Intestinal drug transporters: an overview
The importance of drug transporters as one of the determinants of pharmacokinetics has
become increasingly evident [1]. While much research has been conducted focusing the role …
become increasingly evident [1]. While much research has been conducted focusing the role …
Drug-permeability and transporter assays in Caco-2 and MDCK cell lines
DA Volpe - Future medicinal chemistry, 2011 - Taylor & Francis
The human colon adenocarcinoma Caco-2 and Madin–Darby canine kidney epithelial cell
lines provide in vitro tools to assess a drug's permeability and transporter interactions during …
lines provide in vitro tools to assess a drug's permeability and transporter interactions during …
Integrated Gut and Liver Microphysiological Systems for Quantitative In Vitro Pharmacokinetic Studies
Investigation of the pharmacokinetics (PK) of a compound is of significant importance during
the early stages of drug development, and therefore several in vitro systems are routinely …
the early stages of drug development, and therefore several in vitro systems are routinely …
ADME properties evaluation in drug discovery: prediction of Caco-2 cell permeability using a combination of NSGA-II and boosting
The Caco-2 cell monolayer model is a popular surrogate in predicting the in vitro human
intestinal permeability of a drug due to its morphological and functional similarity with human …
intestinal permeability of a drug due to its morphological and functional similarity with human …
Brivaracetam, a selective high‐affinity synaptic vesicle protein 2A (SV 2A) ligand with preclinical evidence of high brain permeability and fast onset of action
JM Nicolas, J Hannestad, D Holden, S Kervyn… - …, 2016 - Wiley Online Library
Objective Rapid distribution to the brain is a prerequisite for antiepileptic drugs used for
treatment of acute seizures. The preclinical studies described here investigated the high …
treatment of acute seizures. The preclinical studies described here investigated the high …
Drug Discovery and Regulatory Considerations for Improving In Silico and In Vitro Predictions that Use Caco-2 as a Surrogate for Human Intestinal Permeability …
CA Larregieu, LZ Benet - The AAPS journal, 2013 - Springer
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 …
facilitate drug discovery and development. Results from in vitro permeation studies across …
Molecular dynamics simulations and experimental studies reveal differential permeability of withaferin-A and withanone across the model cell membrane
Poor bioavailability due to the inability to cross the cell membrane is one of the major
reasons for the failure of a drug in clinical trials. We have used molecular dynamics …
reasons for the failure of a drug in clinical trials. We have used molecular dynamics …
Multi-functional scaling methodology for translational pharmacokinetic and pharmacodynamic applications using integrated microphysiological systems (MPS)
Microphysiological systems (MPS) provide relevant physiological environments in vitro for
studies of pharmacokinetics, pharmacodynamics and biological mechanisms for …
studies of pharmacokinetics, pharmacodynamics and biological mechanisms for …
Reliable prediction of Caco-2 permeability by supervised recursive machine learning approaches
G Falcón-Cano, C Molina, MÁ Cabrera-Pérez - Pharmaceutics, 2022 - mdpi.com
The heterogeneity of the Caco-2 cell line and differences in experimental protocols for
permeability assessment using this cell-based method have resulted in the high variability of …
permeability assessment using this cell-based method have resulted in the high variability of …
Systems biological approach of molecular descriptors connectivity: optimal descriptors for oral bioavailability prediction
SSSJ Ahmed, V Ramakrishnan - PLoS One, 2012 - journals.plos.org
Background Poor oral bioavailability is an important parameter accounting for the failure of
the drug candidates. Approximately, 50% of developing drugs fail because of unfavorable …
the drug candidates. Approximately, 50% of developing drugs fail because of unfavorable …