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Development of ⁶⁸Ga-labelled DTPA galactosyl human serum albumin for liver function imaging. 2013

Roland Haubner, and David R Vera, and Salman Farshchi-Heydari, and Anna Helbok, and Christine Rangger, and Daniel Putzer, and Irene J Virgolini
Department of Nuclear Medicine, Innsbruck Medical University, Innsbruck, Austria. roland.haubner@i-med.ac.at

OBJECTIVE The hepatic asialoglycoprotein receptor is responsible for degradation of desialylated glycoproteins through receptor-mediated endocytosis. It has been shown that imaging of the receptor density using [(99m)Tc]diethylenetriamine pentaacetic acid (DTPA) galactosyl human serum albumin ([(99m)Tc]GSA) allows non-invasive determination of functional hepatocellular mass. Here we present the synthesis and evaluation of [(68)Ga]GSA for the potential use with positron emission tomography (PET). METHODS Labelling of GSA with (68)Ga was carried out using a fractionated elution protocol. For quality control thin-layer chromatography (TLC), high-performance liquid chromatography (HPLC) and size exclusion chromatography (SEC) techniques were evaluated. Stability of [(68)Ga]GSA was studied in phosphate-buffered saline (PBS) and human serum. For in vivo evaluation [(68)Ga]GSA distribution in Lewis rats was compared with [(99m)Tc]GSA by using a dual isotope protocol. PET and planar imaging studies were performed using the same scaled molar dose of [(68)Ga]GSA and [(99m)Tc]GSA. Time-activity curves (TAC) for heart and liver were generated and corresponding parameters calculated (t50, t90). RESULTS [(68)Ga]GSA can be produced with high radiochemical purity. The best TLC methods for determining potential free (68)Ga include 0.1 M sodium citrate as eluent. None of the TLC methods tested were able to determine potential colloids. This can be achieved by SEC. HPLC confirmed high radiochemical purity (>98%). Stability after 120 min incubation at 37 °C was high in PBS (>95% intact tracer) and low in human serum (∼27% intact tracer). Biodistribution studies simultaneously injecting both tracers showed comparable liver uptake, whereas activity concentration in blood was higher for [(68)Ga]GSA compared to [(99m)Tc]GSA. The [(99m)Tc]GSA TACs exhibited a small degree of hepatic metabolism compared to the [(68)Ga]GSA curves. The mean [(68)Ga]GSA t90 was higher than the mean t90 for [(99m)Tc]GSA. The mean [(68)Ga]GSA t50 was not significantly different from the mean t50 for [(99m)Tc]GSA. CONCLUSIONS This study provides a promising new (68)Ga-labelled compound based on a commercially used kit for imaging the functional hepatocellular mass.

UI MeSH Term Description Entries
D008099 Liver A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances. Livers
D009942 Organometallic Compounds A class of compounds of the type R-M, where a C atom is joined directly to any other element except H, C, N, O, F, Cl, Br, I, or At. (Grant & Hackh's Chemical Dictionary, 5th ed) Metallo-Organic Compound,Metallo-Organic Compounds,Metalloorganic Compound,Organometallic Compound,Metalloorganic Compounds,Compound, Metallo-Organic,Compound, Metalloorganic,Compound, Organometallic,Compounds, Metallo-Organic,Compounds, Metalloorganic,Compounds, Organometallic,Metallo Organic Compound,Metallo Organic Compounds
D004369 Pentetic Acid An iron chelating agent with properties like EDETIC ACID. DTPA has also been used as a chelator for other metals, such as plutonium. DTPA,Diethylenetriamine Pentaacetic Acid,Pentetates,Penthanil,Ca-DTPA,CaDTPA,CaNa-DTPA,Calcium Trisodium Pentetate,DETAPAC,Indium-DTPA,Mn-Dtpa,Pentacin,Pentacine,Pentaind,Pentetate Calcium Trisodium,Pentetate Zinc Trisodium,Sn-DTPA,Zinc-DTPA,Indium DTPA,Pentaacetic Acid, Diethylenetriamine,Pentetate, Calcium Trisodium,Zinc DTPA
D005710 Gallium Radioisotopes Unstable isotopes of gallium that decay or disintegrate emitting radiation. Ga atoms with atomic weights 63-68, 70 and 72-76 are radioactive gallium isotopes. Radioisotopes, Gallium
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000418 Albumins Water-soluble proteins found in egg whites, blood, lymph, and other tissues and fluids. They coagulate upon heating. Albumin
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013668 Technetium Tc 99m Aggregated Albumin A gamma-emitting radionuclide imaging agent used for the diagnosis of diseases in many tissues, particularly in cardiovascular and cerebral circulation. Tc 99m-Albumin,Tc 99m-Albumin Colloid,99m-Tc-HSA,99mTc-Albures,99mTc-HSA,99mTc-Human Serum Albumin,Tc-99m-HAM,Tc-99m-MAA,Tc-99m-Microalbumin,Tc-HAMM,Tc99m-Albumin,Technetium-99m Albumin Colloid,99mTc Albures,99mTc Human Serum Albumin,99mTcAlbures,Albumin Colloid, Technetium-99m,Albumin, 99mTc-Human Serum,Colloid, Tc 99m-Albumin,Colloid, Technetium-99m Albumin,Serum Albumin, 99mTc-Human,Tc 99m Albumin,Tc 99m Albumin Colloid,Tc 99m HAM,Tc 99m MAA,Tc 99m Microalbumin,Tc HAMM,Tc99m Albumin,Technetium 99m Albumin Colloid
D014018 Tissue Distribution Accumulation of a drug or chemical substance in various organs (including those not relevant to its pharmacologic or therapeutic action). This distribution depends on the blood flow or perfusion rate of the organ, the ability of the drug to penetrate organ membranes, tissue specificity, protein binding. The distribution is usually expressed as tissue to plasma ratios. Distribution, Tissue,Distributions, Tissue,Tissue Distributions
D016284 Technetium Tc 99m Pentetate A technetium imaging agent used in renal scintigraphy, computed tomography, lung ventilation imaging, gastrointestinal scintigraphy, and many other procedures which employ radionuclide imaging agents. Tc 99m-DTPA,Tc-DTPA,Technetium-DTPA,Technetium (99m) Pentetate,Technetium Pentetic Acid,Technetium diethylenetriamine pentaacetic acid,99m-DTPA, Tc,Pentetic Acid, Technetium,Tc 99m DTPA,Technetium DTPA

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