Clinical probes and endogenous biomarkers as substrates for transporter drug‐drug interaction evaluation: perspectives from the international transporter consortium

X Chu, M Liao, H Shen, K Yoshida… - Clinical …, 2018 - Wiley Online Library
Drug transporters can govern the absorption, distribution, metabolism, and excretion of
substrate drugs and endogenous substances. Investigations to examine their potential …

Regulation of drug transport proteins—From mechanisms to clinical impact: A white paper on behalf of the international transporter consortium

KLR Brouwer, R Evers, E Hayden, S Hu… - Clinical …, 2022 - Wiley Online Library
Membrane transport proteins are involved in the absorption, disposition, efficacy, and/or
toxicity of many drugs. Numerous mechanisms (eg, nuclear receptors, epigenetic gene …

[HTML][HTML] Recent advances in the translation of drug metabolism and pharmacokinetics science for drug discovery and development

Y Lai, X Chu, L Di, W Gao, Y Guo, X Liu, C Lu… - … Pharmaceutica Sinica B, 2022 - Elsevier
Drug metabolism and pharmacokinetics (DMPK) is an important branch of pharmaceutical
sciences. The nature of ADME (absorption, distribution, metabolism, excretion) and PK …

Physiologically‐based pharmacokinetic models for evaluating membrane transporter mediated drug–drug interactions: current capabilities, case studies, future …

KS Taskar, V Pilla Reddy, H Burt… - Clinical …, 2020 - Wiley Online Library
Physiologically‐based pharmacokinetic (PBPK) modeling has been extensively used to
quantitatively translate in vitro data and evaluate temporal effects from drug–drug …

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 …

Dose‐dependent inhibition of OATP1B by rifampicin in healthy volunteers: comprehensive evaluation of candidate biomarkers and OATP1B probe drugs

D Mori, E Kimoto, B Rago, Y Kondo… - Clinical …, 2020 - Wiley Online Library
To address the most appropriate endogenous biomarker for drug–drug interaction risk
assessment, eight healthy subjects received an organic anion transporting polypeptide 1B …

Comparative study of the dose-dependence of OATP1B inhibition by rifampicin using probe drugs and endogenous substrates in healthy volunteers

I Takehara, T Yoshikado, K Ishigame, D Mori… - Pharmaceutical …, 2018 - Springer
Purpose To evaluate association of the dose-dependent effect of rifampicin, an OATP1B
inhibitor, on the plasma concentration–time profiles among OATP1B substrates drugs and …

[HTML][HTML] Current status and future directions of high-throughput ADME screening in drug discovery

WZ Shou - Journal of Pharmaceutical Analysis, 2020 - Elsevier
During the last decade high-throughput in vitro absorption, distribution, metabolism and
excretion (HT-ADME) screening has become an essential part of any drug discovery effort of …

[HTML][HTML] Evaluation of pharmacokinetic drug–drug interactions: a review of the mechanisms, in vitro and in silico approaches

Y Peng, Z Cheng, F Xie - Metabolites, 2021 - mdpi.com
Pharmacokinetic drug–drug interactions (DDIs) occur when a drug alters the absorption,
transport, distribution, metabolism or excretion of a co-administered agent. The occurrence …

Clinical investigation of coproporphyrins as sensitive biomarkers to predict mild to strong OATP1B-mediated drug–drug interactions

A Kunze, EN Ediage, L Dillen, M Monshouwer… - Clinical …, 2018 - Springer
Abstract Introduction Coproporphyrin (CP) I and III have recently been proposed as
endogenous clinical biomarkers to predict organic anion-transporting polypeptide 1B …