Advancing Nuclear Medicine Through Innovation (2007) / Chapter Skim
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6 Radiotracer and Radiopharmaceutical Chemistry
6 Radiotracer and Radiopharmaceutical Chemistry
Pages 89-103
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From page 89... ...
. The content of this chapter, particularly the sections delineating needs and impediments, is derived largely from discussions with and presentations from chemists and other researchers working in the nuclear medicine field.
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From page 90... ...
6.2 SIGNIFICANT DISCOVERIES Government investments in chemistry have facilitated the advancement of nuclear medicine, molecular imaging,1 and targeted radionuclide therapy. For example, research in nuclear chemistry and radiochemistry (Sidebar 6.1)
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From page 91... ...
Of particular relevance to radiopharmaceutical chemistry is bioinorganic chemistry, which includes coordination chemistry and the incorporation of radio metals into targeted radiopharmaceuticals. Radiopharmaceutical chemistry designs, synthesizes, and evaluates chemi cal compounds that are labeled with a radionuclide.
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From page 92... ...
. Targeted Radionuclide Therapy Targeted radionuclide therapy (see Sidebar 2.3)
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From page 93... ...
Cancer Biology and Targeted Radionuclide Therapy. Greater understanding of the abnormal biology of tumor cells will allow cancer treatments to be developed that target these features (rather than non-specifically targeting rapidly dividing cells, which is the approach of most chemotherapeutics)
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A and B, a nicotine binding site (green) , and brain glucose metabolism along with radiotracer structures and human brain images corresponding to 6-2 each of these molecular targets.
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From page 95... ...
PET tracers have also provided additional gains in accurately diagnosing coronary artery disease, reducing the need for invasive diagnostic procedures, such as coronary angiography. One research priority in cardiology includes identifying techniques for characterizing the functional and biological processes associated with structural alterations in the vessel wall that play a central role in the development of coronary artery disease.
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From page 96... ...
6.3.2 Specific Technologies and Methods The demand for new radiopharmaceuticals from many medical specialties particularly oncology, cardiology, neurology, and psychiatry, and especially the pharmaceutical industry, has placed a sense of urgency on stimulating the flow of new ideas and accelerating the pace of development. Currently, chemists working in the areas of molecular imaging and targeted radionuclide therapy are focused on designing and synthesizing radiopharmaceuticals with the required bioavailability and specificity to act as true tracers targeting specific cellular elements (e.g., receptors, enzymes, transporters, antigens, etc.)
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From page 97... ...
In addition to performing research directed toward radiotracer synthesis, chemists also design radiotracers and investigate the mechanisms underlying the distribution and kinetics of labeled compounds in living systems. This type of work addresses a major obstacle in radiotracer R&D -- namely, the lack of knowledge for predicting which radiolabeled compounds will have the bioavailability, specificity, and kinetics required to image and quantify specific molecular targets in vivo or to target tumor tissue while sparing healthy organs.
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From page 98... ...
; • To retain the desired targeting properties of the parent compound after labeling; • To develop smaller, less polar,b kinetically stable radiometal ligand com plexes that are readily available; • To develop processing and purification methods to reliably produce high specific-activity radionuclides; • To synthesize more probes with higher affinity for targeting and capture, and smaller capture agents bearing the radionuclide that attach to the carrier for pre-targeting; • To advance radiopharmaceutical applications of the germanium-68/gallium 68 generator to take advantage of the availability of this generator and PET; and • To develop methods to produce clinical and commercial quantities of thera peutic radionuclides and to increase the availability of radionuclides approved by the Food and Drug Administration. aChelation is a chemical process whereby a chelating agent binds to a metal ion, forming a metal complex known as a chelate.
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From page 99... ...
Although there is a need to develop new radiopharmaceuticals for new molecular targets, it is important to note that there are many highly promising radionuclides, precursor molecules, and radiopharmaceuticals that are not readily available to institutions without an infrastructure for isotope production or radiopharmaceutical chemistry. These include fluorine-18fluoro-L-dihydroxyphenylalanine (FDOPA)
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From page 100... ...
00 ADVANCING NUCLEAR MEDICINE THROUGH INNOVATION FIGURE 6.3 Integrated microfluidics for the synthesis of FDG.
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From page 101... ...
has seen a substantial loss of support for basic radiopharmaceutical chemistry research. This includes methodological research in synthetic chemistry, yield optimization, purification strategies, structure-activity relationships, radionuclide and targetry research, and preclinical and clinical evaluation.
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From page 102... ...
Given the somewhat different orientations of the DOE and the National Institutes of Health (NIH) toward nuclear medicine research, the two agencies should find some cooperative mechanism to support radionuclide production and distribution; basic research in radionuclide production, nuclear imaging, radiopharmaceutical/radiotracer and therapy development; and the transfer of these technologies into routine clinical use.
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From page 103... ...
0 RADIOTRACER AND RADIOPHARMACEUTICAL CHEMISTRY RECOMMENDATION 2: Encourage interdisciplinary collaboration. DOE-OBER should support collaborations between basic chemistry and physics laboratories, as well as multi-disciplinary centers focused on nuclear medicine technology development and application, to stimulate the flow of new ideas for the development of next-generation radiopharmaceuticals and imaging instrumentation.
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