Pharmacokinetics of the thymidine analog 2′-fluoro-5-methyl-1-β-d-arabinofuranosyluracil (FMAU) in tumor-bearing rats

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• 作者：Bading ; James R. ; Shahinian ; Antranik H. ; Vail ; Amy ; Bathija ; Pravin ; Koszalka ; G.W. ; Koda ; Robert T. ; et. al.
• 关键词：[¹¹C]FMAU ; Proliferation marker ; Tumor imaging ; PET ; Rat ; Pharmacokinetics
• 刊名：Nuclear Medicine and Biology
• 出版年：2004
• 期刊代码：43_09698051
• 类别：ph
• 出版时间：May, 2004
• 卷：31
• 期：4
• 页码：407-418
• 文件大小：309 K

摘要

The thymidine analog 2′-fluoro-5-methyl-1-β-d-arabinofuranosyluracil (FMAU) is incorporated into DNA and is resistant to catabolism. We performed pharmacokinetic measurements with [¹⁴C]FMAU and PET studies with [¹¹C]FMAU using rats bearing several different syngeneic tumors. Among normal tissues, FMAU uptake reflected relative cell turnover rates. Among tumors, the highest uptake occurred in a rapidly growing colon carcinoma, but was similarly low in both rapidly and slowly growing prostate tumors. FMAU was not catabolized and was rapidly incorporated into DNA by small intestine and colon tumors. Results indicate that FMAU may be useful for imaging tissue DNA synthesis, although tumor uptake was modest and not well correlated with growth rate among the models examined.