinez; Gilles Subra; Pascal Dumy; Didier Boturyn; Abdel Aouacheria; Jean-Luc Coll
Journal:  Mol Ther       Date:  2017-02-01       Impact factor: 11.454

3.  A novel PET tracer for targeted imaging of atherosclerosis.

Authors:  Eliana Reyes
Journal:  J Nucl Cardiol       Date:  2015-02-28       Impact factor: 5.952

Review 4.  High-Throughput Approaches to the Development of Molecular Imaging Agents.

Authors:  Lina Y Hu; Kimberly A Kelly; Julie L Sutcliffe
Journal:  Mol Imaging Biol       Date:  2017-04       Impact factor: 3.488

5.  The Distribution Volume of 18F-Albumin as a Potential Biomarker of Antiangiogenic Treatment Efficacy.

Authors:  Jyoti Roy; Frank Kuo; Falguni Basuli; Mark R Williams; Karen Wong; Michael V Green; Jurgen Seidel; Stephen S Adler; Biying Xu; Peter L Choyke; Elaine M Jagoda
Journal:  Cancer Biother Radiopharm       Date:  2019-02-15       Impact factor: 3.099

6.  Preparation and evaluation of a 68Ga-labeled RGD-containing octapeptide for noninvasive imaging of angiogenesis: biodistribution in non-human primate.

Authors:  Irina Velikyan; Örjan Lindhe
Journal:  Am J Nucl Med Mol Imaging       Date:  2018-02-05

7.  (99m)Tc-3P-RGD2 SPECT to monitor early response to bevacizumab therapy in patients with advanced non-small cell lung cancer.

Authors:  Bin Chen; Guoqing Zhao; Qingjie Ma; Bin Ji; Tiefeng Ji; Hua Xin; Shi Gao
Journal:  Int J Clin Exp Pathol       Date:  2015-12-01

8.  RGD PET: From Lesion Detection to Therapy Response Monitoring.

Authors:  Gang Niu; Xiaoyuan Chen
Journal:  J Nucl Med       Date:  2015-11-25       Impact factor: 10.057

9.  [(18)F]FPRGD2 PET/CT imaging of integrin αvβ3 levels in patients with locally advanced rectal carcinoma.

Authors:  Nadia Withofs; Philippe Martinive; Jean Vanderick; Noëlla Bletard; Irène Scagnol; Frédéric Mievis; Fabrice Giacomelli; Philippe Coucke; Philippe Delvenne; Didier Cataldo; Sanjiv S Gambhir; Roland Hustinx
Journal:  Eur J Nucl Med Mol Imaging       Date:  2015-10-22       Impact factor: 9.236

Review 10.  Clinical Application of Radiolabeled RGD Peptides for PET Imaging of Integrin αvβ3.

Authors:  Haojun Chen; Gang Niu; Hua Wu; Xiaoyuan Chen
Journal:  Theranostics       Date:  2016-01-01       Impact factor: 11.556

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