The expanding utility of microdosing
Clinical Pharmacology in Drug Development November 1, 2015 DOI: 10.1002/cpdd.235 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Review Peer reviewed |
|---|---|
| Topics | Microdosing |
| Key findings | Approximately 80% of drugs tested orally and 100% intravenously exhibit scalable pharmacokinetics between a microdose and a therapeutic dose within a factor of 2. |
Abstract
AbstractThe concept of microdosing has been around for more than a decade. It consists of the subpharmacologic administration of an investigational drug (1% of the pharmacologic dose or 100 µg, whichever is lower) to human subjects to attain pre–phase 1 pharmacokinetics (PK) in humans. The major concern with microdosing has been the potential for nonlinear PK between doses, but methods are emerging to evaluate the potential for nonlinear PK prior to conducting a study. Currently, approximately 80% of drugs tested by the oral route and 100% by the intravenous route have exhibited scalable PK between a microdose and a therapeutic dose (within a factor of 2). Over the past few years microdosing has found utility in pediatrics, protein‐based therapeutics, and a new application known as intra‐arterial microdosing that focuses more on localized pharmacodynamics than PK. Compared with other PK predictive methods, such as physiologically based pharmacokinetic modeling, allometry, and in vitro–in vivo extrapolation, microdosing appears to provide a significantly better understanding of PK prior to phase 1, albeit within what is currently a limited database.
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 8
- 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
- Microdosing and drug development: past, present and future Expert Opinion on Drug Metabolism & Toxicology April 4, 2013
- Microdosing: A Critical Assessment of Human Data Journal of Pharmaceutical Sciences August 23, 2012
- To Apply Microdosing or Not? Recommendations to Single Out Compounds with Non-Linear Pharmacokinetics. Clinical Pharmacokinetics January 2016
and 3 more in the library