ReviewThe AAPS journal2006
Current industrial practices of assessing permeability and P-glycoprotein interaction.
Review in The AAPS journal, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 48 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
48 citing papers in PubMed.
- Assessment of In Vivo Clinical Product Performance of a Weak Basic Drug by Integration of In Vitro Dissolution Tests and Physiologically Based Absorption Modeling.The AAPS journal · 2015Trial
- Knockout Transporter Cell Lines to Assess Substrate Potential Towards Efflux Transporters.The AAPS journal · 2024Article
- In Vitro Evaluation of Drug-Drug Interaction Potential of Epetraborole, a Novel Bacterial Leucyl-tRNA Synthetase Inhibitor.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Small molecules targeting different cellular pathologies for the treatment of amyotrophic lateral sclerosis.Medicinal research reviews · 2023Review
- Combining SILCS and Artificial Intelligence for High-Throughput Prediction of the Passive Permeability of Drug Molecules.Journal of chemical information and modeling · 2023Article
- Reliable Prediction of Caco-2 Permeability by Supervised Recursive Machine Learning Approaches.Pharmaceutics · 2022Article
- Why 90% of clinical drug development fails and how to improve it?Acta pharmaceutica Sinica. B · 2022Review
- Amino-Heterocycle Tetrahydroisoquinoline CXCR4 Antagonists with Improved ADME Profiles via Late-Stage Buchwald Couplings.ACS medicinal chemistry letters · 2021Article
- Meta-Assessment of Metformin Absorption and Disposition Pharmacokinetics in Nine Species.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Matrix Metalloproteinase 13 Inhibitors for Modulation of Osteoclastogenesis: Enhancement of Solubility and Stability.ChemMedChem · 2021Article
- An epoxide hydrolase inhibitor reduces neuroinflammation in a mouse model of Alzheimer's disease.Science translational medicine · 2020Article
- A peptide for transcellular cargo delivery: Structure-function relationship and mechanism of action.Journal of controlled release : official journal of the Controlled Release Society · 2020Article
- Purine and Purine Isostere Derivatives of Ferrocene: An Evaluation of ADME, Antitumor and Electrochemical Properties.Molecules (Basel, Switzerland) · 2020Article
- Article
- Benzaldehyde thiosemicarbazone derivatives against replicating and nonreplicating Mycobacterium tuberculosis.The Journal of antibiotics · 2019Article
- Prediction of Membrane Permeation of Drug Molecules by Combining an Implicit Membrane Model with Machine Learning.Journal of chemical information and modeling · 2019Article
- Nanofibrous Scaffolds Support a 3DFrontiers in pharmacology · 2019Article
- Theoretical Prediction of the Complex P-Glycoprotein Substrate Efflux Based on the Novel Hierarchical Support Vector Regression Scheme.Molecules (Basel, Switzerland) · 2018Article
- Human Primary Cell-Based Organotypic Microtissues for Modeling Small Intestinal Drug Absorption.Pharmaceutical research · 2018Article
- Antimycobacterial activity of nitrogen heterocycles derivatives: 7-(pyridine-4-yl)-indolizine derivatives. Part VIIJournal of enzyme inhibition and medicinal chemistry · 2017Article
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
No grant is acknowledged in the PubMed record.
Abstract
Combination of the in vitro models that are high throughput but less predictive and the in vivo models that are low throughput but more predictive is used effectively to evaluate the intestinal permeability and transport characteristics of a large number of drug candidates during lead selection and lead optimization processes. Parallel artificial membrane permeability assay and Caco-2 cells are the most frequently used in vitro models to assess intestinal permeability. The popularity of these models stems from their potential for high throughput, cost effectiveness, and adequate predictability of absorption potential in humans. However, several caveats associated with these models (eg, poor predictability for transporter-mediated and paracellularly absorbed compounds, significant nonspecific binding to cells/devices leading to poor recovery, variability associated with experimental factors) need to be considered carefully to realize their full potential. P-glycoprotein, among other pharmaceutically relevant transporters, has been well demonstrated to be the major determinant of drug disposition. The review article presents an objective analysis of the permeability and transporter models currently being used in the pharmaceutical industry and could help guide the discovery scientists in implementing these models in an optimal fashion.
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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.