title: Microdosing and drug development: past, present and future.
abstract: BACKGROUND
  Microdosing is an approach to early drug development where exploratory pharmacokinetic data are acquired in humans using inherently safe sub-pharmacologic doses of drug. The first publication of microdose data was 10 years ago and this review comprehensively explores the microdose concept from conception, over the past decade, up until the current date.
  
  
  METHODS
  The authors define and distinguish the concept of microdosing from similar approaches. The authors review the ability of microdosing to provide exploratory pharmacokinetics (concentration-time data) but exclude microdosing using positron emission tomography. The article provides a comprehensive review of data within the peer-reviewed literature as well as the latest applications and a look into the future, towards where microdosing may be headed.
  
  
  CONCLUSIONS
  Evidence so far suggests that microdosing may be a better predictive tool of human pharmacokinetics than alternative methods and combination with physiologically based modelling may lead to much more reliable predictions in the future. The concept has also been applied to drug-drug interactions, polymorphism and assessing drug concentrations over time at its site of action. Microdosing may yet have more to offer in unanticipated directions and provide benefits that have not been fully realised to date.
authors.affiliation: University of Lincoln, Brayford Pool, Lincoln, LN6 7TS, UK. glappin@lincoln.ac.uk
authors.forename: Graham
authors.initials: G
authors.lastname: Lappin
authors.forename: Robert
authors.initials: R
authors.lastname: Noveck
authors.forename: Tal
authors.initials: T
authors.lastname: Burt
mesh_terms: D061605:Administration, Intravenous / Q000639:trends; D000284:Administration, Oral; D000818:Animals; D017321:Clinical Trials, Phase I as Topic; D016208:Databases, Factual; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D017408:Guidelines as Topic; D006801:Humans; D004364:Pharmaceutical Preparations / Q000008:administration & dosage*; D010599:Pharmacokinetics; D049268:Positron-Emission Tomography
chemical_list: D004364:Pharmaceutical Preparations
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