ReviewExpert opinion on drug metabolism & toxicology2010
Rationalization and prediction of in vivo metabolite exposures: the role of metabolite kinetics, clearance predictions and in vitro parameters.
Review in Expert opinion on drug metabolism & toxicology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 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
17 citing papers in PubMed.
- An S-warfarin and AZD1981 interaction: in vitro and clinical pilot data suggest the N-deacetylated amino acid metabolite as the primary perpetrator.British journal of clinical pharmacology · 2017Trial
- Chiral Plasma Pharmacokinetics and Urinary Excretion of Bupropion and Metabolites in Healthy Volunteers.The Journal of pharmacology and experimental therapeutics · 2016Trial
- Development of Integrated Parent-Metabolite Pharmacokinetic Model With Apparent Presystemic Metabolism to Characterize the Disposition of Alverine.CPT: pharmacometrics & systems pharmacology · 2026Article
- Exploratory Pharmacokinetic Characterization of Enrofloxacin and Ciprofloxacin in Plasma and Interstitial Fluid of Dogs: Nonlinear Mixed-Effects Modeling and PK/PD Target Attainment Analysis.Antibiotics (Basel, Switzerland) · 2026Article
- Role of metabolites in drug-drug interactions.Drug metabolism and pharmacokinetics · 2026Review
- Assessment of Telisotuzumab Vedotin Drug-Drug Interaction Potential Using Physiologically-Based Pharmacokinetic Modeling and Simulations.Journal of clinical pharmacology · 2025Article
- Comprehensive interpretation of in vitro micronucleus test results for 292 chemicals: from hazard identification to risk assessment application.Archives of toxicology · 2022Article
- Review
- Article
- Metabolite Profiling and Characterization of LW6, a Novel HIF-1α Inhibitor, as an Antitumor Drug Candidate in Mice.Molecules (Basel, Switzerland) · 2021Article
- Seconds-Resolved, In Situ Measurements of Plasma Phenylalanine Disposition Kinetics in Living Rats.Analytical chemistry · 2021Article
- The effect of grape seed and green tea extracts on the pharmacokinetics of imatinib and its main metabolite, N-desmethyl imatinib, in rats.BMC pharmacology & toxicology · 2020Article
- The effect of cannabidiol on the pharmacokinetics of carbamazepine in rats.Naunyn-Schmiedeberg's archives of pharmacology · 2020Article
- Minimal Physiologically Based Pharmacokinetic Model of Intravenously and Orally Administered Delta-9-Tetrahydrocannabinol in Healthy Volunteers.European journal of drug metabolism and pharmacokinetics · 2019Article
- Quantitative Prediction of Drug-Drug Interactions Involving Inhibitory Metabolites in Drug Development: How Can Physiologically Based Pharmacokinetic Modeling Help?CPT: pharmacometrics & systems pharmacology · 2016Article
- Prediction of relative in vivo metabolite exposure from in vitro data using two model drugs: dextromethorphan and omeprazole.Drug metabolism and disposition: the biological fate of chemicals · 2012Article
- Allosteric activation of cytochrome P450 3A4 by α-naphthoflavone: branch point regulation revealed by isotope dilution analysis.Biochemistry · 2011Article
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.
Funding
Abstract
importance of the fieldDue to growing concerns over toxic or active metabolites, significant efforts have been focused on qualitative identification of potential in vivo metabolites from in vitro data. However, limited tools are available to quantitatively predict their human exposures. AREAS COVERED IN THIS REVIEW: Theory of clearance predictions and metabolite kinetics is reviewed together with supporting experimental data. In vitro and in vivo data of known circulating metabolites and their parent drugs were collected and the predictions of in vivo exposures of the metabolites were evaluated. WHAT THE READER WILL GAIN: The theory and data reviewed will be useful in early identification of human metabolites that will circulate at significant levels in vivo and help in designing in vivo studies that focus on characterization of metabolites. It will also assist in rationalization of metabolite-to-parent ratios used as markers of specific enzyme activity. TAKE HOME MESSAGE: The relative importance of a metabolite in comparison to the parent compound as well as other metabolites in vivo can only be predicted using the metabolite's in vitro formation and elimination clearances, and the in vivo disposition of a metabolite can only be rationalized when the elimination pathways of that metabolite are known.
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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.