Handbook of Radiopharmaceuticals: Methodology and Applications

Cover
Title Page
Contents
About the Editors
List of Contributors
Foreword
Preface
Abbreviations
Part I Introduction to Radiopharmaceuticals
	Chapter 1 Targeted Diagnostic Radiopharmaceuticals: Design Options for Small-Molecule Radiotracers
		1.1 INTRODUCTION
		1.2 LABEL AN ENDOGENOUS COMPOUND OR DERIVATIVE
		1.3 LABEL A PHARMACEUTICAL OR DERIVATIVE
		1.4 FROM IN VITRO REAGENTS TO IN VIVO IMAGING
		1.5 DO HIGH-THROUGHPUT SCREENING OF A CHEMICAL LIBRARY
		1.6 LABEL A NATURAL PRODUCT OR DERIVATIVE
		1.7 SUMMARY
		REFERENCES
	Chapter 2 Concepts and Issues for Therapeutic Radiopharmaceuticals
		2.1 INTRODUCTION
		2.2 THERANOSTICS
		2.3 EXAMPLES OF RADIOTHERAPEUTICS
		2.4 SUMMARY AND FUTURE OUTLOOK
		REFERENCES
Part II Production of Radionuclides
	Chapter 3 Production of Short Half-Life PET Radionuclides
		3.1 INTRODUCTION
		3.2 PRODUCTION OF COMMONLY USED PET RADIONUCLIDES: 18F, 11C, 13N, 15O, 82Rb, AND 68Ga
		3.3 68Ge/68Ga GENERATORS
		REFERENCES
	Chapter 4 Production of Radionuclides Used in SPECT
		4.1 INTRODUCTION
		4.2 TECHNETIUM-99m
		4.3 IODINE-131
		4.4 XENON-133
		4.5 CYCLOTRON-PRODUCED RADIONUCLIDES
		4.6 THALLIUM-201
		4.7 GALLIUM-67
		4.8 INDIUM-111
		4.9 IODINE-123
		4.A. APPENDIX
		REFERENCES
	Chapter 5 Production of Therapeutic Radionuclides
		5.1 INTRODUCTION
		5.2 NUCLEAR REACTIONS AND ISOTOPE PRODUCTION BASICS
		5.3 REACTOR PRODUCTION OF THERAPEUTIC RADIONUCLIDES
		5.4 PRODUCTION OF THERAPEUTIC RADIONUCLIDES USING CHARGED-PARTICLE REACTIONS
		5.5 PRODUCTION OF THERAPEUTIC RADIONUCLIDES USING PHOTONUCLEAR REACTIONS
		5.6 ADDITIONAL OPPORTUNITIES FOR THERAPEUTIC RADIONUCLIDE PRODUCTION
		5.7 SUMMARY
		REFERENCES
Part III Synthetic Methods for Radiopharmaceuticals
	Chapter 6 Synthesis of 13N- and 15O-Labeled Radiopharmaceuticals
		6.1 NITROGEN-13
		6.2 OXYGEN-15
		6.3 FUTURE PERSPECTIVES
		ACKNOWLEDGMENTS
		REFERENCES
	Chapter 7 Radiochemistry with Carbon-11
		7.1 INTRODUCTION
		7.2 SYNTHESIS OF COMMON CARBON-11 PRECURSORS
		7.3 TECHNOLOGICAL INNOVATIONS IN LABELLING METHODS
		7.4 METHODOLOGY FOR THE INCORPORATION OF CARBON-11 INTO BIOACTIVE MOLECULES
		REFERENCES
	Chapter 8 Fluorine-18 Radiochemistry
		8.1 INTRODUCTION
		8.2 ALIPHATIC FLUORINATION WITH FLUORINE-18
		8.3 CF3 CHEMISTRY
		8.4 OTHER ALIPHATIC C–F BOND FORMATION METHODS
		8.5 AROMATIC FLUORINATION WITH FLUORINE-18
		8.6 OTHER STRATEGIES FOR RADIOLABELING WITH FLUORINE-18
		8.7 RADIOFLUORINATION BEYOND THE C–F BOND
		8.8 CONCLUSIONS AND FUTURE DIRECTIONS
		REFERENCES
	Chapter 9 Labeling with Gallium-68
		9.1 INTRODUCTION
		9.2 ISOTOPE PRODUCTION AND ITS EFFECT ON RADIOLABELING
		9.3 GALLIUM(III) CHEMISTRY AND GALLIUM-68 RADIOCHEMISTRY
		9.4 TRACER DESIGN AND CHELATOR CHOICE
		9.5 PRACTICAL ASPECTS OF GALLIUM-68 RADIOLABELING
		9.6 CLINICAL TRACERS: DEVELOPMENT, RADIOSYNTHESIS, AND APPLICATIONS
		9.7 FUTURE PERSPECTIVES
		ACKNOWLEDGMENTS
		REFERENCES
	Chapter 10 Cu-Mediated Radiohalogenation of Organoboranes
		10.1 INTRODUCTION AND BACKGROUND
		10.2 Cu-MEDIATED RADIOFLUORINATION
		10.3 Cu-MEDIATED HEAVY HALIDE RADIOHALOGENATION
		10.4 CONCLUSIONS
		REFERENCES
	Chapter 11 The Radiochemistry of Zirconium
		11.1 INTRODUCTION
		11.2 HISTORICAL BACKGROUND OF ZIRCONIUM
		11.3 RADIONUCLIDES OF ZIRCONIUM
		11.4 ZIRCONIUM-89 PRODUCTION AND NUCLEAR CHEMISTRY
		11.5 ZIRCONIUM CHEMISTRY AND RADIOCHEMISTRY
		11.6 PRECLINICAL AND CLINICAL REPORTS USING ZIRCONIUM-89-RADIOLABELLED PROTEINS
		11.7 FUTURE DIRECTIONS AND EMERGING TECHNOLOGIES
		ACKNOWLEDGMENTS
		REFERENCES
	Chapter 12 99mTc Radiopharmaceutical Chemistry
		12.1 INTRODUCTION
		12.2 TECHNETIUM-99m CHELATORS AND COMPLEXES
		12.3 MYOCARDIAL IMAGING AGENTS
		12.4 99mTc-FATTY ACIDS DERIVATIVES
		12.5 BRAIN IMAGING AGENTS
		12.6 RENAL IMAGING AGENTS
		12.7 BONE IMAGING AGENTS
		12.8 TUMOR-TARGETED IMAGING AGENTS
		12.9 SENTINEL LYMPH NODE IMAGING AGENTS
		12.10 INFLAMMATION AND INFECTION IMAGING AGENTS
		12.11 99mTc-LABELLED INTERCALATORS FOR THERAPY
		12.12 CONCLUDING REMARKS
		REFERENCES
Part IV Practical Aspects of Radiopharmaceutical Production and Use
	Chapter 13 Automated Synthesis Modules for PET Radiochemistry
		13.1 INTRODUCTION
		13.2 EARLY RADIOCHEMISTRY SYNTHESIS MODULES
		13.3 MODERN CASSETTE-BASED MODULES
		13.4 FULLY AUTOMATED FIXED-TUBING MODULES
		13.5 HYBRID MODULES
		13.6 MICROFLUIDIC SYSTEMS
		13.7 SYNTHESIS MODULES FOR USE WITH SOLID TARGETS
		13.8 AUTOMATED QUALITY CONTROL TESTING
		13.9 CONCLUSIONS AND FUTURE DIRECTIONS
		REFERENCES
	Chapter 14 Automation of PET Radiopharmaceutical Quality Control
		14.1 OVERVIEW
		14.2 PET MILESTONES RELEVANT TO QC AUTOMATION
		14.3 LABORATORY SETUP FOR QC IN PET TRACER PRODUCTION
		14.4 DRIVERS OF AUTOMATED QC
		14.5 BARRIERS TO QC AUTOMATION
		14.6 QC INNOVATION
		14.7 DISCUSSION OF AUTOMATED QC SOLUTIONS
		14.8 CHOOSING AN AUTOMATED QC SYSTEM
		14.9 REGULATORY ASPECTS
		14.10 FUTURE DEVELOPMENTS
		REFERENCES
	Chapter 15 Moving PET Drugs from the Lab to the Patient in the USA
		15.1 INTRODUCTION
		15.2 PET DRUGS BEFORE THE FOOD AND DRUG ADMINISTRATION MODERNIZATION ACT
		15.3 FOOD AND DRUG ADMINISTRATION MODERNIZATION ACT
		15.4 21 CFR 212
		15.5 USP GENERAL CHAPTER <823>
		15.6 IMAGING PATIENTS WITH PET DRUGS
		15.7 IND
		15.8 RDRC
		15.9 NDA
		15.10 ANDA
		15.11 DRUG MASTER FILE (DMF)
		15.12 SUMMARY
		REFERENCES
	Chapter 16 Moving from the Lab to the Patient in Asia
		16.1 INTRODUCTION
		16.2 RADIOPHARMACEUTICALS
		16.3 TECHNICAL TRANSFER
		16.4 TECHNICAL TRANSFER IN ASIA
		16.5 TECHNICAL TRANSFERS IN AND OUT OF ASIA
		16.6 CONCLUSION
		REFERENCES
	Chapter 17 Moving a Radiotracer from Bench to Bedside in Europe
		17.1 INTRODUCTION
		17.2 GENERAL OVERVIEW
		17.3 REGULATORY ENVIRONMENT FOR RADIOPHARMACEUTICALS IN CLINICAL TRIALS
		17.4 EU CLINICAL TRIALS REGISTER and EudraCT DATABASE
		17.5 EANM AND PIC/S GUIDELINES
		17.6 EUROPEAN PHARMACOPOEIA RADIOPHARMACEUTICALS MONOGRAPHS
		REFERENCES
Part IV Major Applications of Radiopharmaceuticals
	Chapter 18 Radiopharmaceuticals in Oncology
		18.1 INTRODUCTION
		18.2 RADIOPHARMACEUTICALS FOR IMAGING CANCER
		18.3 RADIOPHARMACEUTICALS FOR CANCER THERAPY
		18.4 CONCLUSIONS
		ACKNOWLEDGMENTS
		REFERENCES
	Chapter 19 Neurological Applications of Radiopharmaceuticals
		19.1 INTRODUCTION
		19.2 CSF FLOW IMAGING: PLANAR AND SPECT APPLICATIONS
		19.3 CBF IMAGING: PLANAR AND SPECT APPLICATIONS
		19.4 DOPAMINE TRANSPORTER SPECT IMAGING
		19.5 GLUCOSE METABOLIC PET IMAGING
		19.6 β-AMYLOID PET IMAGING
		19.7 FUTURE DIRECTIONS
		19.8 CONCLUSIONS
		ACKNOWLEDGMENTS
		REFERENCES
	Chapter 20 CardiacApplications of Radiopharmaceuticals
		20.1 INTRODUCTION
		20.2 MYOCARDIAL PERFUSION IMAGING (MPI)
		20.3 IMAGING CARDIAC MORPHOLOGY AND FUNCTION
		20.4 IMAGING OF MYOCARDIAL METABOLISM
		20.5 MOLECULAR IMAGING
		20.6 CARDIAC AMYLOIDOSIS
		20.7 CONCLUSION
		REFERENCES
	Chapter 21 Radiopharmaceuticals in Pediatric Nuclear Medicine
		21.1 INTRODUCTION
		21.2 CLINICALLY APPROVED SINGLE-PHOTON PROCEDURES AND RADIOPHARMACEUTICALS
		21.3 ESTABLISHED CLINICAL PET RADIOPHARMACEUTICALS AND THEIR USES
		21.4 RESEARCH RADIOPHARMACEUTICALS AND METHODS
		21.5 SUMMARY
		REFERENCES
	Chapter 22 PET Imaging in Drug Discovery and Development
		22.1 INTRODUCTION
		22.2 THE DRUG DISCOVERY AND DEVELOPMENT PROCESS
		22.3 DESIGN CRITERIA OF A NOVEL PET RADIOLIGAND
		22.4 PET IMAGING AND PET RADIOLIGANDS IN DRUG DISCOVERY AND DEVELOPMENT
		22.5 CONCLUSION
		REFERENCES
Index
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