ReviewExpert opinion on drug metabolism & toxicology2013
Microdosing and drug development: past, present and future.
Review in Expert opinion on drug metabolism & toxicology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 49 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
49 citing papers in PubMed, 97 citations in OpenAlex.
- Pharmacokinetics, Excretion, and Mass Balance of [Clinical pharmacology in drug development · 2018Trial
- A human microdose study of the antimalarial drug GSK3191607 in healthy volunteers.British journal of clinical pharmacology · 2018Trial
- Determination of the absolute oral bioavailability of niraparib by simultaneous administration of aCancer chemotherapy and pharmacology · 2018Trial
- Successful Use of [Clinical pharmacokinetics · 2017Trial
- Intra-Target Microdosing - A Novel Drug Development Approach: Proof of Concept, Safety, and Feasibility Study in Humans.Clinical and translational science · 2017Trial
- Drug-drug interaction of microdose and regular-dose omeprazole with a CYP2C19 inhibitor and inducer.Drug design, development and therapy · 2017Trial
- A microdose study of ¹⁴C-AR-709 in healthy men: pharmacokinetics, absolute bioavailability and concentrations in key compartments of the lung.European journal of clinical pharmacology · 2013Trial
- Review
- Central Nervous System Biodistribution and Pharmacokinetics of Radiolabeled Tofersen in Rodents, Nonhuman Primates, and Humans.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2026Article
- Selection of Solubility Enhancement Technologies for S-892216, a Novel COVID-19 Drug Candidate.Pharmaceutics · 2025Article
- The Finite Absorption Time Concept Guiding Model Informed Drug & Generics Development in Clinical Pharmacology.Pharmaceutical research · 2025Review
- A sub-pharmacological test dose does not predict individual docetaxel exposure in prostate cancer patients.Cancer chemotherapy and pharmacology · 2024Article
- Dynamic PET reveals compartmentalized brain and lung tissue antibiotic exposures of tuberculosis drugs.Nature communications · 2024Observational
- 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 · 2024Review
- Development of a sensitive LC-MS/MS assay to support human microdose study for an oral agonist of the GLP-1 receptor.Bioanalysis · 2024Article
- Dynamic PET Reveals Compartmentalized Brain and Lung Tissue Antibiotic Exposures.Research square · 2024Article
- The application of Phase 0 and microtracer approaches in early clinical development: past, present, and future.Frontiers in pharmacology · 2024Review
- Linezolid does not improve bactericidal activity of rifampin-containing first-line regimens in animal models of TB meningitis.International journal of antimicrobial agents · 2024Article
- When to consider intra-target microdosing: physiologically based pharmacokinetic modeling approach to quantitatively identify key factors for observing target engagement.Frontiers in pharmacology · 2024Article
- A naïve pooled data approach for extrapolation of Phase 0 microdose trials to therapeutic dosing regimens.Clinical and translational science · 2023Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
3 authors at 3 institutions in 2 countries.
Funding
Abstract
introductionMicrodosing 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. AREAS COVERED: 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. EXPERT OPINION: 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.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.