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A phase I safety and pharmacokinetic study of OGT 719 in patients with liver cancer (2004)_香港中文大学

香港中文大学 辅仁网/2017-06-27

A phase I safety and pharmacokinetic study of OGT 719 in patients with liver cancer
Publication in refereed journal


香港中文大学研究人员 ( 现职)
庄立信教授 (肿瘤学系)
杨明明教授 (肿瘤学系)
陈德章教授 (肿瘤学系)
梁惠棠教授 (肿瘤学系)
莫树锦教授 (肿瘤学系)


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引用次数
Web of Sciencehttp://aims.cuhk.edu.hk/converis/portal/Publication/3WOS source URL

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摘要OGT 719 (Oxford GlycoSciences, Abingdon, UK) is a novel nucleoside analogue with a galactose molecule attached to a fluorinated pyrimidine. OGT 719 has the capacity selectively to bind to asialoglycoprotein receptors that are found exclusively on hepatocytes and hepatocellular carcinoma (HCC) cells. The aim of this study was to establish the safety and to examine the pharmacokinetics of this novel compound in patients with liver cancer. Fourteen patients received a total of http://aims.cuhk.edu.hk/converis/portal/Publication/37 cycles of OGT 719 at four dose levels ([500 mg/m(2) first cycle, 1000 mg/m(2) subsequent cycles], 1000 mg/m(2), http://aims.cuhk.edu.hk/converis/portal/Publication/3 http://aims.cuhk.edu.hk/converis/portal/Publication/300 mg/m(2) and 7500 mg/m(2)). OGT 719 was administered as a http://aims.cuhk.edu.hk/converis/portal/Publication/3-h intravenous infusion in a 250 ml saline solution, daily for 5 days every 4 weeks. Pharmacokinetic parameters were studied during the first cycle of dose levels 1 and 2 (500 mg/m(2), and 1000 mg/m(2), respectively). The maximum plasma concentration was attained within 5 min of completing the infusion and almost doubled, dose dependently, with a doubling of the infused dose. The plasma level declined rapidly in a monophasic manner with an elimination half-life of 2.1 and 2.5 h for dose level 1 and 2, respectively. The mean area under the curve (AUC(o-t), area under the curve to 24 h; AUC(o-infinity), area under the curve to infinity) doubled at the higher dose level. None of the patients had a significant tumor response. Elimination half-life of OGT 719 by http://aims.cuhk.edu.hk/converis/portal/Publication/3-h intravenous infusion is short and monophasic. Toxicity was minimal at the highest dose level.

着者Mok TSK, Leung TWT, Brown G, Moyses C, Chan ATC, Yeo W, Wong H, Chak K, Johnson P
期刊名称Acta Oncologica
出版年份2004
月份4
日期1
卷号4http://aims.cuhk.edu.hk/converis/portal/Publication/3
期次http://aims.cuhk.edu.hk/converis/portal/Publication/3
出版社TAYLOR & FRANCIS AS
页次245 - 251
国际标準期刊号0284-186X
语言英式英语

Web of Science 学科类别Oncology; ONCOLOGY

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