Human Microdosing/Phase 0 Studies to Accelerate Drug Development
Human-based Systems for Translational Research December 9, 2014 DOI: 10.1039/9781782620136-00241 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Review Peer reviewed |
|---|---|
| Topics | Microdosing |
| Key findings | Microdosing Phase 0 studies are more relevant and predictive of a drug's ADME at therapeutic doses than early in vitro and preclinical studies. |
Abstract
Human microdosing Phase 0 studies are used to obtain key information in early drug development concerning a drug's pharmacokinetic and limited pharmacodynamic parameters. Developed as a method in the 2000s, microdosing has become part of the critical path of drug development. Microdosing studies can assist in drug candidate selection prior to going into expensive Phase I studies. This chapter provides a historical perspective of microdose studies, details the steps involved in conducting a successful microdose study and highlights the value of the ultrasensitive bioanalytical technology accelerator mass spectrometry in microdose study conduct. The scientific, regulatory, ethical and commercial aspects of microdosing are reviewed, together with where the method has most utility. On the basis that the best model for humans is human, the chapter explains why microdose studies should be undertaken at the expense of early in vitro and preclinical studies as being more relevant and predictive of a drug's ADME at therapeutic doses and thus provide a new paradigm for early drug development.
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 5
- Use of microdosing to predict pharmacokinetics at the therapeutic dose: Experience with 5 drugs Clinical Pharmacology & Therapeutics September 1, 2006
- Identification of the Rate-Determining Process in the Hepatic Clearance of Atorvastatin in a Clinical Cassette Microdosing Study Clinical Pharmacology & Therapeutics August 10, 2011
- Microdosing Clinical Study: Pharmacokinetic, Pharmacogenomic (SLCO2B1), and Interaction (Grapefruit Juice) Profiles of Celiprolol Following the Oral Microdose and Therapeutic Dose The Journal of Clinical Pharmacology May 19, 2011
- Microdosing: A Critical Assessment of Human Data Journal of Pharmaceutical Sciences August 23, 2012
- Predicting Drug Candidate Victims of Drug-Drug Interactions, using Microdosing Clinical Pharmacokinetics February 16, 2012