Radiopharmaceutical Chemistry Between Imaging And Endoradiotherapy

This book is a printed edition of the Special Issue "Radiopharmaceutical Chemistry between Imaging and Radioendotherapy" that was published in Pharmaceuticals

Annotation 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.

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.

A comprehensive, authoritative and up-to-date reference for the newcomer to radiopharmaceuticals and those already in the field. Radiopharmaceuticals are used to detect and characterise disease processes, or normal biological function, in living cells, animals or humans. Used as tracer molecules, they map the distribution, uptake and metabolism of the molecule in clinical studies, basic research or applied research. The area of radiopharmaceuticals is expanding rapidly. The number of PET centers in the world is increasing at 20% per year, and many drug companies are utilising PET and other forms of radiopharmaceutical imaging to evaluate products. * Readers will find coverage on a number of important topics such as radionuclide production, PET and drug development, and regulations * Explains how to use radiopharmaceuticals for the diagnosis and therapy of cancer and other diseases * The editors and a majority of the contributors are from the United States

The thoroughly updated new edition of the authoritative reference in Radiopharmaceutical Sciences The second edition of Handbook of Radiopharmaceuticals is a comprehensive review of the field, presenting up-to-date coverage of central topics such as radionuclide production, synthetic methodology, radiopharmaceutical development and regulations, and a wide range of practical applications. A valuable reference work for those new to the Radiopharmaceutical Sciences and experienced professionals alike, this volume explores the latest concepts and issues involving both targeted diagnostic and therapeutic radiopharmaceuticals. Contributions from a team of experts from across sub-disciplines provide readers with an immersive examination of radiochemistry, nuclear medicine, molecular imaging, and more. Since the first edition of the Handbook was published, Nuclear Medicine and Radiopharmaceutical Sciences have undergone major changes. New radiopharmaceuticals for diagnosis and therapy have been approved by the FDA, the number of clinical PET and SPECT scans have increased significantly, and advances in Artificial Intelligence have dramatically improved research techniques. This fully revised edition reflects the current state of the field and features substantially updated and expanded content. New chapters cover topics including current Good Manufacturing Practice (cGMP), regulatory oversight, novel approaches to quality control—ensuring that readers are informed of the exciting developments of recent years. This important resource: Features extensive new and revised content throughout Covers key areas of application for diagnosis and therapy in oncology, neurology, and cardiology Emphasizes the multidisciplinary nature of Radiopharmaceutical Sciences Discusses how drug companies are using modern radiopharmaceutical imaging techniques to support drug discovery Examines current and emerging applications of Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) Edited by recognized experts in radiochemistry and PET imaging, Handbook of Radiopharmaceuticals: Radiochemistry and Applications, 2 nd Edition is an indispensable reference for post-doctoral fellows, research scientists, and professionals in the pharmaceutical industry, and for academics, graduate students, and newcomers in the field of radiopharmaceuticals.

To continue the support for the growing trend of chemistry involvement in nuclear medicine, the Division of Nuclear Chemistry and Technology (DNCT) of the American Chemical Society (ACS) planned for a symposium to cover this aspect. This was expressed in arequest to me, as a member of the Program Committee, to organize a symposium on topics related to nuclear and radiochemistry applications to nuclear medicine. Realizing the growing interest in imaging, specially with positron emitting radioisotopes, I invited several colleagues to study with me the idea of imaging centers and the involvement of chemists in their structure and function. The formulated Organizing Committee supported this idea which evolved in proposing an extended international symposium to be held in conjunction with the 206th ACS National meeting in Chicago, Illinois, U. S. A. on August 22-27, 1993. The following are the members of the Organizing Committee: Jorge R. Barrio, Ph. D. Thomas E. Boothe, Ph. D. J. Robert Dahl, Ph. D. Robert F. Dannals, Ph. D. Bruce R. Erdal, Ph. D. Mark M. Goodman, Ph. D. George W. Kabalka, Ph. D. James F. Lamb, Ph. D. Ronald G. Manning, Ph. D. Henry C. Padgett, Ph. D. Roy S. Tilbury, Ph. D. Steven W. Yates, Ph. D. and Ali M. Emran, Ph. D.

One Radiobiopharmaceutics.- 1 Preparation of radiopharmaceuticals.- Production of radionuclides.- Synthesis of the non-radioactive compound.- Reaction of the radionuclide with the non-radioactive compound.- References.- 2 Ideal characteristics of radiopharmaceuticals.- Availability and cost.- Preparation.- Biologic behavior.- Radionuclidic characteristics.- Hematology.- 3 Quality control of radiopharmaceuticals.- Biologic tests.- Physicochemical tests.- References.- 4 Design of radiopharmaceuticals.- Radionuclide.- Chemistry.- Biology.- Human studies.- Registration.- References.- 5 The fate of.

A new edition of a book is warranted when the book is successful and there are many new developments in the related discipline. Both have occurred for this book during the past 7 years since its second edition. The growth and development in nuclear pharmacy and radiopharmaceutical chemistry along with the continued success of the book have convinced us to update the book; hence this third edition. This book is a ramification of my nuclear pharmacy courses offered to pharmacy students specializing in nuclear pharmacy, nuclear medicine resi dents, and nuclear medicine technology students. The book is written in an integrated form from the basic concept of atomic structure to the practical clinical uses of radiopharmaceuticals. It serves both as a textbook on nu clear pharmacy for pharmacy students and nuclear medicine technologists, and as a useful reference book for many professionals related to nuclear medicine, such as nuclear medicine physicians and radiologists. The book contains 12 chapters. Each chapter is written as comprehen sively as possible based on my personal experience and understanding. At the end of each chapter, a section of pertinent questions and problems and so me suggested reading materials are included. I have made justifiably many additions and deletions as weIl as some reorganization in this edition. Chapter 3 is entirely dedicated to instru ments for radiation detection and measurement, including brief description of gas detectors, gamma-detecting instruments, and tomographic scanners.