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) …

Preincubation Time-Dependent, Long-Lasting Inhibition of Drug Transporters and Impact on the Prediction of Drug− Drug Interactions

Y Nozaki, S Izumi - Drug Metabolism and Disposition, 2023 - ASPET
Transporter-mediated drug− drug interaction (DDI) is of clinical concern, and the quantitative
prediction of DDIs is an indispensable part of drug development. Cell-based inhibition …

Effect of hepatic impairment on OATP1B activity: quantitative pharmacokinetic analysis of endogenous biomarker and substrate drugs

J Lin, E Kimoto, S Yamazaki… - Clinical …, 2023 - Wiley Online Library
Hepatic impairment (HI) is known to modulate drug disposition and may lead to elevated
plasma exposure. The aim of this study was to quantitate the in vivo OATP1B‐mediated …

Using Endogenous Biomarkers to Derisk Assessment of Transporter‐Mediated Drug‐Drug Interactions: A Scientific Perspective

V Arya, KS Reynolds, X Yang - The Journal of Clinical …, 2022 - Wiley Online Library
Comprehensive characterization of transporter mediated drug‐drug interactions (DDIs) is
important to formulate clinical management strategies and ensure the safe and effective use …

Membrane transporters in drug development and as determinants of precision medicine

A Galetin, KLR Brouwer, D Tweedie… - Nature Reviews Drug …, 2024 - nature.com
The effect of membrane transporters on drug disposition, efficacy and safety is now well
recognized. Since the initial publication from the International Transporter Consortium …

Effect of a Ketohexokinase Inhibitor (PF‐06835919) on In Vivo OATP1B Activity: Integrative Risk Assessment Using Endogenous Biomarker and a Probe Drug

DA Tess, E Kimoto, A King‐Ahmad… - Clinical …, 2022 - Wiley Online Library
PF‐06835919 is a first‐in‐class ketohexokinase inhibitor (KHKi), recently under
development for the treatment of metabolic and fatty liver diseases, which inhibited organic …

Evaluation of the selectivity of several organic anion transporting polypeptide 1B biomarkers using relative activity factor method

GH Chan, R Houle, J Zhang, R Katwaru, Y Li… - Drug Metabolism and …, 2023 - ASPET
In recent years, some endogenous substrates of organic anion transporting polypeptide 1B
(OATP1B) have been identified and characterized as potential biomarkers to assess …

Change of metformin concentrations in the liver as a pharmacological target site of metformin after long-term combined treatment with ginseng berry extract

CW Lee, BH You, S Yim, SY Han, HS Chae… - Frontiers in …, 2023 - frontiersin.org
Metformin as an oral glucose-lowering drug is used to treat type 2 diabetic mellitus.
Considering the relatively high incidence of cardiovascular complications and other …

Utilization of OATP1B Biomarker Coproporphyrin‐I to Guide Drug–Drug Interaction Risk Assessment: Evaluation by the Pharmaceutical Industry

R Kikuchi, PP Chothe, X Chu, F Huth… - Clinical …, 2023 - Wiley Online Library
Drug–drug interactions (DDIs) involving hepatic organic anion transporting polypeptides
1B1/1B3 (OATP1B) can be substantial, however, challenges remain for predicting …

[HTML][HTML] Use of In Vivo Imaging and Physiologically-Based Kinetic Modelling to Predict Hepatic Transporter Mediated Drug–Drug Interactions in Rats

N Melillo, D Scotcher, JG Kenna, C Green, CDG Hines… - Pharmaceutics, 2023 - mdpi.com
Gadoxetate, a magnetic resonance imaging (MRI) contrast agent, is a substrate of organic-
anion-transporting polypeptide 1B1 and multidrug resistance-associated protein 2. Six …