Impact of microdosing clinical study — Why necessary and how useful?
Advanced Drug Delivery Reviews October 14, 2010 Yuichi Sugiyama, Shinji Yamashita 60 citations
Microdose clinical studies, which administer less than 100 μg of a test compound, allow selection of drug candidates with favorable pharmacokinetic profiles in humans while minimizing risk of harmful events. However, the low dose may produce different pharmacokinetic profiles than at therapeutic doses, and no efficacy or safety information is obtained from such studies. Combining microdose study data with physiologically based pharmacokinetic (PBPK) model analysis of in vitro metabolism, transport, and binding enables accurate prediction of therapeutic-dose pharmacokinetics. Positron emission tomography molecular imaging can further provide efficacy and safety information. Coordinating these methodologies is expected to innovate drug discovery and development.