Radiopharmaceutical Chemistry between Imaging and Endoradiotherapy by Klaus KopkaRadiopharmaceutical Chemistry between Imaging and Endoradiotherapy by Klaus Kopka

Radiopharmaceutical Chemistry between Imaging and Endoradiotherapy

Guest editorKlaus Kopka

Hardcover | September 1, 2015

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Positron emission tomography (PET), single photon emission computed tomography (SPECT), and the combined imaging modalities realised in the en-vogue hybrid technologies PET/CT and PET/MR represent the state-of-the-art diagnostic imaging technologies in nuclear medicine which are used for the highly sensitive non-invasive imaging of biological processes at the subcellular and molecular level in a respective patient for the visualisation of rather early disease states or for early inspection of treatment response after chemotherapy, radiation- or radioendotherapy.

Radiolabelled molecules, bearing a “radioactive lantern”, function as so called Radiopharmaceuticals which have to be compliant with the pharmaceuticals act, and can be termed as “food” of nuclear medicine. In general, the specialised field Radiopharmaceutical Chemistry focusses on the development, synthesis and radiolabelling of aforementioned “food”, such as small molecules, biotechnology-derived antibodies or (cyclised) (oligo)peptides which are used to address clinically relevant biological “downstream” targets such as receptors, enzymes, transport systems and others. Addressing “upstream” targets such as DNA- and RNA-fragments using corresponding radioactive substrates represents a further feasible strategy.

Originally, Radiopharmaceutical Chemistry descends from radiochemistry and radiopharmacy as well as nuclear chemistry and uses methods finally aiming at the production of radioactive substances for human application which are essential for non-invasive in vivo imaging by means of the aforementioned scintigraphic methods PET or SPECT.

The cornerstone for applicable radiochemistry in nuclear medicine was set by the Hungarian chemist George Charles de Hevesy who received the Nobel Prize in 1943 for his work on the radioindicator principle. This principle is based on the idea that the absolute amount of the administered substance is below the dose needed to induce a pharmacodynamic effect. Nowadays, a radioactive substance that can be traced in vivo as it moves through the living organism is termed radiotracer or radiopharmaceutical. As mentioned above, the biodistribution of radiopharmaceuticals is measured non-invasively reflecting functional or molecular disorders without pharmacologically affecting the organism.

In the era of personalised medicine the diagnostic potential of radiopharmaceuticals is directly linked to a subsequent individual therapeutic approach called radioendotherapy. Depending on the “radioactive lantern” (gamma or particle emitter) used for radiolabelling of the respective tracer molecule, the field Radiopharmaceutical Chemistry can contribute to the set-up of an in vivo “theranostic” approach especially in tumour patients by offering tailor-made (radio)chemical entities labelled either with a diagnostic or a therapeutic radionuclide.

To succeed in the design of targeted high-affinity radiopharmaceuticals that can measure the alteration of receptors serving at the same time as biological targets for individualised radioendotherapy several aspects need to be considered: (i) reasonable pharmacological behaviour (especially pharmacokinetics adjusted to the physical half-life of the used radionuclide), (ii) ability to penetrate and cross biological membranes, (iii) usage of chemical as well as biological amplification strategies (e.g. pretargeting, biological trapping of converted ligands, change of the physicochemical behaviour of the radiopharmaceutical after target interaction, combination with biotransporters and heterodimer approaches), (iv) availability of radiopharmaceuticals with high specific activities and in vivo stability.

Title:Radiopharmaceutical Chemistry between Imaging and EndoradiotherapyFormat:HardcoverProduct dimensions:256 pages, 9.61 × 6.69 × 0.81 inShipping dimensions:9.61 × 6.69 × 0.81 inPublished:September 1, 2015Publisher:MDPI AGLanguage:English

The following ISBNs are associated with this title:

ISBN - 10:3038420840

ISBN - 13:9783038420842


Table of Contents

Preface: Pharmaceuticals-Special Issue on Radiopharmaceutical Chemistry betweenImaging and EndoradiotherapyChapter 1: DefinitionsImaging Biomarkers or Biomarker Imaging?Chapter 2: Radiopharmaceutical AspectsNovel Preclinical and Radiopharmaceutical Aspects of [68Ga]Ga-PSMA-HBED-CC:A New PET Tracer for Imaging of Prostate CancerDevelopment and Successful Validation of Simple and Fast TLC Spot Tests forDetermination of Kryptofix® 2.2.2 and Tetrabutylammonium in 18F-LabeledRadiopharmaceuticalsChapter 3: Theranostic ApproachesIn Vivo Monitoring of the Antiangiogenic Effect of Neurotensin Receptor-MediatedRadiotherapy by Small-Animal Positron Emission Tomography: A Pilot StudySynthesis, Radiolabelling and In Vitro Characterization of the Gallium-68-, Yttrium-90- andLutetium-177-Labelled PSMA Ligand, CHX-A''-DTPA-DUPA-PepRadiolabeled Cetuximab Conjugates for EGFR Targeted Cancer Diagnostics and TherapyChapter 4: A Bispecific ApproachA Bombesin-Shepherdin Radioconjugate Designed for Combined Extra- and IntracellularTargetingChapter 5: A Targeted Alpha-Endoradiotherapy ApproachFolate Receptor Targeted Alpha-Therapy Using Terbium-149Chapter 6: The Nanoparticle ApproachRadiolabeling of Nanoparticles and Polymers for PET ImagingChapter 7: Targeted Brain ImagingSynthesis and Preliminary Evaluation of a 2-Oxoquinoline Carboxylic Acid Derivative for PETImaging the Cannabinoid Type 2 ReceptorAsymmetric Synthesis of Spirocyclic 2-Benzopyrans for Positron Emission Tomography of ?1Receptors in the Brain