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用于正电子发射断层扫描的放射性标记抗癌药物的药代动力学。

Pharmacokinetics of radiolabelled anticancer drugs for positron emission tomography.

作者信息

Hutchinson O Clyde, Collingridge David R, Barthel Henryk, Price Pat M, Aboagye Eric O

机构信息

Cancer Research UK, Imperial College School of Medicine, Hammersmith Hospital, Du Cane Road, London W12 0NN, UK.

出版信息

Curr Pharm Des. 2003;9(11):917-29. doi: 10.2174/1381612033455288.

Abstract

Positron emission tomography (PET) provides the oncologist with information on tumour diagnosis, and treatment response monitoring. Mathematical modelling of tissue data, and online plasma radioactive metabolite profiling, enables important tissue kinetic parameters relating to the uptake, distribution and washout as well as arterial input function to be derived. The resultant kinetic data allow for not only diagnosis but also the assessment of therapeutic response endpoints. These endpoints can be used to measure specific therapeutic effects. This novel application of PET can provide information that is often difficult to measure in the intact animal or patient. The pharmacokinetics of radiolabelled N-[2-(dimethylamino)ethyl]acridine-4-carboxamide (DACA), temozolomide and 5-fluorouracil (5-FU) are described.

摘要

正电子发射断层扫描(PET)为肿瘤学家提供有关肿瘤诊断和治疗反应监测的信息。对组织数据进行数学建模以及在线血浆放射性代谢物分析,能够得出与摄取、分布、清除以及动脉输入函数相关的重要组织动力学参数。所得的动力学数据不仅可用于诊断,还能用于评估治疗反应终点。这些终点可用于测量特定的治疗效果。PET的这种新应用能够提供在完整动物或患者中通常难以测量的信息。本文描述了放射性标记的N-[2-(二甲氨基)乙基]吖啶-4-甲酰胺(DACA)、替莫唑胺和5-氟尿嘧啶(5-FU)的药代动力学。

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