Lappin Graham, Garner R Colin
Xceleron Ltd, York Biocentre, Innovation Way, Heslington, York YO10 5NY, UK.
Nat Rev Drug Discov. 2003 Mar;2(3):233-40. doi: 10.1038/nrd1037.
The process of early clinical drug development has changed little over the past 20 years despite an up to 40% failure rate associated with inappropriate drug metabolism and pharmacokinetics of candidate molecules. A new method of obtaining human metabolism data known as microdosing has been developed which will permit smarter candidate selection by taking investigational drugs into humans earlier. Microdosing depends on the availability of two ultrasensitive 'big-physics' techniques: positron emission tomography (PET) can provide pharmacodynamic information, whereas accelerator mass spectrometry (AMS) provides pharmacokinetic information. Microdosing allows safer human studies as well as reducing the use of animals in preclinical toxicology.
在过去20年里，早期临床药物开发过程变化不大，尽管候选分子的药物代谢和药代动力学不当导致的失败率高达40%。一种被称为微剂量给药的获取人体代谢数据的新方法已经开发出来，它将通过更早地将研究药物应用于人体来实现更明智的候选药物筛选。微剂量给药依赖于两种超灵敏的“大物理”技术：正电子发射断层扫描（PET）可提供药效学信息，而加速器质谱（AMS）则提供药代动力学信息。微剂量给药不仅能使人体研究更安全，还能减少临床前毒理学中动物的使用。
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