DOCSLIB.ORG

PET Imaging Agents (FES, FFNP, and FDHT) for Estrogen, Androgen, and Progesterone Receptors to Improve Management of Breast and Prostate Cancers by Functional Imaging

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
PET Imaging Agents (FES, FFNP, and FDHT) for Estrogen, Androgen, and Progesterone Receptors to Improve Management of Breast and Prostate Cancers by Functional Imaging cancers Review PET Imaging Agents (FES, FFNP, and FDHT) for Estrogen, Androgen, and Progesterone Receptors to Improve Management of Breast and Prostate Cancers by Functional Imaging John A. Katzenellenbogen Department of Chemistry and Cancer Center at Illinois, University of Illinois at Urbana-Champaign, Urbana, IL 61801, USA; [email protected], Tel.: +1-217-333-6310; Fax: +1-217-333-7325 Received: 1 June 2020; Accepted: 17 July 2020; Published: 23 July 2020 Abstract: Many breast and prostate cancers are driven by the action of steroid hormones on their cognate receptors in primary tumors and in metastases, and endocrine therapies that inhibit hormone production or block the action of these receptors provide clinical benefit to many but not all of these cancer patients. Because it is difficult to predict which individuals will be helped by endocrine therapies and which will not, positron emission tomography (PET) imaging of estrogen receptor (ER) and progesterone receptor (PgR) in breast cancer, and androgen receptor (AR) in prostate cancer can provide useful, often functional, information on the likelihood of endocrine therapy response in individual patients. This review covers our development of three PET imaging agents, 16α-[18F]fluoroestradiol (FES) for ER, 21-[18F]fluoro-furanyl-nor-progesterone (FFNP) for PgR, and 16β-[18F]fluoro-5α-dihydrotestosterone (FDHT) for AR, and the evolution of their clinical use. For these agents, the pathway from concept through development tracks with an emerging understanding of critical performance criteria that is needed for successful PET imaging of these low-abundance receptor targets. Progress in the ongoing evaluation of what they can add to the clinical management of breast and prostate cancers reflects our increased understanding of these diseases and of optimal strategies for predicting the success of clinical endocrine therapies. Keywords: FES; FFNP; FDHT; receptor-targeting; PET imaging; radiopharmaceuticals; endocrine therapy; breast cancer; prostate cancer; hormone-challenge test 1. Introduction Steroid receptors are transcription factors that play major roles during development, and in both adult men and women, they control reproduction and regulate many other organ systems; they are also important regulators of the growth and spread of various hormone-dependent cancers. This review will cover principally the development of agents to image the estrogen receptor (ER) and the progesterone receptor (PgR) in breast cancer and the androgen receptor (AR) in prostate cancer. Imaging agents for these targets have been labeled with different radioisotopes (various radiohalogens, carbon-11, and radiometals) and have been developed for use with different tomographic imaging devices. Here, I will cover the development of three positron emission tomography (PET) imaging agents labeled with fluorine-18 that have reached the clinic and continue to be of great utility and actively investigated: 16α-[18F]fluoroestradiol (FES) and 21-[18F]fluoro-furanyl-nor-progesterone (FFNP) for breast cancer and 16β-[18F]fluoro-5α-dihydrotestosterone (FDHT) for prostate cancer (Figure1). Cancers 2020, 12, 2020; doi:10.3390/cancers12082020 www.mdpi.com/journal/cancers Cancers 2020, 12, 2020 2 of 32 CancersCancers 2020 2020, 12, 12, ,x x 22 of of 32 32 EstrogenEstrogen Receptor Receptor Breast Cancer Breast Cancer FESFES ProgesteroneProgesterone Receptor Receptor BreastBreast Cancer Cancer FFNPFFNP AndrogenAndrogen Receptor Receptor ProstateProstate Cancer Cancer FDHTFDHT FigureFigure 1. 1. Structures Structures of of 16 16 αα-[-[1818F]fluoroestradiolF]fluoroestradiolF]fluoroestradiol (FES), (FES), (FES), 21-[ 21-[ 21-[181818F]fluoro-furanyl-nor-progesteroneF]fluoro-furanyl-nor-progesteroneF]fluoro-furanyl-nor-progesterone (FFNP) (FFNP) andand 16 16ββ-[-[1818F]fluoro-5F]fluoro-5F]fluoro-5αα-dihydrotestosteroneα-dihydrotestosterone-dihydrotestosterone (FDHT), (FDHT), (FDHT), with with with thei thei theirr rhormone hormone hormone receptor receptor receptor targets targets and and use use in in cancercancer noted noted at at left. left. TheThe initial initial synthesis, synthesis, radiolabeling, radiolabeling, and and in in vivo vivo studies studies in in animal animal models models and and humans humans for for these these threethree PET PET probes probesprobes were werewere initiated initiatedinitiated in inin the thethe 1970s 1970s1970s and andand 1980s, 1980s,1980s, and andand culminated culminatedculminated with withwith first-in-man/woman first-in-manfirst-in-man/woman/woman reportsreports for for FES FES in in 1984 1984 [1,2], [[1,2],1,2], FDHT FDHTFDHT in inin 2005 20052005 [3], [[3],3], and andand FFNP FFNPFFNP in inin 2012 20122012 [4]. [[4].4]. For For several several prior prior years, years, early early investigationsinvestigations leadingleading to toto the thethe development developmentdevelopment of these ofof thesthes agentsee agentsagents animated animatedanimated the frontier thethe frontierfrontier of the rapidly ofof thethe evolving rapidlyrapidly evolvingfieldevolving of receptor-binding field field of of receptor receptor radiotracers.-binding-binding radiotracers. radiotracers. The results The The from results results our researchfrom from our our and research research that of and others,and that that and of of others, theothers, insights and and thewethe insights allinsights gained we we from all all gained them,gained werefrom fromoften them, them, taking were were theoften often lead taking taking in defining the the lead lead the in in technical defining defining advances the the technical technical and conceptualadvances advances andunderstandingand conceptual conceptual understanding thatunderstanding are now common that that are are knowledgenow now commo commo innn theknowledge knowledge design and in in the developmentthe design design and and of development development radiotracers forof of radiotracerslimitedradiotracers capacity for for limited limited high acapacity fficapacitynity receptor hi highgh affinity affinity targets. receptor receptor The technicaltargets. targets. The The advances technical technical were advances advances in isotope were were production; in in isotope isotope production;chemicalproduction; reactivity chemical chemical of reactivity reactivity the radionuclide; of of the the radionuclide; radionuclide; and efficiency, and and ease, efficiency, efficiency, and speed ease, ease, of and and radiolabeling speed speed of of radiolabeling radiolabeling and product andpurification;and product product thepurification;purification; conceptual the the understandings conceptual conceptual understand understand were of performanceingsings were were of criteriaof performance performance critical for criteria criteria receptor-targeted critical critical for for receptor-targetedradiotracers,receptor-targeted i.e., radiotracers, targetradiotracers, binding i.e., i.e., affi target nity;target selectivitybindin bindingg affinity; affinity; and capacity; selectivity selectivity imaging and and probecapacity;capacity; molar imaging imaging activity; probe probe and molardistribution,molar activity; activity; metabolism, and and distribution, distribution, and clearancemetabolism, metabolism, behavior. and and clea clea Attentionrancerance behavior. behavior. to all Attentionof Attention these factors to to all all of wasof these these needed factors factors to wasproducewas needed needed PET to to probes produce produce that PET PET gave probes probes informative that that gave gavein vivo informative informativeimages, becausein in vivo vivo images, onlyimages, low because because levels of only only these low low high levels levels affinity of of thesereceptorsthese high high areaffinity affinity present receptors receptors in human are are present breastpresent andin in human human prostate breast breast tumors. and and Inprostate prostate the three tumors. tumors. sections In In the the that three three follow, sections sections these thatfacetsthat follow, follow, of technical these these facets facets and conceptualof of technical technical advancesand and conceptual conceptual are wrapped advances advances into are are historical wrapped wrapped accounts into into historical historical of the developmentaccounts accounts of of the the of developmentFES,development FDHT, and ofof FFNP,FES,FES, FDHT, includingFDHT, andand informative FFNP,FFNP, includingincluding missteps informativeinformative that occurred misstepsmissteps along the thatthat development occurredoccurred along pathways.along thethe developmentEachdevelopment of these pathways. threepathways. sections Each Each ends of of these these with three athree description sections sections ofen ends edsff ortswith with to a a improvedescription description these of of threeefforts efforts clinically to to improve improve used these these PET threeimagingthree clinically clinically agents, used used including PET PET imaging imaging some agents, suggestionsagents, including including for future some some studiessuggestions suggestions that for mightfor future future be worthwhile.studies studies that that might Themight final be be worthwhile.sectionworthwhile. provides The The final final a summary section section provides ofprovides clinical a a summary investigationssummary of of clinical clinical involving investigations investigations these three involving involving agents, these withthese anthree three indication agents, agents, withthatwith an manyan indication indication new studies that that many many are ongoingnew
Load more

Recommended publications
  • Colitis Caused by Non-Steroidal Anti-Inflammatory Drugs
    Postgrad Med J: first published as 10.1136/pgmj.62.730.773 on 1 August 1986. Downloaded from Postgraduate Medical Journal (1986) 62, 773-776 Colitis caused by non-steroidal anti-inflammatory drugs S. Ravi', A.C. Keat2 and E.C.B. Keat1 'Cuckfield Hospital, Cuckfield, West Sussex, and2Westminster Hospital, Horseferry Road, London SWIP2AP, UK. Summary: Four cases of acute proctocolitis associated with non-steroidal anti-inflammatory drug therapy are presented. The drugs implicated were flufenamic acid, mefenamic acid, naproxen and ibuprofen. After resolution of symptoms and signs of proctocolitis three of the four patients were subsequently rechallenged with the implicated drug: in each there was a rapid relapse. Introduction Ulcerative colitis is a disease of unknown aetiology Case reports with characteristic clinical features and a protracted course. A similar clinical picture, but running a shorter Case I and usually benign course, is occasionally seen follow- ing the administration of certain drugs. This was first A 77 year old woman was referred with intermittent noticed following the administration of antibiotics, bleeding per rectum for 6 months, associated for the often with pseudomembrane formation. Later, this last 2 months with bloody diarrhoea up to eight times was shown to be associated with infection by toxigenic daily. Previously, she had had troublesome symptoms Clostridium difficile. Until 1978, most cases were from osteoarthritis of her back and knees for which copyright. associated with treatment with clindamycin but since she had been prescribed flufenamic acid 200 mg thrice that time nearly all antibiotics have been implicated. daily. Her general health had remained good but she Other drugs capable of causing proctocolitis, though appeared pale and her haemoglobin was reduced to by different mechanisms, include phenindione (Keat & 8 g/dl.
    [Show full text]
  • Investigating the Influence of Polymers on Supersaturated
    Page 1 of 45 Molecular Pharmaceutics 1 2 3 4 5 6 7 Investigating the Influence of Polymers on 8 9 10 11 12 Supersaturated Flufenamic Acid Cocrystal Solutions 13 14 15 16 1 1 2 2 1 17 Minshan Guo , Ke Wang , Noel Hamill , Keith Lorimer and Mingzhong Li * 18 19 20 1School of pharmacy, De Montfort University, Leicester, UK 21 22 23 2Almac Science, Seagoe Industrial Estate, Craigavon, UK 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 ACS Paragon Plus Environment 1 Molecular Pharmaceutics Page 2 of 45 1 2 3 4 5 6 7 Table of contents graphic 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 ACS Paragon Plus Environment 2 Page 3 of 45 Molecular Pharmaceutics 1 2 3 Abstract 4 5 6 7 The development of enabling formulations is a key stage when demonstrating the effectiveness 8 9 10 of pharmaceutical cocrystals to maximize the oral bioavailability for poorly water soluble drugs. 11 12 Inhibition of drug crystallization from a supersaturated cocrystal solution through a fundamental 13 14 understanding of the nucleation and crystal growth is important. In this study, the influence of 15 16 17 the three polymers of polyethylene glycol (PEG), polyvinylpyrrolidone (PVP) and a copolymer 18 19 of N-vinly-2-pyrrodidone (60%) and vinyl acetate (40%) (PVP-VA) on the flufenamic acid 20 21 22 (FFA) crystallization from three different supersaturated solutions of the pure FFA and two 23 24 cocrystals of FFA-NIC CO and FFA-TP CO has been investigated by measuring nucleation 25 26 induction times and desupersaturation rates in the presence and absence of seed crystals.
    [Show full text]
  • Systems and Chemical Biology Approaches to Study Cell Function and Response to Toxins
    Dissertation submitted to the Combined Faculties for the Natural Sciences and for Mathematics of the Ruperto-Carola University of Heidelberg, Germany for the degree of Doctor of Natural Sciences Presented by MSc. Yingying Jiang born in Shandong, China Oral-examination: Systems and chemical biology approaches to study cell function and response to toxins Referees: Prof. Dr. Rob Russell Prof. Dr. Stefan Wölfl CONTRIBUTIONS The chapter III of this thesis was submitted for publishing under the title “Drug mechanism predominates over toxicity mechanisms in drug induced gene expression” by Yingying Jiang, Tobias C. Fuchs, Kristina Erdeljan, Bojana Lazerevic, Philip Hewitt, Gordana Apic & Robert B. Russell. For chapter III, text phrases, selected tables, figures are based on this submitted manuscript that has been originally written by myself. i ABSTRACT Toxicity is one of the main causes of failure during drug discovery, and of withdrawal once drugs reached the market. Prediction of potential toxicities in the early stage of drug development has thus become of great interest to reduce such costly failures. Since toxicity results from chemical perturbation of biological systems, we combined biological and chemical strategies to help understand and ultimately predict drug toxicities. First, we proposed a systematic strategy to predict and understand the mechanistic interpretation of drug toxicities based on chemical fragments. Fragments frequently found in chemicals with certain toxicities were defined as structural alerts for use in prediction. Some of the predictions were supported with mechanistic interpretation by integrating fragment- chemical, chemical-protein, protein-protein interactions and gene expression data. Next, we systematically deciphered the mechanisms of drug actions and toxicities by analyzing the associations of drugs’ chemical features, biological features and their gene expression profiles from the TG-GATEs database.
    [Show full text]
  • Epilepsy & Seizure
    Epilepsy & Seizure Journal of Japan Epilepsy Society Vol.4 No.1 (2011) pp.15-25 Original Article Usefulness of 123I-iomazenil SPECT for childhood focal epilepsies 1) 1) 1) 1) Kentaro Okamoto, MD , Hirokazu Oguni, MD , Yoshiko Hirano, MD , Makiko Osawa, MD 1Department of Pediatrics, Tokyo Women's Medical University, 8-1 Kawada-cho, Shinjuku-ku, Tokyo 162-8666, Japan Key words: focal epilepsy, children, 123I-iomazenil SPECT, epileptic foci Published online July 29, 2011 Abstract Purpose: We investigated the usefulness of obtained from visualization of IMZ-SPECT 123I-iomazenil (IMZ-) SPECT to detect epilep- images and those speculated based on a com- tic foci in children with symptomatic focal bination of clinical manifestations, EEG find- epilepsy (SFE). ings, and brain MRI. We then verified the Subjects: 21 children with SFE who under- concordance of the results between the two went IMZ-SPECT to identify the epileptic fo- methods. cus were studied. Results: There was concordance in both later- Methods: We retrospectively compared the alization and localization in 9/12 patients with localization and lateralization of epileptic foci temporal lobe epilepsy (75%), in 2/5 patients Correspondence to: Hirokazu Oguni, MD, Department of Pediatrics, Tokyo Women's Medical University, 8-1 Kawada-cho, Shinjuku-ku, Tokyo 162, Japan Tel. 81-3-3353-8111, Fax. 81-3-5269-7338, [email protected] 15 Kentaro Okamoto, et al. IMZ-SPECT for childhood epilepsy with frontal lobe epilepsy (40%), and in 2/4 interictal/ictal cerebral blood flow single pho- patients with parieto-occipital lobe epilepsy ton emission computed tomography (SPECT) (50%).
    [Show full text]
  • Big Pain Assays Aren't a Big Pain with the Raptor Biphenyl LC Column
    Featured Application: 231 Pain Management and Drugs of Abuse Compounds in under 10 Minutes by LC-MS/MS Big Pain Assays Aren’t a Big Pain with the Raptor Biphenyl LC Column • 231 compounds, 40+ isobars, 10 drug classes, 22 ESI- compounds in 10 minutes with 1 column. • A Raptor SPP LC column with time-tested Restek Biphenyl selectivity is the most versatile, multiclass-capable LC column available. • Achieve excellent separation of critical isobars with no tailing peaks. • Run fast and reliable high-throughput LC-MS/MS analyses with increased sensitivity using simple mobile phases. The use of pain management drugs is steadily increasing. As a result, hospital and reference labs are seeing an increase in patient samples that must be screened for a wide variety of pain management drugs to prevent drug abuse and to ensure patient safety and adherence to their medication regimen. Thera- peutic drug monitoring can be challenging due to the low cutoff levels, potential matrix interferences, and isobaric drug compounds. To address these chal- lenges, many drug testing facilities are turning to liquid chromatography coupled with mass spectrometry (LC-MS/MS) for its increased speed, sensitivity, and specificity. As shown in the analysis below, Restek’s Raptor Biphenyl column is ideal for developing successful LC-MS/MS pain medication screening methodologies. With its exceptionally high retention and unique selectivity, 231 multiclass drug compounds and metabolites—including over 40 isobars—can be analyzed in just 10 minutes. In addition, separate panels have been optimized on the Raptor Biphenyl column specifically for opioids, antianxiety drugs, barbiturates, NSAIDs and analgesics, antidepressants, antiepileptics, antipsychotics, hallucinogens, and stimulants for use during confirmation and quantitative analyses.
    [Show full text]
  • Flufenamic Acid, Mefenamic Acid and Niflumic Acid Inhibit Single Nonselective Cation Channels in the Rat Exocrine Pancreas
    View metadata, citation and similar papers at core.ac.uk brought to you by CORE provided by Elsevier - Publisher Connector Volume 268, number 1, 79-82 FEBS 08679 July 1990 Flufenamic acid, mefenamic acid and niflumic acid inhibit single nonselective cation channels in the rat exocrine pancreas H. Gagelein*, D. Dahlem, H.C. Englert** and H.J. Lang** Max-Planck-Institutfir Biophysik, Kennedyallee 70, D-600 Frankfurt/Main 70, FRG Received 17 May 1990 The non-steroidal anti-inflammatory drugs, flufenamic acid, mefenamic acid and niflumic acid, block Ca2+-activated non-selective cation channels in inside-out patches from the basolateral membrane of rat exocrine pancreatic cells. Half-maximal inhibition was about 10 PM for flufenamic acid and mefenamic acid, whereas niflumic acid was less potent (IC,, about 50 PM). Indomethacin, aspirin, diltiazem and ibuprofen (100 /IM) had not effect. It is concluded that the inhibitory effect of flufenamate, mefenamate and niflumate is dependent on the specific structure, consisting of two phenyl rings linked by an amino bridge. Mefenamic acid; Flufenamic acid; Niflumic acid; Indomethacin; Non-selective cation channel; Rat exocrine pancreas 1. INTRODUCTION indomethacin, ibuprofen, diltiazem and acetylsalicylic acid (aspirin) were obtained from Sigma (Munich, FRG). The substances were dissolved in dimethylsulfoxide (DMSO, Merck, Darmstadt, FRG, Recently it was reported that the drug, 3 ’ ,5-dichloro- 0.1% of total volume) before addition to the measuring solution. diphenylamine-2-carboxylic acid (DCDPC), blocks DMSO alone had no effect on the single channel recordings. non-selective cation channels in the basolateral mem- 2.2. Methods brane of rat exocrine pancreatic cells [ 11.
    [Show full text]
  • Imaging in Parkinson's Disease
    Clinical Medicine 2016 Vol 16, No 4: 371–5 CME MOVEMENT DISORDERS I m a g i n g i n P a r k i n s o n ’ s d i s e a s e Authors: G e n n a r o P a g a n o , A F l a v i a N i c c o l i n i B a n d M a r i o s P o l i t i s C The clinical presentation of Parkinson’s disease (PD) Abnormal intra-neuronal (Lewy bodies) and intra-neuritic is heterogeneous and overlaps with other conditions, (Lewy neurites) deposits of fibrillary aggregates are currently including the parkinsonian variant of multiple system considered the key neuropathological alterations in PD. atrophy (MSA-P), progressive supranuclear palsy (PSP) and The majority of these aggregates, mainly composed of alpha essential tremor. Imaging of the brain in patients with (α)−synuclein, are located at presynaptic level and impair ABSTRACT parkinsonism has the ability to increase the accuracy of axonal trafficking, resulting in a series of noxious events that differential diagnosis. Magnetic resonance imaging (MRI), cause neuronal damage to the substantia nigra pars compacta single photon emission computed tomography (SPECT) and with a subsequent dopaminergic denervation of the striatum. positron emission tomography (PET) allow brain imaging The cardinal motor features of PD (bradykinesia and rigidity, of structural, functional and molecular changes in vivo in with or without resting tremor) manifest after a substantial patients with PD. Structural MRI is useful to differentiate denervation of substantia nigra, which is associated with about PD from secondary and atypical forms of parkinsonism.
    [Show full text]
  • Chapter 2 PET and SPECT Imaging of Steroid Hormone Receptors
    University of Groningen PET imaging of brain sex steroid hormone receptors and the role of estrogen in depression Khayum, Mohamed Abdul IMPORTANT NOTE: You are advised to consult the publisher's version (publisher's PDF) if you wish to cite from it. Please check the document version below. Publication date: 2015 Link to publication in University of Groningen/UMCG research database Citation for published version (APA): Khayum, M. A. (2015). PET imaging of brain sex steroid hormone receptors and the role of estrogen in depression. University of Groningen. Copyright Other than for strictly personal use, it is not permitted to download or to forward/distribute the text or part of it without the consent of the author(s) and/or copyright holder(s), unless the work is under an open content license (like Creative Commons). Take-down policy If you believe that this document breaches copyright please contact us providing details, and we will remove access to the work immediately and investigate your claim. Downloaded from the University of Groningen/UMCG research database (Pure): http://www.rug.nl/research/portal. For technical reasons the number of authors shown on this cover page is limited to 10 maximum. Download date: 27-09-2021 Chapter 2 PET and SPECT Imaging of Steroid Hormone Receptors Khayum MA, Doorduin J, Glaudemans AWJM, Dierckx RAJO, de Vries EFJ. PET and SPECT of Neurobiological Systems, R.A.J.O. Dierckx et al. (eds.) DOI 10.1007/978-3-642-42014-6_14, © Springer-Verlag Berlin Heidelberg 2014 Chapter 2 Abstract Steroid hormones like estrogens, progestins, androgens and corticosteroids are involved in normal brain function.
    [Show full text]
  • Preclinical Evaluation of Protein Disulfide Isomerase Inhibitors for the Treatment of Glioblastoma by Andrea Shergalis
    Preclinical Evaluation of Protein Disulfide Isomerase Inhibitors for the Treatment of Glioblastoma By Andrea Shergalis A dissertation submitted in partial fulfillment of the requirements for the degree of Doctor of Philosophy (Medicinal Chemistry) in the University of Michigan 2020 Doctoral Committee: Professor Nouri Neamati, Chair Professor George A. Garcia Professor Peter J. H. Scott Professor Shaomeng Wang Andrea G. Shergalis [email protected] ORCID 0000-0002-1155-1583 © Andrea Shergalis 2020 All Rights Reserved ACKNOWLEDGEMENTS So many people have been involved in bringing this project to life and making this dissertation possible. First, I want to thank my advisor, Prof. Nouri Neamati, for his guidance, encouragement, and patience. Prof. Neamati instilled an enthusiasm in me for science and drug discovery, while allowing me the space to independently explore complex biochemical problems, and I am grateful for his kind and patient mentorship. I also thank my committee members, Profs. George Garcia, Peter Scott, and Shaomeng Wang, for their patience, guidance, and support throughout my graduate career. I am thankful to them for taking time to meet with me and have thoughtful conversations about medicinal chemistry and science in general. From the Neamati lab, I would like to thank so many. First and foremost, I have to thank Shuzo Tamara for being an incredible, kind, and patient teacher and mentor. Shuzo is one of the hardest workers I know. In addition to a strong work ethic, he taught me pretty much everything I know and laid the foundation for the article published as Chapter 3 of this dissertation. The work published in this dissertation really began with the initial identification of PDI as a target by Shili Xu, and I am grateful for his advice and guidance (from afar!).
    [Show full text]
  • Brain Imaging
    Publications · Brochures Brain Imaging A Technologist’s Guide Produced with the kind Support of Editors Fragoso Costa, Pedro (Oldenburg) Santos, Andrea (Lisbon) Vidovič, Borut (Munich) Contributors Arbizu Lostao, Javier Pagani, Marco Barthel, Henryk Payoux, Pierre Boehm, Torsten Pepe, Giovanna Calapaquí-Terán, Adriana Peștean, Claudiu Delgado-Bolton, Roberto Sabri, Osama Garibotto, Valentina Sočan, Aljaž Grmek, Marko Sousa, Eva Hackett, Elizabeth Testanera, Giorgio Hoffmann, Karl Titus Tiepolt, Solveig Law, Ian van de Giessen, Elsmarieke Lucena, Filipa Vaz, Tânia Morbelli, Silvia Werner, Peter Contents Foreword 4 Introduction 5 Andrea Santos, Pedro Fragoso Costa Chapter 1 Anatomy, Physiology and Pathology 6 Elsmarieke van de Giessen, Silvia Morbelli and Pierre Payoux Chapter 2 Tracers for Brain Imaging 12 Aljaz Socan Chapter 3 SPECT and SPECT/CT in Oncological Brain Imaging (*) 26 Elizabeth C. Hackett Chapter 4 Imaging in Oncological Brain Diseases: PET/CT 33 EANM Giorgio Testanera and Giovanna Pepe Chapter 5 Imaging in Neurological and Vascular Brain Diseases (SPECT and SPECT/CT) 54 Filipa Lucena, Eva Sousa and Tânia F. Vaz Chapter 6 Imaging in Neurological and Vascular Brain Diseases (PET/CT) 72 Ian Law, Valentina Garibotto and Marco Pagani Chapter 7 PET/CT in Radiotherapy Planning of Brain Tumours 92 Roberto Delgado-Bolton, Adriana K. Calapaquí-Terán and Javier Arbizu Chapter 8 PET/MRI for Brain Imaging 100 Peter Werner, Torsten Boehm, Solveig Tiepolt, Henryk Barthel, Karl T. Hoffmann and Osama Sabri Chapter 9 Brain Death 110 Marko Grmek Chapter 10 Health Care in Patients with Neurological Disorders 116 Claudiu Peștean Imprint 126 n accordance with the Austrian Eco-Label for printed matters.
    [Show full text]
  • Nuclear Medicine Imaging in Neuroblastoma: Current Status and New Developments
    Journal of Personalized Medicine Review Nuclear Medicine Imaging in Neuroblastoma: Current Status and New Developments Atia Samim 1,2, Godelieve A.M. Tytgat 1, Gitta Bleeker 3, Sylvia T.M. Wenker 1,2, Kristell L.S. Chatalic 1,2, Alex J. Poot 1,2, Nelleke Tolboom 1,2, Max M. van Noesel 1 , Marnix G.E.H. Lam 2 and Bart de Keizer 1,2,* 1 Princess Maxima Center for Pediatric Oncology, Heidelberglaan 25, 3584 CS Utrecht, The Netherlands; [email protected] (A.S.); [email protected] (G.A.M.T.); [email protected] (S.T.M.W.); [email protected] (K.L.S.C.); [email protected] (A.J.P.); [email protected] (N.T.); [email protected] (M.M.v.N.) 2 Department of Radiology and Nuclear Medicine, University Medical Center Utrecht/Wilhelmina Children’s Hospital, Heidelberglaan 100, 3584 CX Utrecht, The Netherlands; [email protected] 3 Department of Radiology and Nuclear Medicine, Northwest Clinics, Wilhelminalaan 12, 1815 JD Alkmaar, The Netherlands; [email protected] * Correspondence: [email protected]; Tel.: +31-887-571-794 Abstract: Neuroblastoma is the most common extracranial solid malignancy in children. At diagnosis, approximately 50% of patients present with metastatic disease. These patients are at high risk for refractory or recurrent disease, which conveys a very poor prognosis. During the past decades, Citation: Samim, A.; Tytgat, G.A.M.; nuclear medicine has been essential for the staging and response assessment of neuroblastoma. 123 123 Bleeker, G.; Wenker, S.T.M.; Currently, the standard nuclear imaging technique is meta-[ I]iodobenzylguanidine ([ I]mIBG) Chatalic, K.L.S.; Poot, A.J.; whole-body scintigraphy, usually combined with single-photon emission computed tomography Tolboom, N.; van Noesel, M.M.; with computed tomography (SPECT-CT).
    [Show full text]
  • (12) United States Patent (10) Patent No.: US 6,264,917 B1 Klaveness Et Al
    USOO6264,917B1 (12) United States Patent (10) Patent No.: US 6,264,917 B1 Klaveness et al. (45) Date of Patent: Jul. 24, 2001 (54) TARGETED ULTRASOUND CONTRAST 5,733,572 3/1998 Unger et al.. AGENTS 5,780,010 7/1998 Lanza et al. 5,846,517 12/1998 Unger .................................. 424/9.52 (75) Inventors: Jo Klaveness; Pál Rongved; Dagfinn 5,849,727 12/1998 Porter et al. ......................... 514/156 Lovhaug, all of Oslo (NO) 5,910,300 6/1999 Tournier et al. .................... 424/9.34 FOREIGN PATENT DOCUMENTS (73) Assignee: Nycomed Imaging AS, Oslo (NO) 2 145 SOS 4/1994 (CA). (*) Notice: Subject to any disclaimer, the term of this 19 626 530 1/1998 (DE). patent is extended or adjusted under 35 O 727 225 8/1996 (EP). U.S.C. 154(b) by 0 days. WO91/15244 10/1991 (WO). WO 93/20802 10/1993 (WO). WO 94/07539 4/1994 (WO). (21) Appl. No.: 08/958,993 WO 94/28873 12/1994 (WO). WO 94/28874 12/1994 (WO). (22) Filed: Oct. 28, 1997 WO95/03356 2/1995 (WO). WO95/03357 2/1995 (WO). Related U.S. Application Data WO95/07072 3/1995 (WO). (60) Provisional application No. 60/049.264, filed on Jun. 7, WO95/15118 6/1995 (WO). 1997, provisional application No. 60/049,265, filed on Jun. WO 96/39149 12/1996 (WO). 7, 1997, and provisional application No. 60/049.268, filed WO 96/40277 12/1996 (WO). on Jun. 7, 1997. WO 96/40285 12/1996 (WO). (30) Foreign Application Priority Data WO 96/41647 12/1996 (WO).
    [Show full text]