ArticleThe AAPS journal2013
Drug discovery and regulatory considerations for improving in silico and in vitro predictions that use Caco-2 as a surrogate for human intestinal permeability measurements.
Article in The AAPS journal, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 57 papers.
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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.
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Who cites it
57 citing papers in PubMed.
- Review
- Two- and Three-Dimensional Human Intestinal Tissue Models for Cryptosporidium Infection.Methods in molecular biology (Clifton, N.J.) · 2026Article
- Three-dimensional multicellular layer structure: an advanced in vitro model for studying inflammatory bowel diseases.Scientific reports · 2025Article
- Gastrointestinal tract, its pathophysiology andWorld journal of gastroenterology · 2025Review
- Characterization and Anti-Inflammatory Effects ofMicroorganisms · 2025Article
- Article
- Assessment of drug permeability using a small airway microphysiological system.Frontiers in pharmacology · 2025Article
- Article
- Informing the risk assessment related to lactation and drug exposure: A physiologically based pharmacokinetic lactation model for pregabalin.CPT: pharmacometrics & systems pharmacology · 2024Article
- Improving the Accuracy of Permeability Data to Gain Predictive Power: Assessing Sources of Variability in Assays Using Cell Monolayers.Membranes · 2024Review
- HumanTissue barriers · 2024Review
- Model-Informed Drug Development: In Silico Assessment of Drug Bioperformance following Oral and Percutaneous Administration.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Characterization and optimization of variability in a human colonic epithelium culture model.ALTEX · 2024Article
- Exploring the therapeutic potential of cinnamoyl derivatives in attenuating inflammation in lipopolysaccharide-induced Caco-2 cells.Future medicinal chemistry · 2024Article
- Recent Advances in the Gastrointestinal Complex in Vitro Model for ADME Studies.Pharmaceutics · 2023Review
- Collagen Hydrolysates: A Source of Bioactive Peptides Derived from Food Sources for the Treatment of Osteoarthritis.Medicines (Basel, Switzerland) · 2023Review
- Anti-Hypercholesterolemia Effects of Edible Seaweed Extracts and Metabolomic Changes in Hep-G2 and Caco-2 Cell Lines.Life (Basel, Switzerland) · 2023Article
- Edible Seaweeds Extracts: Characterization and Functional Properties for Health Conditions.Antioxidants (Basel, Switzerland) · 2023Article
- Systematic comparison of transcriptomes of Caco-2 cells cultured under different cellular and physiological conditions.Archives of toxicology · 2023Article
- Characterization of a Potential KOR/DOR Dual Agonist with No Apparent Abuse Liability via a Complementary Structure-Activity Relationship Study on Nalfurafine Analogues.ACS chemical neuroscience · 2022Article
Corrections and comments
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Authors and funding
2 authors.
Funding
Abstract
There is a growing need for highly accurate in silico and in vitro predictive models to facilitate drug discovery and development. Results from in vitro permeation studies across the Caco-2 cell monolayer are commonly used for drug permeability screening in industry and are also accepted as a surrogate for human intestinal permeability measurements by the US FDA to support new drug applications. Countless studies carried out in this cell line with published permeability measurements have enabled the development of many in silico prediction models. We identify several common cases that illustrate how using Caco-2 permeability measurements in these in silico and in vitro predictive models will not correlate with human intestinal permeability and will further lead to inaccuracies in these models. We provide guidelines and recommendations for improving these models to more accurately predict clinically relevant information, thereby enhancing the drug discovery, development, and regulatory approval processes.
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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.