ArticleClinical and translational science2020
Prediction of Metabolite-to-Parent Drug Exposure: Derivation and Application of a Mechanistic Static Model.
Article in Clinical and translational science, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
What it found
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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.
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Who cites it
4 citing papers in PubMed, 9 citations in OpenAlex.
- Trial
- Applications of Pharmacometrics in Antibody-Drug Conjugate Development.Pharmaceutics · 2026Review
- The Current State of Biotransformation Science - Industry Survey of In Vitro and In Vivo Practices, Clinical Translation, and Future Trends.Pharmaceutical research · 2024Article
- Pharmacokinetic Variability of Oral Cannabidiol and Its Major Metabolites after Short-Term High-Dose Exposure in Healthy Subjects.Medical cannabis and cannabinoidsArticle
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
In the development of new drugs, the prediction of metabolite-to-parent plasma exposure ratio in humans prior to administration in a clinical study has emerged as an important need. In this work, we derived a mechanistic static model based on first principles to estimate metabolite-to-parent plasma exposure ratio, considering the contribution of liver and gut metabolism and drug transport. Knowledge (or assumptions) of mechanisms of clearance and organs involved is required. Input parameters needed included intrinsic clearance, fraction of clearance to the metabolite of interest, various binding values, and, in some cases, active transport clearance. The principles are illustrated with four drugs that yield six metabolites, with one in which clearance is dependent on a pathway subject to genetic polymorphism. Overall, the approach yielded metabolite-to-parent ratios within about twofold of the actual values and, thus, can be valuable in decision making in the drug development process.
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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.