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Radioisotopes in Drug Research and Development: Focus on Positron Emission Tomography [chapter]

Sosuke Miyoshi, Keisuke Mitsuoka, Shintaro Nishimura, Stephan A.
2011 Radioisotopes - Applications in Bio-Medical Science  
Other applications of radiolabeled compounds are to investigate apoptosis (Glaser et al., 2003) , DNA replication and cell cycle progression (Hoy et al., 1990) in oncology.  ...  These findings gave new insights in the metabolism, pharmacology and toxicology of the drug.  ...  Currently, only two PET tracers have been described in a guidance by the FDA to assist applicants in preparing New Drug Applications (NDAs) (Guidance PET Drug Applications -Content and Format for NDAs  ... 
doi:10.5772/22728 fatcat:rowvddrarrhf3j5iwh3gkc2ale

Molecular imaging with SPECT as a tool for drug development

Célia M. Gomes, Antero J. Abrunhosa, Pedro Ramos, Ernest K.J. Pauwels
2011 Advanced Drug Delivery Reviews  
Radionuclide-based imaging modalities such as single-photon emission computed tomography (SPECT) and positron emission tomography (PET) have proven to be useful in phases ranging from preclinical development  ...  The high sensitivity of these imaging modalities makes them particularly suited for exploratory investigational new drug (IND) studies as they have the potential to characterize in vivo pharmacokinetics  ...  A variety of SPECT tracers exist for many important targets in oncology and neurology. An overview of the most important is given below.  ... 
doi:10.1016/j.addr.2010.09.015 pmid:20933557 fatcat:xeyfnkixhredflujzzns5ybixm

Interest and Limits of [18F]ML-10 PET Imaging for Early Detection of Response to Conventional Chemotherapy

Elodie Jouberton, Sébastien Schmitt, Aurélie Maisonial-Besset, Emmanuel Chautard, Frédérique Penault-Llorca, Florent Cachin
2021 Frontiers in Oncology  
This review has pointed out the challenges of applying various apoptosis imaging strategies in clinical trials, the current methodologies available for image analysis and the future of molecular imaging  ...  One of the current challenges in oncology is to develop imaging tools to early detect the response to conventional chemotherapy and adjust treatment strategies when necessary.  ...  No Alternative Strategies to Overcome the Limited Applicability of [ 18 F]ML-10 PET Imaging Is Not the Right Candidate for Early Assessment of Therapeutic Response in Solid Tumors Applications Frontiers  ... 
doi:10.3389/fonc.2021.789769 pmid:34988022 pmcid:PMC8722713 fatcat:owz2uomgmndsbnjf6oxaa4zazu

TSPO expression in brain tumours: is TSPO a target for brain tumour imaging?

Federico Roncaroli, Zhangjie Su, Karl Herholz, Alexander Gerhard, Federico E. Turkheimer
2016 Clinical and translational imaging  
In this review, we will discuss the impact of preclinical PET studies and the application of TSPO imaging in human brain tumours, the advantages and disadvantages of TSPO imaging compared to other imaging  ...  modalities and other PET tracers, and pathology studies on the extent and distribution of TSPO in gliomas.  ...  Introduction PET imaging has increasingly been explored in the field of neuro-oncology for pre-operative prediction of tumour grade, monitoring of disease progression and response to treatment, and to  ... 
doi:10.1007/s40336-016-0168-9 pmid:27077069 pmcid:PMC4820497 fatcat:llvqgf35zffprjoxh77ibwzszq

PET Imaging of Inflammation Biomarkers

Chenxi Wu, Fang Li, Gang Niu, Xiaoyuan Chen
2013 Theranostics  
This review summarizes the potential inflammation imaging targets and corresponding PET tracers, and the applications of PET in major inflammatory diseases and tumor associated inflammation.  ...  In addition to glucose metabolism, a variety of targets for inflammation imaging are being discovered and utilized, some of which are considered superior to FDG for imaging inflammation.  ...  Acknowledgement This work was supported by the Intramural Research Program (IRP) of the National Institute of Biomedical Imaging and Bioengineering (NIBIB), National Institutes of Health (NIH).  ... 
doi:10.7150/thno.6592 pmid:23843893 pmcid:PMC3706689 fatcat:nj2t5la37bfohihsievanhf7iq

Molecular SPECT Imaging: An Overview

Magdy M. Khalil, Jordi L. Tremoleda, Tamer B. Bayomy, Willy Gsell
2011 International Journal of Molecular Imaging  
Moreover, the last section covers several application, of SPECT imaging in many areas of disease detection and diagnosis.  ...  between SPECT and PET, and focusing on different SPECT designs and detection systems.  ...  Tremoleda and Tamer B. Saleh contributed equally to the work.  ... 
doi:10.1155/2011/796025 pmid:21603240 pmcid:PMC3094893 fatcat:yfh6kqcdmnh53c5y6zh5dbzjpy

PET Imaging of the Human Nicotinic Cholinergic Pathway in Atherosclerosis

Matthias Bauwens, Felix M. Mottaghy, Jan Bucerius
2015 Current Cardiology Reports  
that might be an option for vascular nAChR PET imaging in the future.  ...  We also provide an overview of currently available nAChR positron emission tomography (PET) tracers and their performance in the noninvasive imaging of vascular nAChRs, as well as potential nAChR PET tracers  ...  coronary arteries, and to develop new PET tracers for different nAChRs, with the goal of proving the feasibility of nAChR PET imaging in the clinical context.  ... 
doi:10.1007/s11886-015-0614-8 pmid:26183620 pmcid:PMC4504985 fatcat:6du4esxmcbclhc6ffw5oz2sizm

Current paradigm of the 18-kDa translocator protein (TSPO) as a molecular target for PET imaging in neuroinflammation and neurodegenerative diseases

Alex Sik Chung Ching, Bertrand Kuhnast, Annelaure Damont, Dirk Roeda, Bertrand Tavitian, Frédéric Dollé
2011 Insights into Imaging  
From medical imaging perspectives, this review focuses on the current concepts related to the TSPO, and discusses briefly on the status of its PET imaging related to neuroinflammation and neurodegenerative  ...  TSPO expression may constitute a biomarker for brain inflammation that could be monitored by using TSPO tracers as neuroimaging agents.  ...  affinity for the TSPO with better uptake and binding potential than [ 11 C]PK11195 Table 2 2 Examples of new potential PET tracers for TSPO imaging in clinical studies AD Alzheimer's disease, ALS amyotrophic  ... 
doi:10.1007/s13244-011-0128-x pmid:22696004 pmcid:PMC3292648 fatcat:zktuxfhh6bfa7kzl2yfxpjcsne

Radioligands for Tropomyosin Receptor Kinase (Trk) Positron Emission Tomography Imaging

Ralf Schirrmacher, Justin J. Bailey, Andrew V. Mossine, Peter J. H. Scott, Lena Kaiser, Peter Bartenstein, Simon Lindner, David R. Kaplan, Alexey Kostikov, Gert Fricker, Anne Mahringer, Pedro Rosa-Neto (+6 others)
2019 Pharmaceuticals  
Basic developments in medicinal chemistry, radiolabeling and translational PET imaging in multiple species including humans are highlighted.  ...  Neurologic and oncologic studies of the spatiotemporal alterations in TrkA/B/C expression and density and the determination of target engagement of emerging antineoplastic clinical inhibitors in normal  ...  Another potential application for Trk-targeted radioligands stems from the renewed and rapidly growing interest in anti-Trk therapy for cancer.  ... 
doi:10.3390/ph12010007 pmid:30609832 pmcid:PMC6469173 fatcat:6qfskwzu3jdbncbto2vztuhxce

Unparalleled contribution of 18F-FDG PET to medicine over 3 decades

Sandip Basu, Abass Alavi
2008 Journal of Nuclear Medicine  
F-FDG PET to Medicine Over 3 Decades 18 Unparalleled Contribution of This article and updated information are available at:  ...  The success of 18 F-FDG has led the way for the development of new PET tracers with great promise for future expansion of the role of PET (2) (3) (4) (5) .  ...  for thrombolysis treatment. 18 F-FDG PET provides important prognostic information in CNS malignancies.  ... 
pmid:18832112 fatcat:bupf6hlzmjgbjopkhgbtq7gdgi

CXCR4-directed theranostics in oncology and inflammation

Malte Kircher, Peter Herhaus, Margret Schottelius, Andreas K. Buck, Rudolf A. Werner, Hans-Jürgen Wester, Ulrich Keller, Constantin Lapa
2018 Annals of Nuclear Medicine  
suitable for positron emission tomography (PET) imaging, in both hematologic and solid malignancy as well as in inflammatory conditions.  ...  Given its prominent role in inflammation and cancer biology, the C-X-C motif chemokine receptor 4 (CXCR4) has gained a lot of attention in the recent years.  ...  reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made.  ... 
doi:10.1007/s12149-018-1290-8 pmid:30105558 fatcat:giggpqhpobdhjkrvrqhjrulidi

Recent Advances in the Development and Application of Radiolabeled Kinase Inhibitors for PET Imaging

Vadim Bernard-Gauthier, Justin Bailey, Sheldon Berke, Ralf Schirrmacher
2015 Molecules  
Given that inhibitor coverage of the kinome is continuously expanding, in vivo PET imaging will likely find increasing applications for therapy monitoring and receptor density studies both in-and outside  ...  Novel radioligands for cancer and PET neuroimaging originating from novel but relevant target kinases are currently being explored in preclinical studies.  ...  Both [ 11 C]GW441756 and [ 18 F]40 are lead tracers for Trk PET imaging. Single tracers for EphB4 and MET have also been reported for tumor imaging.  ... 
doi:10.3390/molecules201219816 pmid:26690113 fatcat:q6zrowx5rfg7xfr7xl2fopx5vi

Fluorine-18 patents (2009–2015). Part 1: novel radiotracers

Allen F Brooks, Lindsey R Drake, Megan N Stewart, Brian P Cary, Isaac M Jackson, Dale Mallette, Andrew V Mossine, Peter JH Scott
2016 Pharmaceutical Patent Analyst  
In this review, we present the first analysis of patents issued for radiotracers labeled with fluorine-18 (between 2009 and 2015), and provide perspective on current trends and future directions in PET  ...  The most commonly utilized PET radionuclide is fluorine-18 ( 18 F) because of its convenient half-life and excellent imaging properties.  ...  New radiotracers for oncology imaging In oncology, PET imaging is a powerful diagnostic tool that allows for in vivo, noninvasive imaging for the improvement of diagnosis, management of therapy and improving  ... 
doi:10.4155/ppa.15.36 pmid:26670619 pmcid:PMC5561792 fatcat:ifg2j4ddirgr3gn5bc7eyql6pq

Molecular imaging in the development of a novel treatment paradigm for glioblastoma (GBM): an integrated multidisciplinary commentary

Monika A. Jarzabek, Kieron J. Sweeney, Rhys L. Evans, Andreas H. Jacobs, Roger Stupp, Donncha O'Brien, Mitchel S. Berger, Jochen H.M. Prehn, Annette T. Byrne
2013 Drug Discovery Today  
For the first time, using expertise from an integrated multidisciplinary group of authors, herein we present a comprehensive evaluation of state-of-the-art GBM imaging and explore how advances facilitate  ...  The part played by molecular imaging (MI) in the development of novel therapies has gained increasing traction in recent years.  ...  Acknowledgements Funding is acknowledged within the context of the Irish National Biophotonics and Imaging Platform and the European Commission Framework Programme 7 AngioTox and AngioPredict initiatives  ... 
doi:10.1016/j.drudis.2013.06.004 pmid:23792334 fatcat:lzpkvjdurrfxxjtskmbtk4epzy

Positron emission tomography imaging of coronary atherosclerosis

Alastair J Moss, Philip D Adamson, David E Newby, Marc R Dweck
2016 Future Cardiology  
Using novel radiotracers targeted at specific cellular pathways, the potential exists to observe inflammation, apoptosis, cellular hypoxia, microcalcification and angiogenesis in vivo.  ...  Several clinical studies are now underway assessing the ability of this hybrid imaging modality to inform about atherosclerotic disease activity and the prediction of future cardiovascular risk.  ...  In addition, improvements in spatial resolution and techniques for correcting cardiac motion will be required if these new tracers are to prove of use in the small and highly mobile coronary arteries.  ... 
doi:10.2217/fca-2016-0017 pmid:27322032 pmcid:PMC4926532 fatcat:d3p7zfgj5zd5dfozzu42tzduum
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