Biodistribution and pharmacokinetics of I-131 labelled 4-Iodophenylacetic acid

Show simple item record Zeevaart, Jan Rijn Szucs, Zoltan Pulker, Tamsyn A. Sello, Thato Bracher, Jacqueline Sathekge, Mike Machaba 2012-12-12T11:33:51Z 2013-10-31T00:20:04Z 2012-10-11
dc.description.abstract Phenylacetate has been reported to have a potent anti-proliferative and anti-differentiating effect in haematological malignancies and in solid tumours at non-toxic concentrations. This study is a preliminary investigation of 131Iradiolabelled 4-iodophenylacetic acid as a potential radiopharmaceutical equivalent. Radiolabelling by isotope exchange gave a radiochemical yield of 53 ± 6 %, and a radiochemical purity of 97.8 ± 1.2 %, as qualified by HPLC. The labelled product was used in Sprague Dawley rats and athymic nude (balb/c) mice xenografted with WHCO1 cells (an oesophageal cancer cell line). Dynamic and static scans were carried out on *rats with a SPECT camera to determine the biodistribution of 4-[131I]-iodophenylacetic acid. No target organ was found after 5 h with fast excretion from all organs via the kidney into the urine. Ex vivo studies (termination 5 h after injection) were performed in 12 xenograft mice carrying tumours of 5-8 mm on their right flank. Tumour uptake of 4 + 0.4 % ID/g was recorded with a tumour to background ratio of 2. As the blood pool still contains high levels of activity after 5 h in mice, increased tumour uptake may occur at later time points, which might warrant further investigation. en_US
dc.description.uri en_US
dc.identifier.citation Zeevaart, JR, Szucs, Z, Pulker, T, Sello, T, Bracher, J & Sathekge, M 2012, 'Biodistribution and pharmacokinetics of I-131 labelled 4-Iodophenylacetic acid', Current Radiopharmaceuticals, vol. 5, no. 4, pp. 356-362. en_US
dc.identifier.issn 1874-4710 (print)
dc.identifier.issn 1874-4729 (online)
dc.language.iso en en_US
dc.publisher Bentham Science en_US
dc.rights Bentham Science en_US
dc.subject SPECT en_US
dc.subject Phenylacetic acid metabolism en_US
dc.subject Solid tumour en_US
dc.title Biodistribution and pharmacokinetics of I-131 labelled 4-Iodophenylacetic acid en_US
dc.type Postprint Article en_US

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