The utility of microdosing over the past 5 years
Expert Opinion on Drug Metabolism & Toxicology November 28, 2008 DOI: 10.1517/17425250802531767 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Systematic review Peer reviewed |
|---|---|
| Sample size | 18 |
| Population | Drugs with published comparisons of microdose and therapeutic dose pharmacokinetics |
| Topics | Microdosing |
| Keywords | Microdose Pharmacokinetics Pharmacology Clinical trial Therapeutic index Drug |
| Citations | 89 |
| Key findings | 15 of 18 drugs demonstrated linear pharmacokinetics within a factor of 2 between a microdose and a therapeutic dose. |
Abstract
Background: 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.
Objective: To review the current literature on microdosing and assess how well microdose data have predicted the pharmacokinetics obtained at a therapeutic dose.
Methods: 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.
Conclusions: 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.
Comparable studies
Other systematic reviews and meta-analyses on microdosing, most cited first.
| Study | Year | Design | Participants |
|---|---|---|---|
| The emerging science of microdosing: A systematic review of research on low dose psychedelics (1955–2021) and recommendations for the field Human participants in microdosing studies | 2022 | Systematic review | n = 44 |
| The therapeutic potential of microdosing psychedelics in depression Healthy volunteers and patient samples | 2020 | Systematic review | |
| Potential safety, benefits, and influence of the placebo effect in microdosing psychedelic drugs: A systematic review | 2020 | Systematic review | |
| Microdosing Psychedelics: Current Evidence From Controlled Studies. Healthy adults | 2024 | Systematic review | |
| Keeping the promise: a critique of the current state of microdosing research | 2024 | Systematic review |
Citations in the library
Cited by 12
- 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
- Microdosing: Current and The Future Bioanalysis March 1, 2010
- Microdosing psychedelics: More questions than answers? An overview and suggestions for future research Journal of Psychopharmacology July 14, 2019
- The Use of Microdosing for In vivo Phenotyping of Cytochrome P450 Enzymes: Where Do We Stand? A Narrative Review European Journal of Drug Metabolism and Pharmacokinetics April 30, 2024
and 7 more in the library
Cites 3
- Positron emission tomography microdosing: a new concept with application in tracer and early clinical drug development European Journal of Clinical Pharmacology September 1, 2003
- 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