Tumor trapping of 5-fluorouracil: in vivo 19F NMR spectroscopic pharmacokinetics in tumor-bearing humans and rabbits

作者: W. Wolf , C. A. Presant , K. L. Servis , A. el-Tahtawy , M. J. Albright

DOI: 10.1073/PNAS.87.1.492

关键词: PathologyAdenocarcinomaNuclear magnetic resonance spectroscopyFluorine-19 NMRMagnetic resonance imagingHalf-lifeIn vivoChemotherapyBiochemistryChemistryPharmacokinetics

摘要: Abstract The pharmacokinetics of 5-fluorouracil (5FU) were studied in vivo patients with discrete tumors and rabbits bearing VX2 by using 19F NMR spectroscopy. The human studies conducted a 1.5-T Magnetom magnetic resonance imager (Siemens), the rabbit 4.7-T GE/Nicolet 33-cm bore magnet. Free 5FU was detected four six all but not normal tissues. No other metabolites seen these tumors, contrary to extensive catabolism we had previously documented spectroscopy both animal livers. tumor pool free those that trapped determined have half-life 0.4-2.1 hr, much longer than expected significantly blood (5-15 min), whereas ranged from 1.05 1.22 hr. In this initial experience, patient response chemotherapy may correlate extent trapping tumors. These document is clinically feasible vivo, allows noninvasive pharmacokinetic analyses at drug-target tissue real time, produce therapeutically important information time drug administration. Demonstration provides model for studying metabolic modulation experimental (in animals) method testing strategies patients).

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