[PDF][PDF] Extended Clearance Classification System (ECCS) informed approach for evaluating investigational drugs as substrates of drug transporters
MV Varma, AF El‐Kattan, B Feng… - Clinical …, 2017 - researchgate.net
Drug transporters are recognized widely for their role in clinical pharmacokinetics and drug–
drug interactions (DDIs). This has provided impetus to the inclusion of transporter substrate …
drug interactions (DDIs). This has provided impetus to the inclusion of transporter substrate …
In vitro–in vivo extrapolation scaling factors for intestinal P-glycoprotein and breast cancer resistance protein: part I: a cross-laboratory comparison of transporter …
Over the last 5 years the quantification of transporter-protein absolute abundances has
dramatically increased in parallel to the expanded use of in vitro–in vivo extrapolation …
dramatically increased in parallel to the expanded use of in vitro–in vivo extrapolation …
Intracellular metabolomics identifies efflux transporter inhibitors in a routine Caco-2 cell permeability assay—Biological implications
A Naseem, A Pal, S Gowan, Y Asad, A Donovan… - Cells, 2022 - mdpi.com
Caco-2 screens are routinely used in laboratories to measure the permeability of
compounds and can identify substrates of efflux transporters. In this study, we hypothesized …
compounds and can identify substrates of efflux transporters. In this study, we hypothesized …
Development of novel, 384-well high-throughput assay panels for human drug transporters: drug interaction and safety assessment in support of discovery research
H Tang, DR Shen, YH Han, Y Kong… - Journal of …, 2013 - journals.sagepub.com
Transporter proteins are known to play a critical role in affecting the overall absorption,
distribution, metabolism, and excretion characteristics of drug candidates. In addition to …
distribution, metabolism, and excretion characteristics of drug candidates. In addition to …
Insights in drug metabolism and transport: 2021
J Piñeiro-Llanes, DE Stec, R Cristofoletti - Frontiers in Pharmacology, 2023 - frontiersin.org
Improving drug translation is becoming a top priority as research and development costs
keep increasing. It typically takes 10–20 years and a couple of billion dollars to bring a new …
keep increasing. It typically takes 10–20 years and a couple of billion dollars to bring a new …
Methodologies to study human intestinal absorption. A review
CHM Versantvoort, CJM Rompelberg, A Sips - 2000 - rivm.openrepository.com
Concepts in risk assessment practice are expressed in terms of external exposure, while
internal exposure determines whether toxic effects will occur. Often only a fraction of the …
internal exposure determines whether toxic effects will occur. Often only a fraction of the …
Identification and quantitation of enzyme and transporter contributions to hepatic clearance for the assessment of potential drug-drug interactions
E Kimoto, RS Obach, MVS Varma - Drug Metabolism and …, 2020 - Elsevier
Drug-drug interactions (DDIs) involving drug-metabolizing enzymes and membrane
transporters can lead to alteration in substrate drug (victim) exposure, and can influence the …
transporters can lead to alteration in substrate drug (victim) exposure, and can influence the …
Consumer product in vitro digestion model: bioaccessibility of contaminants and its application in risk assessment
EFA Brandon, AG Oomen, CJM Rompelberg… - Regulatory Toxicology …, 2006 - Elsevier
This paper describes the applicability of in vitro digestion models as a tool for consumer
products in (ad hoc) risk assessment. In current risk assessment, oral bioavailability from a …
products in (ad hoc) risk assessment. In current risk assessment, oral bioavailability from a …
Transporter biology in drug approval: regulatory aspects
K Maeda, Y Sugiyama - Molecular Aspects of Medicine, 2013 - Elsevier
Previous in vitro and clinical research have indicated that a wide variety of drug transporters
as well as metabolic enzymes dominate the pharmacokinetics of drugs and that some drugs …
as well as metabolic enzymes dominate the pharmacokinetics of drugs and that some drugs …
In-vitro physiologically based extraction of solid materials: Do we have reliable analytical methods for bioaccessibility studies of emerging organic contaminants?
C Rodríguez-Navas, M Rosende, M Miró - TrAC Trends in Analytical …, 2017 - Elsevier
In-vitro oral bioaccessibility tests do remain alluring as viable tools for fast assessment of
potential human exposure to environmental contaminants to comply with the ethical …
potential human exposure to environmental contaminants to comply with the ethical …