Hume S P, Myers R
Imaging Research Solutions Ltd., Cyclotron Building, Hammersmith Hospital, DuCane Road, London, W12 0NN, UK.
Curr Pharm Des. 2002;8(16):1497-511. doi: 10.2174/1381612023394412.
Nuclear imaging techniques can provide information about the time course of uptake, the spatial distribution, and the functional effects of a drug in the human body. Recently, PET has also acquired the potential to affect the drug development process during a very early stage, when a drug is undergoing animal testing. The development of dedicated small animal scanners with high resolution has made it possible to assess the time course of uptake of a drug within a single animal, providing that the drug is labelled with a positron-emitting isotope. Dedicated small animal scanners may therefore prove to be very useful, especially in those parts of the drug development process that require a longitudinal study design. However, in the case of receptor and enzyme studies, there may be pharmacological constraints and specific radioactivity of the radiopharmaceuticals may become an important issue. This paper will assess the potential and also the limitations of high-resolution PET in animal testing of therapeutic drugs.
核成像技术能够提供有关药物在人体中的摄取时间进程、空间分布以及功能效应的信息。最近,正电子发射断层扫描(PET)在药物处于动物试验的非常早期阶段时,也获得了影响药物研发过程的潜力。高分辨率专用小动物扫描仪的发展使得在单只动物体内评估药物摄取的时间进程成为可能,前提是该药物用正电子发射同位素进行了标记。因此,专用小动物扫描仪可能会被证明非常有用,尤其是在药物研发过程中那些需要纵向研究设计的部分。然而,在受体和酶研究中,可能存在药理学限制,放射性药物的比活度可能会成为一个重要问题。本文将评估高分辨率PET在治疗性药物动物试验中的潜力以及局限性。