Clinical implications of altered drug transporter abundance/function and PBPK modeling in specific populations: an ITC perspective

X Chu, B Prasad, S Neuhoff, K Yoshida… - Clinical …, 2022 - Wiley Online Library
The role of membrane transporters on pharmacokinetics (PKs), drug–drug interactions
(DDIs), pharmacodynamics (PDs), and toxicity of drugs has been broadly recognized …

Validation of cell-based OATP1B1 assays to assess drug transport and the potential for drug–drug interaction to support regulatory submissions

P Sharma, VE Holmes, R Elsby, C Lambert, D Surry - Xenobiotica, 2010 - Taylor & Francis
Transporters are carrier proteins that may influence pharmacokinetic, pharmacodynamic,
and toxicological characteristics of drugs. The development of validated in vitro transporter …

Progress in the Quantitative Assessment of Transporter-Mediated Drug–Drug Interactions Using Endogenous Substrates in Clinical Studies

T Mochizuki, H Kusuhara - Drug Metabolism and Disposition, 2023 - ASPET
Variations in drug transporter activities, caused by genetic polymorphism and drug–drug
interactions (DDIs), alter the systemic exposure of substrate drugs, leading to differences in …

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 …

Clinical importance of OATP1B1 and OATP1B3 in drug–drug interactions

Y Shitara - Drug metabolism and pharmacokinetics, 2011 - jstage.jst.go.jp
OATP1B1 and OATP1B3 are transporters that are expressed on the sinusoidal membrane of
hepatocytes; they accept a number of therapeutic reagents as their substrates. In vitro and in …

In silico and in vitro modeling of hepatocyte drug transport processes: importance of ABCC2 expression levels in the disposition of carboxydichlorofluroscein

K Howe, GG Gibson, T Coleman, N Plant - Drug Metabolism and Disposition, 2009 - ASPET
The impact of transport proteins in the disposition of chemicals is becoming increasingly
evident. Alteration in disposition can cause altered pharmacokinetic and pharmacodynamic …

Evaluation and quantitative prediction of renal transporter‐mediated drug‐drug interactions

B Feng, MV Varma - The Journal of Clinical Pharmacology, 2016 - Wiley Online Library
With numerous drugs cleared renally, inhibition of uptake transporters localized on the
basolateral membrane of renal proximal tubule cells, eg, organic anion transporters (OATs) …

In vitro-in vivo extrapolation of transporter-mediated clearance in the liver and kidney

H Kusuhara, Y Sugiyama - Drug metabolism and pharmacokinetics, 2009 - jstage.jst.go.jp
Transporters govern drug movement into and out of tissues, thereby playing an important
role in drug disposition in plasma and to the site of action. The molecular cloning of such …

Role of Oatp2b1 in drug absorption and drug-drug interactions

M Chen, S Hu, Y Li, AA Gibson, Q Fu, SD Baker… - Drug Metabolism and …, 2020 - ASPET
The organic anion transporting polypeptide (OATP) 2B1 is localized on the basolateral
membrane of hepatocytes and is expressed in enterocytes. Based on its distribution pattern …

Future directions for drug transporter modelling

S Ekins, GF Ecker, P Chiba, PW Swaan - Xenobiotica, 2007 - Taylor & Francis
Since the late 1980s computational methods such as quantitative structure–activity
relationship (QSAR) and pharmacophore approaches have become more widely applied to …