Clinical aspects of transporter‐mediated drug–drug interactions

A Gessner, J König, MF Fromm - Clinical Pharmacology & …, 2019 - Wiley Online Library
Drug transporters play an essential role in disposition and effects of multiple drugs. Plasma
concentrations of the victim drug can be modified by drug–drug interactions occurring in …

The next frontier in ADME science: Predicting transporter-based drug disposition, tissue concentrations and drug-drug interactions in humans

F Storelli, M Yin, AR Kumar, MK Ladumor… - Pharmacology & …, 2022 - Elsevier
Predicting transporter-based drug clearance (CL) and tissue concentrations (TC) in humans
is important to reduce the risk of failure during drug development. In addition, when …

Overcoming the shortcomings of the extended-clearance concept: a framework for developing a physiologically-based pharmacokinetic (PBPK) model to select drug …

X Liang, Y Lai - Expert Opinion on Drug Metabolism & Toxicology, 2021 - Taylor & Francis
Introduction: Human pharmacokinetic (PK) prediction can be a significant challenge to drug
candidates undergoing transporter-mediated clearance, when only animal data and in vitro …

Transporter-mediated drug-drug interactions and their significance

X Liu - Drug Transporters in Drug Disposition, Effects and …, 2019 - Springer
Drug transporters are considered to be determinants of drug disposition and effects/toxicities
by affecting the absorption, distribution, and excretion of drugs. Drug transporters are …

The international transporter consortium: summarizing advances in the role of transporters in drug development

KM Giacomini, A Galetin… - Clinical …, 2018 - research.manchester.ac.uk
The past few years have ushered in a wealth of new information on transporter biology,
ranging from the publication of new crystal structures of the human glucose transporters …

Computational approaches to modeling drug transporters

C Chang, PW Swaan - European Journal of Pharmaceutical Sciences, 2006 - Elsevier
Computational modeling has advanced our understanding of drug absorption, tissue
distribution, excretion and toxicity profiles by providing both direct and indirect knowledge of …

Reimagining the framework supporting the static analysis of transporter drug interaction risk; integrated use of biomarkers to generate Pan‐transporter inhibition …

AD Rodrigues - Clinical Pharmacology & Therapeutics, 2023 - Wiley Online Library
Solute carrier (SLC) transporters present as the loci of important drug–drug interactions
(DDIs). Therefore, sponsors generate in vitro half‐maximal inhibitory concentration (IC50) …

Transport− Metabolism Interplay

L Salphati - Molecular pharmaceutics, 2009 - ACS Publications
The hypothesis that cytochrome P450 3A (CYP3A) and P-glycoprotein (P-gp) played
complementary roles in drug absorption and disposition was first proposed 15 years ago. 1 …

[引用][C] Biomarkers Come of Age in Clinical Pharmacology

KM Giacomini - Clinical Pharmacology & Therapeutics, 2023 - Wiley Online Library
Therapeutics in 2001, the National Institutes of Health Biomarkers Definitions Working
Group provided an early definition of a biomarker as “a characteristic that is objectively …

[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 …