[HTML][HTML] Membrane transporter data to support kinetically-informed chemical risk assessment using non-animal methods: Scientific and regulatory perspectives

LA Clerbaux, A Paini, A Lumen… - Environment …, 2019 - Elsevier
Humans are continuously exposed to low levels of thousands of industrial chemicals, most
of which are poorly characterised in terms of their potential toxicity. The new paradigm in …

[HTML][HTML] Capturing the applicability of in vitro-in silico membrane transporter data in chemical risk assessment and biomedical research

LA Clerbaux, S Coecke, A Lumen, T Kliment… - Science of the Total …, 2018 - Elsevier
Costs, scientific and ethical concerns related to animal tests for regulatory decision-making
have stimulated the development of alternative methods. When applying alternative …

New approach methodologies (NAMs) for human-relevant biokinetics predictions: Meeting the paradigm shift in toxicology towards an animal-free chemical risk …

A Punt, H Bouwmeester, BJ Blaauboer, S Coecke… - Altex, 2020 - research.utwente.nl
For almost fifteen years, the availability and regulatory acceptance of new approach
methodologies (NAMs) to assess the absorption, distribution, metabolism and excretion …

Human variability in influx and efflux transporters in relation to uncertainty factors for chemical risk assessment

K Darney, L Turco, FM Buratti, E Di Consiglio… - Food and Chemical …, 2020 - Elsevier
Transporters are divided into the ABC and SLC super-families, mediating the cellular efflux
and influx of various xenobiotic and endogenous substrates. Here, an extensive literature …

Studying the right transporter at the right time: an in vitro strategy for assessing drug-drug interaction risk during drug discovery and development

R Elsby, H Atkinson, P Butler… - Expert Opinion on Drug …, 2022 - Taylor & Francis
Introduction Transporters are significant in dictating drug pharmacokinetics, thus inhibition of
transporter function can alter drug concentrations resulting in drug-drug interactions (DDIs) …

Expanding Role of Endogenous Biomarkers for Assessment of Transporter Activity in Drug Development: Current Applications and Future Horizon

V Arya, JD Ma, KE Kvitne - Pharmaceutics, 2024 - mdpi.com
The evaluation of transporter-mediated drug–drug interactions (DDIs) during drug
development and post-approval contributes to benefit–risk assessment and helps formulate …

Environmental chemicals as substrates, inhibitors or inducers of drug transporters: implication for toxicokinetics, toxicity and pharmacokinetics

O Fardel, E Kolasa, M Le Vee - Expert Opinion on Drug Metabolism …, 2012 - Taylor & Francis
Introduction: Membrane drug transporters are well recognized as important contributing
factors to pharmacokinetics, notably involved in drug–drug interactions. Besides drugs …

In vitro and in vivo approaches to characterize transporter-mediated disposition in drug discovery

B Feng, MV Varma, C Costales, H Zhang… - Expert opinion on drug …, 2014 - Taylor & Francis
Introduction: It is becoming increasingly evident that transporters play an important role in
the absorption, distribution and elimination of many drugs. Different approaches have been …

Mitigating permeability-mediated risks in drug discovery

J Wang, S Skolnik - Expert Opinion on Drug Metabolism & …, 2010 - Taylor & Francis
Importance of the field: Adequate permeability is essential for good oral absorption and
proper interpretation of pharmacokinetic and pharmacological data. Permeability-limiting …

Involvement of drug transporters in organ toxicity: the fundamental basis of drug discovery and development

Y Cheng, A El-Kattan, Y Zhang, AS Ray… - Chemical research in …, 2016 - ACS Publications
Membrane transporters play a pivotal role in many organs to maintain their normal
physiological functions and contribute significantly to drug absorption, distribution, and …