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Personalized medicine employing patient-based tailor-made therapeutic drugs is taking over treatment paradigms in a variety of ?elds in oncology and the central nervous system. The success of such therapies is mainly dependent on ef?cacious therapeutic drugs and a selective imaging probe for identi?cation of potential responders as well as therapy monitoring for an early bene?t assessment. Molecular imaging (MI) is based on the selective and speci?c interaction of a molecular probe with a biological target which is visualized through nuclear, magnetic resonance, near infrared or other methods. Therefore it is the method of choice for patient selection and therapy monitoring as well as for speci?c e- point monitoring in modern drug development. PET (positron emitting tomography), a nuclear medical imaging modality, is ideally suited to produce three-dimensional images of various targets or processes. The rapidly increasing demand for highly selective probes for MI strongly pushes the development of new PET tracers and PET chemistry. ‘PET chemistry’ can be de?ned as the study of positron-emitting compounds regarding their synthesis, structure, composition, reactivity, nuclear properties and processes and their properties in natural and - natural environments. In practice PET chemistry is strongly in?uenced by the unique properties of the radioisotopes used (e. g. , half-life, che- cal reactivity, etc. ) and integrates scienti?c aspects of nuclear-, organic-, inorganic- and biochemistry.
Marking the 200th National Meeting of the American Chemical Society, The Division of Nuclear Chemistry and Technology hosted a group of about 90 scientists from 15 different countries to discuss the new trends in radiopharmaceutical synthesis, quality assurance and regulatory control. This event took place in Washington, D.C. on August 27-30, 1990. When I first suggested the idea for this symposium, a group of scientists who pioneered the proposed topics offered their help to organize and run such a big task with me. Their names are listed here in appreciation. Thomas E. Boothe Cyclotron Facility, Mt. Sinai Medical Center, Miami Beach, Florida, USA Robert F. Dannals Division of Nuclear Medicine, The Johns Hopkins Medical Institutions, Baltimore, Maryland, USA Anthony L. Feliu Julich Nuclear Research Center, Julich, Germany Joanna S. Fowler Chemistry Department, Brookhaven National Laboratory, Upton, New York, USA George W. Kabalka Department of Chemistry, University of Tennessee, Knoxville, Tennessee, USA Hank F. Kung Department of Radiology, University of Pennsylvania, Philadelphia, Pennsylvania, USA James F. Lamb Imagents, Inc., Houston, Texas, USA Harold A. O'Brien, Jr. Los Alamos National Laboratory, Los Alamos, New Mexico, USA Joseph R. Peterson Dept. of Chemistry, University of Tennessee, Knoxville, Tennessee, USA Hernan Vera Ruiz International Atomic Energy Agency, Vienna, Austria Roy S. Tilbury University of Texas, M. D. Anderson Cancer Center, Houston, Texas, USA In addition, a number of distinguished colleagues have participated in the process of reviewing the manuscripts presented in this volume. Their effort is sincerely acknowledged.
This book is a comprehensive guide to radiopharmaceutical chemistry. The stunning clinical successes of nuclear imaging and targeted radiotherapy have resulted in rapid growth in the field of radiopharmaceutical chemistry, an essential component of nuclear medicine and radiology. However, at this point, interest in the field outpaces the academic and educational infrastructure needed to train radiopharmaceutical chemists. For example, the vast majority of texts that address radiopharmaceutical chemistry do so only peripherally, focusing instead on nuclear chemistry (i.e. nuclear reactions in reactors), heavy element radiochemistry (i.e. the decomposition of radioactive waste), or solely on the clinical applications of radiopharmaceuticals (e.g. the use of PET tracers in oncology). This text fills that gap by focusing on the chemistry of radiopharmaceuticals, with key coverage of how that knowledge translates to the development of diagnostic and therapeutic radiopharmaceuticals for the clinic. The text is divided into three overarching sections: First Principles, Radiochemistry, and Special Topics. The first is a general overview covering fundamental and broad issues like “The Production of Radionuclides” and “Basics of Radiochemistry”. The second section is the main focus of the book. In this section, each chapter’s author will delve much deeper into the subject matter, covering both well established and state-of-the-art techniques in radiopharmaceutical chemistry. This section will be divided according to radionuclide and will include chapters on radiolabeling methods using all of the common nuclides employed in radiopharmaceuticals, including four chapters on the ubiquitously used fluorine-18 and a “Best of the Rest” chapter to cover emerging radionuclides. Finally, the third section of the book is dedicated to special topics with important information for radiochemists, including “Bioconjugation Methods,” “Click Chemistry in Radiochemistry”, and “Radiochemical Instrumentation.” This is an ideal educational guide for nuclear medicine physicians, radiologists, and radiopharmaceutical chemists, as well as residents and trainees in all of these areas.
Radioisotope-based molecular imaging probes provide unprecedented insight into biochemistry and function involved in both normal and disease states of living systems, with unbiased in vivo measurement of regional radiotracer activities offering very high specificity and sensitivity. No other molecular imaging technology including functional magnetic resonance imaging (fMRI) can provide such high sensitivity and specificity at a tracer level. The applications of this technology can be very broad ranging from drug development, pharmacokinetics, clinical investigations, and finally to routine diagnostics in radiology. The design and the development of radiopharmaceuticals for molecular imaging studies using PET/MicroPET or SPECT/MicroSPECT are a unique challenge. This book is intended for a broad audience and written with the main purpose of educating the reader on various aspects including potential clinical utility, limitations of drug development, and regulatory compliance and approvals.
This book explores the close connection between immunology and nuclear medicine, which has led to radioimmunoimaging and radioimmunotherapy (RIT). Molecular imaging with positron emission tomography (PET) and single-photon emission computed tomography (SPECT) is increasingly being used to diagnose, characterize, and monitor disease activity in the context of inflammatory disorders of known and unknown etiology, such as sarcoidosis, atherosclerosis, vasculitis, inflammatory bowel disease, rheumatoid arthritis, and degenerative joint disease. The first chapters discuss the various radiopharmaceutical agents and radiolabeled preparations that have been employed in inflammation imaging. Of these, FDG-PET imaging has been shown to have the great value in the detection of inflammation and has become the centerpiece of several initiatives over the last several years. This very powerful technique will play an increasingly important role in the management of patients with inflammatory conditions in the future. The book also explores the growing role of nuclear medicine and molecular imaging in the diagnosis and treatment of cancer. The rapid pace of change has been fueled by advances in our understanding of tumor biology, on the one hand, and the development of specifically targeted medical therapies, diagnostic agents, and radiotherapies, on the other. Written by leading international experts in the field, this book is an invaluable tool for nuclear medicine physicians, radiologists, oncologists, and immunologists.
The recent revolution in molecular biology offers exciting new opportunities for targeted radionuclide therapy. This up-to-date, comprehensive book, written by world-renowned experts, discusses the basic principles of radionuclide therapy, explores in detail the available treatments, explains the regulatory requirements, and examines likely future developments. The full range of clinical applications is considered, including thyroid cancer, hematological malignancies, brain tumors, liver cancer, bone and joint disease, and neuroendocrine tumors. The combination of theoretical background and practical information will provide the reader with all the knowledge required to administer radionuclide therapy safely and effectively in the individual patient. Careful attention is also paid to the role of the therapeutic nuclear physician in coordinating a diverse multidisciplinary team, which is central to the safe provision of treatment.