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Role of Radiolabelled Small Molecules Binding to PSMA in Diagnosis and Therapy of Prostate Cancer

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Book cover PET/CT in Prostate Cancer

Part of the book series: Clinicians’ Guides to Radionuclide Hybrid Imaging ((PET/CT))

Abstract

PET/CT with choline tracers has been used in the past for staging and detection of recurrent disease, but shows a low sensitivity and specificity, especially in patients with low PSA levels [1–3]. Therefore, novel tracers with improved imaging characteristics are needed. In this aspect the prostate-specific membrane antigen (PSMA) is a promising target. PSMA is a type II transmembrane protein with glutamate-carboxypeptidase and folate hydrolase activity, which shows overexpression on prostatic cancer including advanced stage prostate carcinomas [4, 5] and a low expression in normal tissues. After ligand binding to PSMA, the ligand-PSMA complex is internalized (Fig. 6.1), resulting in an effective accumulation of the bound molecule in the tumor cells. Together with a fast clearance of the tracer out of the circulation, this results in a high image quality for diagnosis and a high local dose for therapeutic applications. Several studies report that PSMA expression levels increase according to the stage and grade of the tumor [5–7]. Therefore, a variety of PSMA-targeted radioligands for diagnosis and therapy have been developed [8–23]. This chapter concentrates on small molecules binding to PSMA.

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Author information

Authors and Affiliations

  1. Department of Nuclear Medicine, University Hospital Heidelberg, Im Neuenheimer Feld 400, Heidelberg, 69120, Germany

    Uwe Haberkorn & Michael Eisenhut

  2. Clinical Cooperation Unit Nuclear Medicine, German Cancer Research Center (dkfz), Heidelberg, Germany

    Uwe Haberkorn & Michael Eisenhut

  3. Division of Radiopharmaceutical Chemistry, German Cancer Research Center (dkfz), Heidelberg, Germany

    Matthias Eder, Klaus Kopka & Michael Eisenhut

  4. Department of Radiopharmacy, Weill Cornell Medical College, New York, NY, USA

    John W. Babich

Authors
  1. Uwe Haberkorn
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  2. Matthias Eder
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  3. Klaus Kopka
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  4. John W. Babich
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  5. Michael Eisenhut
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Corresponding author

Correspondence to Uwe Haberkorn .

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Editors and Affiliations

  1. Department of Cancer Imaging, King’s College London, London, United Kingdom

    Gary Cook

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© 2017 Springer International Publishing AG

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Haberkorn, U., Eder, M., Kopka, K., Babich, J.W., Eisenhut, M. (2017). Role of Radiolabelled Small Molecules Binding to PSMA in Diagnosis and Therapy of Prostate Cancer. In: Cook, G. (eds) PET/CT in Prostate Cancer. Clinicians’ Guides to Radionuclide Hybrid Imaging(). Springer, Cham. https://doi.org/10.1007/978-3-319-57624-4_6

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  • DOI: https://doi.org/10.1007/978-3-319-57624-4_6

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  • Publisher Name: Springer, Cham

  • Print ISBN: 978-3-319-57623-7

  • Online ISBN: 978-3-319-57624-4

  • eBook Packages: MedicineMedicine (R0)

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