ReviewAdvanced drug delivery reviews2012
Improving the prediction of the brain disposition for orally administered drugs using BDDCS.
Review in Advanced drug delivery reviews, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 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.
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
25 citing papers in PubMed, 72 citations in OpenAlex.
- Development and application of a quantitative physicochemical model of P-gp substrate specificity.Journal of computer-aided molecular design · 2026Article
- Understanding predictions of drug profiles using explainable machine learning models.BioData mining · 2024Article
- Applicability of MDR1 Overexpressing Abcb1KO-MDCKII Cell Lines for Investigating In Vitro Species Differences and Brain Penetration Prediction.Pharmaceutics · 2024Article
- Experimental and Computational Methods to Assess Central Nervous System Penetration of Small Molecules.Molecules (Basel, Switzerland) · 2024Review
- Solubility-Permeability Interplay in Facilitating the Prediction of Drug Disposition Routes, Extent of Absorption, Food Effects, Brain Penetration and Drug Induced Liver Injury Potential.Journal of pharmaceutical sciences · 2023Review
- State of the Art and Uses for the Biopharmaceutics Drug Disposition Classification System (BDDCS): New Additions, Revisions, and Citation References.The AAPS journal · 2022Review
- A curated diverse molecular database of blood-brain barrier permeability with chemical descriptors.Scientific data · 2021Article
- DrugCentral 2021 supports drug discovery and repositioning.Nucleic acids research · 2021Article
- Can BDDCS illuminate targets in drug design?Drug discovery today · 2019Review
- Membrane transporter data to support kinetically-informed chemical risk assessment using non-animal methods: Scientific and regulatory perspectives.Environment international · 2019Review
- Barriers to Effective Drug Treatment for Brain Metastases: A Multifactorial Problem in the Delivery of Precision Medicine.Pharmaceutical research · 2018Review
- Whole body physiologically based modelling of β-blockers in the rat: events in tissues and plasma following an i.v. bolus dose.British journal of pharmacology · 2018Article
- Microdialysis: the Key to Physiologically Based Model Prediction of Human CNS Target Site Concentrations.The AAPS journal · 2017Review
- BDDCS, the Rule of 5 and drugability.Advanced drug delivery reviews · 2016Review
- Reliability of In Vitro and In Vivo Methods for Predicting the Effect of P-Glycoprotein on the Delivery of Antidepressants to the Brain.Clinical pharmacokinetics · 2016Review
- BDDCS Predictions, Self-Correcting Aspects of BDDCS Assignments, BDDCS Assignment Corrections, and Classification for more than 175 Additional Drugs.The AAPS journal · 2016Review
- Chloroquine inhibits the malignant phenotype of glioblastoma partially by suppressing TGF-beta.Investigational new drugs · 2015Article
- 3D in vitro modeling of the central nervous system.Progress in neurobiology · 2015Review
- Distinguishing between the permeability relationships with absorption and metabolism to improve BCS and BDDCS predictions in early drug discovery.Molecular pharmaceutics · 2014Article
- Prediction of drug disposition on the basis of its chemical structure.Clinical pharmacokinetics · 2013Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 3 institutions in 3 countries.
Funding
Abstract
In modeling blood-brain barrier (BBB) passage, in silico models have yielded ~80% prediction accuracy, and are currently used in early drug discovery. Being derived from molecular structural information only, these models do not take into account the biological factors responsible for the in vivo outcome. Passive permeability and P-glycoprotein (Pgp, ABCB1) efflux have been successfully recognized to impact xenobiotic extrusion from the brain, as Pgp is known to play a role in limiting the BBB penetration of oral drugs in humans. However, these two properties alone fail to explain the BBB penetration for a significant number of marketed central nervous system (CNS) agents. The Biopharmaceutics Drug Disposition Classification System (BDDCS) has proved useful in predicting drug disposition in the human body, particularly in the liver and intestine. Here we discuss the value of using BDDCS to improve BBB predictions of oral drugs. BDDCS class membership was integrated with in vitro Pgp efflux and in silico permeability data to create a simple 3-step classification tree that accurately predicted CNS disposition for more than 90% of 153 drugs in our data set. About 98% of BDDCS class 1 drugs were found to markedly distribute throughout the brain; this includes a number of BDDCS class 1 drugs shown to be Pgp substrates. This new perspective provides a further interpretation of how Pgp influences the sedative effects of H1-histamine receptor antagonists.
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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.