Pharmacokinetics II: 14C-Labelled Microdosing in Assessing Drug Pharmacokinetics at Phase 0
G. Lappin
July 30, 2010 DOI: 10.1007/978-3-7091-0144-5_11 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Review |
|---|---|
| Topics | Microdosing |
| Key findings | Microdose pharmacokinetics scale to therapeutic doses within a factor of two for 84% of orally administered drugs and 100% of intravenously administered drugs, based on 23 drugs with comparable data. Non-linearity is interpreted through mechanistic understanding, and 14C labeling facilitates sensitive analysis and early metabolism assessment. |
Abstract
Microdosing came onto the scene with the first publication of data in 2003. Since this time the number of compounds where the pharmacokinetics observed at a microdose compared to a therapeutic dose has grown steadily. Based on current data in the public domain, there are 23 drugs where microdose and therapeutic dose pharmacokinetics can be compared. Of these, 84% scale within a factor of 2 for oral administration and 100% for intravenous administration. Where pharmacokinetic non-linearity is seen, a growing understanding of the mechanisms involved are being applied to interpret the microdose data in the context of the selection of candidate drugs for further development. Inclusion of a 14C isotopic tracer into the molecule enables sensitive AMS analysis to be used as well as obtaining an early indication of the drug’s metabolism in humans.
Comparable studies
Other narrative reviews on microdosing, most cited first.
| Study | Year | Design | Participants |
|---|---|---|---|
| Big physics, small doses: the use of AMS and PET in human microdosing of development drugs | 2003 | Review | |
| Phase 0/microdosing approaches: time for mainstream application in drug development? | 2020 | Review | |
| Microdosing and drug development: past, present and future | 2013 | Review | |
| Microdosing and Other Phase 0 Clinical Trials: Facilitating Translation in Drug Development | 2016 | Review | |
| Expectancy Effects in Psychedelic Trials. | 2024 | Review |
Citations in the library
Cites 4
- Big physics, small doses: the use of AMS and PET in human microdosing of development drugs Nature Reviews Drug Discovery February 28, 2003
- Use of microdosing to predict pharmacokinetics at the therapeutic dose: Experience with 5 drugs Clinical Pharmacology & Therapeutics September 1, 2006
- The utility of microdosing over the past 5 years Expert Opinion on Drug Metabolism & Toxicology November 28, 2008
- Microdosing: Current and The Future Bioanalysis March 1, 2010