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Journal of Labelled Compounds & Radiopharmaceuticals

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https://read.qxmd.com/read/30741441/clinical-translation-of-theranostic-radiopharmaceuticals-current-regulatory-status-and-recent-examples
#1
Petra Kolenc Peitl, Christine Rangger, Piotr Garnuszek, Renata Mikolajczak, Alicja Hubalewska-Dydejczyk, Theodosia Maina, Paola Erba, Clemens Decristoforo
With the development of ever more radiopharmaceuticals suitable for theranostic applications, translation of novel compounds from the preclinical stage towards clinical application becomes a bottleneck for the advances in Nuclear Medicine. This review article summarizes the current regulatory framework for clinical trials with radiopharmaceuticals in the European Union, provides a general overview of the documentation required and addresses quality, safety and clinical aspects to be considered. By using a recent successful example of translating a theranostic peptide radioligand, namely 111 In-CP04, which targets receptors expressed in medullary thyroid carcinoma, the pathway from the preclinical development over establishing the required pharmaceutical documentation to designing and submitting a clinical trial is reviewed...
February 11, 2019: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/30690759/a-simple-and-efficient-automated-cgmp-compliant-radiosynthesis-of-11-c-metomidate-using-solid-phase-extraction-cartridge-purification
#2
Mitja Kovac, Tunde Miclovitz, Lei Li, Joseph Russell, Roberto Eduardo Canales Candela, Franklin I Aigbirhio, Istvan Boros
[11 C]metomidate ([11 C]MTO) is a radiotracer widely used to detect disorders of adrenocortical origin by positron emission tomography (PET) imaging. [11 C]MTO PET/computed tomography (PET/CT) is considered a sensitive and specific noninvasive alternative to adrenal vein sampling (AVS) in the management of primary hyperaldosteronism (PHA). Herein, we report a reliable automated procedure for the routine manufacturing of [11 C]MTO in current good manufacturing practice (cGMP) conditions on the commercial Synthra MeIPlus Loop Vessel synthesizer...
January 28, 2019: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/30672007/automated-production-of-68-ga-ga-dotanoc-and-68-ga-ga-psma-11-using-a-tracerlab-fx-fn-synthesis-module
#3
Segundo Francisco Garcia-Arguello, Beatriz Lopez-Lorenzo, Rafael Ruiz-Cruces
The interest in gallium-68 labelled PET probes continues to increase around the world. However, one of the barriers for routine clinical use is the cost of the automated synthesis units for relatively simple labelling procedures. Herein, we describe the adaptation of a TRACERlab FXFN synthesis module for the automated production of gallium-68 radiopharmaceuticals using a cation-exchange cartridge for postprocessing of the 68 Ge/68 Ga generator eluate. The recovery of activity from the cartridge was 95.6-98...
January 22, 2019: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/30663099/new-99m-tc-co-3-radiolabeld-arylpiperazine-pharmacophore-as-potent-5-ht-1a-serotonin-receptor-radiotracer-docking-studies-chemical-synthesis-radiolabeling-and-biological-evaluation
#4
Mostafa Erfani, Hadi Malek, Seyed Esmaeil Sadat Ebrahimi, Leila Hassanzadeh
In spite of previous efforts there is lack of a radiotracer for imaging the 5HT1A receptor density in human brain which is involved in several neurological brain disorders. The aim of this study was to prepare a new derivative of 1-(2-methoxyphenyl) piperazine (MPP) as a main chemical structure of 5HT1A receptor antagonist with 3-carbons linker and radio-labeled by [99m Tc][Tc (CO)3 (H2 O)3 ]+ precursor. Docking studies before chemical synthesis, showed similar fashion of interaction for both WAY100635 (potent 5HT1A receptor antagonist) and new designed ligand, despite of addition of 99m Tc-(CO)3 group in the structure of new ligand...
January 20, 2019: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/30663098/ce-141-labeled-dotmp-a-theranostic-option-in-management-of-pain-due-to-skeletal-metastases
#5
K V Vimalnath, A Rajeswari, H D Sarma, Ashutosh Dash, Sudipta Chakraborty
Owing to its favorable radioactive decay characteristics [T1/2 = 32.51 d, Eβ (max) = 434.6 keV (70.5%) and 580.0 keV (29.5%), Eγ = 145.4 keV (48.5%)], 141 Ce could be envisaged as a theranostic radionuclide for use in nuclear medicine. The present article reports synthesis and evaluation of 141 Ce-complex of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetramethylenephosphonic acid (DOTMP) as a potent theranostic agent targeting metastatic skeletal lesions. Ce-141 was produced with 314 ± 29 MBq/mg (n = 6) specific activity and >99...
January 20, 2019: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/30663095/preparation-of-177-lu-labeled-nimotuzumab-for-radioimmunotherapy-of-egfr-positive-cancers-comparison-of-dota-and-chx-a-dtpa-as-bifunctional-chelators
#6
Usha Pandey, Mythili Kameswaran, Naresh Gamre, Ashutosh Dash
OBJECTIVE: This study was aimed at evaluating the role of bifunctional chelators DOTA-NCS and CHX-A"-DTPA-NCS used for conjugating 177 Lu with Nimotuzumab on the radiochemical yields, purity, in vitro stability and specificity of the radioimmunoconjugates to EGFR. METHODS: Two immunoconjugates were prepared wherein Nimotuzumab was conjugated with the acyclic ligand p-NCS-Bn-CHX-A"-DTPA and macrocyclic ligand p-NCS-Bn-DOTA. These were radiolabeled with 177 Lu, purified on PD-10 column and characterized by SE-HPLC...
January 20, 2019: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/30663092/access-to-18-f-labelled-isoxazoles-by-ruthenium-promoted-1-3-dipolar-cycloaddition-of-4-18-f-fluoro-n-hydroxybenzimidoyl-chloride-with-alkynes
#7
Silvia Roscales, Torsten Kniess
4-[18 F]Fluoro-N-hydroxybenzimidoyl chloride (18 FBIC) an 18 F-labelled aromatic nitrile oxide was developed as building block for Ru-promoted 1,3-dipolar cycloaddition with alkynes. 18 FBIC is obtained in a one-pot synthesis in up to 84% radiochemical yield starting from [18 F]fluoride with 4-[18 F]fluorobenzaldehyde (18 FBA) and 4-[18 F]fluorobenzaldehyde oxime (18 FBAO) as intermediates, by reaction of 18 FBAO with N-chlorosuccinimide (NCS). 18 FBIC was found to be a suitable and stable synthon to give access to 18 F-labelled 3,4-diarylsubstituted isoxazoles by [Cp*RuCl (cod)]-catalyzed 1,3-dipolar cycloaddition with various alkynes...
January 20, 2019: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/30644121/an-azeotropic-drying-free-approach-for-copper-mediated-radiofluorination-without-addition-of-base
#8
Xiang Zhang, Falguni Basuli, Rolf E Swenson
Copper-mediated radiofluorination provides a quick and versatile approach for 18 F-labeling of arenes and heteroarenes. However, this method is known to be base-sensitive which has been a barrier for preparative scale radiosynthesis. In this report, we provide an approach for copper-mediated radiofluorination without azeotropic drying or adding a base. [18 F]Fluoride trapped on a PS-HCO3 Sep-Pak was quantitatively eluted with a solution of 4-dimethylaminopyridinium trifluoromethanesulfonate (DMAP·OTf) in anhydrous N,N-dimethylformamide (DMF)...
January 15, 2019: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/30604432/efficient-gallium-68-radiolabeling-reaction-of-dota-derivatives-using-a-resonant-type-microwave-reactor
#9
Yusuke Yagi, Yoichi Shimizu, Kenji Arimitsu, Yuji Nakamoto, Takahiro Higuchi, Kaori Togashi, Hiroyuki Kimura
Gallium-68 (68 Ga, t1/2 = 68 min) can be easily obtained from a 68 Ge/68 Ga generator and several such systems are commercially available. The use of positron emission tomography (PET) imaging using 68 Ga-labeled radiopharmaceuticals is expected to increase in both preclinical and clinical settings. However, the chelation between a 68 Ga cation and the bifunctional macrocyclic chelates that are used for labeling bioactive substances, such as 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA), requires a relatively long reaction time and high temperature to achieve a high radiochemical yield...
January 2, 2019: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/30592529/synthesis-of-15-n-4-purine-labelled-cytokinin-glycosides-derived-from-zeatins-and-topolins-with-9-%C3%AE-d-7-%C3%AE-d-glucopyranosyl-or-9-%C3%AE-d-ribofuranosyl-group
#10
Lenka Tranová, Jan Buček, Marek Zatloukal, Petr Cankař, Jakub Stýskala
Synthesis of [15 N4 ] purine labelled cytokinine glycosides derived from zeatins and topolins containing a 9-β-D, 7-β-D-glucopyranosyl, or 9-β-D-ribofuranosyl group is described. These N6 -substituted adenine derivatives are intended as internal analytic standards for phytohormone analysis. All labelled compounds were prepared from 6-chloro[15 N4 ] purine (1). The equilibrium reaction of 1 with acetobromo-α-D-glucose gave isomeric 7-β-D (3) and 9-β-D (4) chloro glucosyl precursors, which were treated with the corresponding amines to get desired labelled cytokinin 7-β-D (6) and 9-β-D (5) glucopyranosides...
December 28, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/30589452/total-synthesis-of-13-c-2-15-n-imidacloprid-with-three-stable-isotopes-in-the-pyridine-ring
#11
Vladimir Belov, Heiko U Käfferlein
Imidacloprid (IC) is one of the most important crop-protecting insecticides worldwide and commonly used for seed treatment. However, only few data is available on human toxicity of IC. Having in view the metabolic studies at low doses in humans and residue analysis of IC in food and consumer products, we elaborated the synthesis and prepared 13 C2 ,15 N-IC with three stable isotopes of the "heavy" atoms in positions 1, 2 and 3 of the pyridine ring. By using readily available and affordable starting materials, 15 NH4 Cl and 13 C4 -acetic anhydride, the target compound has been prepared in eight steps with an overall yield of 13%...
December 27, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/30556584/-18-f-fpyzide-a-versatile-prosthetic-reagent-for-the-fluorine-18-radiolabeling-of-biologics-via-copper-catalyzed-or-strain-promoted-alkyne-azide-cycloadditions
#12
Mélanie Roche, Simon Specklin, Mylène Richard, Françoise Hinnen, Kevin Génermont, Bertrand Kuhnast
Methods for the radiolabeling of biologics with fluorine-18 have been of interest for several decades. A common approach consists in the preparation of a prosthetic reagent, a small molecule bearing a fluorine-18 that is conjugated with the macromolecule to an appropriate function. Click chemistry, and more particularly cycloadditions, are an interesting approach to radiolabel molecules thanks to mild reaction conditions, high yields, low by-products formation and strong orthogonality. Moreover, the chemical functions involved in the cycloaddition reaction are stable in the drastic radiofluorination conditions, thus allowing a simple radiosynthetic route to prepare the prosthetic reagent...
December 17, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/30556149/synthesis-of-11-c-labeled-ubiquinone-and-ubiquinol-via-pd-0-mediated-rapid-c-11-c-methylation-using-11-c-methyl-iodide-and-39-demethyl-39-pinacolboryl-ubiquinone
#13
Miki Goto, Akira Nishiyama, Takao Yamaguchi, Kyosuke Watanabe, Kenji Fujii, Yasuyoshi Watanabe, Hisashi Doi
To enable positron emission tomography (PET) imaging of the in-vivo kinetics of ubiquinone and ubiquinol, which is referred to as coenzyme Q10 , their 11 C-radiolabeled counterparts were synthesized herein. 11 C-Labeled ubiquinone [11 C]-1 was realized by Pd-mediated rapid C-[11 C] methylation of [11 C]CH3 I with 39-demethyl-39-(pinacolboryl) ubiquinone, prepared by Ru-catalyzed olefin metathesis of unradiolabeled ubiquinone with 2-(pinacolboryl)propene. Subsequent reduction of [11 C]-1 using Na2 S2 O4 yielded 11 C-labeled ubiquinol [11 C]-2...
December 16, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/30537260/a-versatile-synthetic-route-to-the-preparation-of-15-n-heterocycles
#14
Nikita V Chukanov, Bryce M Kidd, Larisa M Kovtunova, Valerii I Bukhtiyarov, Roman V Shchepin, Eduard Y Chekmenev, Boyd M Goodson, Kirill V Kovtunov, Igor V Koptyug
A robust medium-scale (~3 g) synthetic method for 15 N labeling of pyridine (15 N-Py) is reported based on the Zincke reaction. 15 N enrichment in excess of 81% was achieved with ~33% yield. 15 N-Py serves as a standard substrate in a wide range of studies employing a hyperpolarization technique for efficient polarization transfer from parahydrogen to heteronuclei; this technique, called SABRE (Signal Amplification by Reversible Exchange), employs a simultaneous chemical exchange of parahydrogen and to-be-hyperpolarized substrate (e...
December 11, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/30548247/synthesis-of-13-c-labelled-sulfated-n-acetyl-d-lactosamines-to-aid-in-the-diagnosis-of-mucopolysaccharidosis-diseases
#15
Scott A Cameron, Olga V Zubkova, Steven Toms, Richard H Furneaux, Phillip M Rendle
Morquio A syndrome is an autosomal mucopolysaccharide storage disorder that leads to accumulation of keratan sulfate. Diagnosis of this disease can be aided by measuring the levels of keratan sulfate in the urine. This requires the liquid chromatography tandem mass spectrometry (LCMS/MS) measurement of sulfated N-acetyl-d-lactosamines in the urine after cleavage of the keratan sulfate with keratanase II. Quantification requires isotopically-labelled internal standards. The synthesis of these 13 C6 -labelled standards from 13 C6 -galactose and N-acetylglucosamine is described...
November 22, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/30466143/synthesis-of-highly-potent-lymphocyte-function-associated-antigen-1-antagonists-labeled-with-carbon-14-and-with-stable-isotopes-part-3
#16
Bachir Latli, Matt Hrapchak, Guisheng Li, Jon Lorenz, Josh Horan, Carl A Busacca, Chris H Senanayake
The drug candidates (2) and (3) are highly potent LFA-1 inhibitors. They were efficiently prepared labeled with carbon-14 using a palladium-catalyzed carboxylation of an iodo-precursor (5) and sodium formate-14 C to afford acid [14 C]-(6), which was coupled via an amide bond to chiral amines (7) and (8) in 52% and 48% overall yield respectively and with specific activities higher than 56 mCi/mmol and radiochemical purities of 99%. For stable isotopes synthesis, the amine [2 H8 ]-(7) was synthesized in three steps from 2-cyanopyridine-2 H4 using Kulinkovich-Szymonik aminocyclopropanation, followed by coupling to L-alanine-2,3,3,3-2 H4 -N-t-BOC, and then removal of the BOC-protecting group...
November 22, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/30428130/an-efficient-method-for-synthesizing-dimethylsulfonio-34-s-propionate-hydrochloride-from-34-s-8
#17
Joseph S Wirth, William B Whitman
Dimethylsulfoniopropionate (DMSP, (2-carboxyethyl)dimethylsulfonium) is a highly abundant compound in marine environments. As a precursor to the climatically active gas, dimethylsulfide (DMS), DMSP connects the marine and terrestrial sulfur cycles. However, the fate of DMSP in microbial biomass is not well understood as only a few studies have performed isotopic labeling experiments. A previously published method synthesized 34 S-labeled DMSP from 34 S8 , but the efficiency was only 26 % and required five separate reactions, expensive reagents, and purification of the products of each reaction...
November 14, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/30426535/radiolabeling-quality-control-biodistribution-and-imaging-studies-of-177-lu-ibandronate
#18
Qin Xu, Shumao Zhang, Yan Zhao, Yue Feng, Lin Liu, Liang Cai, Wei Zhang, Zhanwen Huang, Hongyuan Wei, Liangang Zhuo, Yue Chen
The purposes of this study were as follows: (1) to radiolabel ibandronic acid (IBA, a third-generation bisphosphonate) with 177 Lu, investigating optimal labeling conditions, and (2) to analyze biodistribution and imaging properties of intravenous 177 Lu-ibandronate (177 Lu-IBA) administered in animals. 177 Lu-labeled methylene diphosphonate (177 Lu-MDP) served as a comparator agent. Differing proportions of IBA solution and 177 LuCl3 solution were combined to determine an optimal ratio for radiolabeling purposes, varying pH, temperature, and time to establish ideal reactivity conditions...
November 13, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/30426529/a-simplified-radiosynthesis-of-18-f-mk-6240-for-tau-pet-imaging
#19
Robert Hopewell, Karen Ross, Alexey Kostikov, Tharick A Pascoal, Thais Alberti, Monica Lacatus-Samoila, Jean-Paul Soucy, Idriss Bennacef, Eliane Kobayashi, Min Su Kang, Pedro Rosa-Neto, Gassan Massarweh
[18 F]MK-6240 (6-(fluoro)-3-(1H-pyrrolo[2,3-c]pyridin-1-yl)isoquinolin-5-amine) is a highly selective PET radiotracer for the in vivo imaging of neurofibrillary tangles (NFTs). [18 F]MK-6240 was synthesized in one step from its bis-Boc protected precursor N-[(tert-butoxy)carbonyl]-N-(6-nitro-3-[1H-pyrrolo[2,3-c]pyridin-1-yl]isoquinolin-5-yl) carbamate in DMSO using [18 F] fluoride with TEA HCO3 with step-wise heating up to 150°C, resulting in an isolated radiochemical yield of 9.8% ± 1.8% (n = 3) calculated from the end of bombardment (5...
November 13, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://read.qxmd.com/read/30414212/evaluation-of-18-f-2fp3-in-pigs-and-non-human-primates
#20
Hanne D Hansen, Cristian C Constantinescu, Olivier Barret, Matthias M Herth, Janus H Magnussen, Szabolcs Lehel, Agnete Dyssegaard, Julie Colomb, Thierry Billard, Luc Zimmer, Gilles Tamagnan, Gitte M Knudsen
So far, no suitable 5-HT7 R radioligand exists for clinical PET imaging. [18 F]2FP3 was first tested in vivo in cats and the results were promising for further evaluations. Here, we evaluate the radioligand in pigs and non-human primates (NHP). Furthermore, we investigate species differences in 5-HT7 R binding with [3 H]SB-269970 autoradiography in post mortem pig, NHP, and human brain tissue. Specific binding of [18 F]2FP3 was investigated by intravenous administration of the 5-HT7 R specific antagonist SB-269970...
November 9, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
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