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Radiochemistry AND FDA

Krishan Kumar, Arijit Ghosh
The clinical applications of positron emission tomography (PET) imaging pharmaceuticals have increased tremendously over the past several years since the approval of 18 fluorine-fluorodeoxyglucose (18 F-FDG) by the Food and Drug Administration (FDA). Numerous 18 F-labeled target-specific potential imaging pharmaceuticals, based on small and large molecules, have been evaluated in preclinical and clinical settings. 18 F-labeling of organic moieties involves the introduction of the radioisotope by C-18 F bond formation via a nucleophilic or an electrophilic substitution reaction...
April 18, 2018: Bioconjugate Chemistry
Alessandra Cavaliere, Katrin C Probst, Andrew D Westwell, Magdalena Slusarczyk
Fluorine-containing nucleoside analogs (NAs) represent a significant class of the US FDA-approved chemotherapeutics widely used in the clinic. The incorporation of fluorine into drug-like agents modulates lipophilic, electronic and steric parameters, thus influencing pharmacodynamic and pharmacokinetic properties of drugs. Fluorine can block oxidative metabolism of drugs and the formation of undesired metabolites by changing H-bonding interactions. In this review, we focus our attention on chemical fluorination reagents and methods used in the NAs field, including positron emission tomography radiochemistry...
October 2017: Future Medicinal Chemistry
Sergio Dall'Angelo, Nouchali Bandaranayaka, Albert D Windhorst, Danielle J Vugts, Dion van der Born, Mayca Onega, Lutz F Schweiger, Matteo Zanda, David O'Hagan
INTRODUCTION: 5-[(18)F]Fluoro-5-deoxyribose ([(18)F]FDR) 3 was prepared as a novel monosaccharide radiotracer in a two-step synthesis using the fluorinase, a C-F bond forming enzyme, and a nucleoside hydrolase. The resulting [(18)F]FDR 3 was then explored as a radiotracer for imaging tumours (A431 human epithelial carcinoma) by positron emission tomography in a mice model. METHODS: 5-[(18)F]Fluoro-5-deoxyribose ([(18)F]FDR) 3, was prepared by incubating S-adenosyl-L-methionine (SAM) and [(18)F]fluoride with the fluorinase enzyme, and then incubating the product of this reaction, [(18)F]-5'-fluoro-5'-deoxadenosine ([(18)F]FDA) 2, with an adenosine hydrolase to generate [(18)F]FDR 3...
May 2013: Nuclear Medicine and Biology
Olli Eskola, Tove J Grönroos, Alexandru Naum, Päivi Marjamäki, Sarita Forsback, Jörgen Bergman, Sami Länkimäki, Jan Kiss, Timo Savunen, Juhani Knuuti, Merja Haaparanta, Olof Solin
PURPOSE: 6-[(18)F]Fluorodopamine (4-(2-aminoethyl)-5-[(18)F]fluorobenzene-1,2-diol, 6-[(18)F]FDA) is a tracer for imaging sympathetically innervated tissues. Previous electrophilic labelling methods produced 6-[(18)F]FDA with low specific radioactivity (SA) which has limited its wider use. Our aim was to employ electrophilic labelling and increase the SA to around 15 GBq/μmol. We also sought to determine an extensive biodistribution pattern for 6-[(18)F]FDA in rats in order to thoroughly identify tissues with dense sympathetic innervation that were specifically labelled with 6-[(18)F]FDA...
May 2012: European Journal of Nuclear Medicine and Molecular Imaging
Shankar Vallabhajosula, Anastasia Nikolopoulou
As an analogue of adrenergic neurotransmitter norepinephrine (NE), metaiodobenzylguanidine (MIBG) demonstrates high uptake both in normal sympathetically innervated tissues, such as the heart and salivary glands, and in tumors that express the NE transporter (NET), specifically those of neural crest and neuroendocrine origin. In 1994, (131)I-MIBG, also known as iobenguane I-131 intravenous, received Food and Drug Administration (FDA) approval as an imaging agent. In 2008, (123)I-MIBG was also approved by FDA as a tumor imaging agent...
September 2011: Seminars in Nuclear Medicine
M D Prager, R P Quintana
Employing an artificial tear preparation composed of six proteins and six lipids as a deposit model, uptake of the lipids 3H-cholesteryl oleate and 14C-dioleoyl phosphatidylcholine was measured on contact lenses representative of the four FDA hydrogel groups and on select RGP lenses. Cholesteryl oleate uptake after 24 h at 37 degrees C generally was less than 1 microgram/lens although occasionally reaching 1-2 micrograms. DuraSoft 3 lenses (Group IV) accumulated the deposits in greater amounts (p = 0.04) with other lens groups not differing significantly from each other...
November 1997: Journal of Biomedical Materials Research
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