Lappin Graham, Garner R Colin
Xceleron Ltd, The Biocentre, Innovation Way, York, YO10 5NY, UK.
Expert Opin Drug Metab Toxicol. 2008 Dec;4(12):1499-506. doi: 10.1517/17425250802531767.
Microdosing studies (human Phase 0) are used to select drug candidates for Phase I clinical trials on the basis of their pharmacokinetic properties, using subpharmacologic doses (maximum 100 microg). There are questions as to whether pharmacokinetic data obtained at these low doses will predict those at the clinically relevant dose.
To review the current literature on microdosing and assess how well microdose data have predicted the pharmacokinetics obtained at a therapeutic dose.
All data published in the peer reviewed literature comparing pharmacokinetics at a microdose with a therapeutic dose were reviewed, excluding those studies aimed at imaging.
Of the 18 drugs reported, 15 demonstrated linear pharmacokinetics within a factor of 2 between a microdose and a therapeutic dose. Therefore, data that support the utility of microdosing are beginning to emerge.
微剂量研究（人体0期试验）用于根据药物的药代动力学特性，采用亚药理剂量（最大100微克）来选择用于I期临床试验的候选药物。关于在这些低剂量下获得的药代动力学数据是否能预测临床相关剂量下的数据，存在一些疑问。
回顾关于微剂量的当前文献，并评估微剂量数据预测治疗剂量下药代动力学的能力。
对同行评审文献中发表的所有比较微剂量和治疗剂量下药代动力学的数据进行回顾，排除那些旨在成像的研究。
在报道的18种药物中，15种在微剂量和治疗剂量之间呈现出2倍以内的线性药代动力学。因此，支持微剂量效用的数据开始出现。
