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 …
and toxicological characteristics of drugs. The development of validated in vitro transporter …
Investigation of the impact of substrate selection on in vitro organic anion transporting polypeptide 1B1 inhibition profiles for the prediction of drug-drug interactions
The risk assessment of organic anion transporting polypeptide (OATP) 1B1–mediated drug-
drug interactions (DDIs) is an indispensable part of drug development. We previously …
drug interactions (DDIs) is an indispensable part of drug development. We previously …
Changes in organic anion transporting polypeptide uptake in HEK293 overexpressing cells in the presence and absence of human plasma
Generating accurate in vitro data is crucial for in vitro to in vivo extrapolation and
pharmacokinetic predictions. The use of human embryonic kidney (HEK) 293 cells …
pharmacokinetic predictions. The use of human embryonic kidney (HEK) 293 cells …
Prediction of the in vivo OATP1B1-mediated drug–drug interaction potential of an investigational drug against a range of statins
P Sharma, CJ Butters, V Smith, R Elsby… - European journal of …, 2012 - Elsevier
To support drug development, the drug–drug interaction potential (DDI) of an investigational
drug (AZX) was assessed against the probe estradiol 17β-glucuronide as well as against …
drug (AZX) was assessed against the probe estradiol 17β-glucuronide as well as against …
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 …
prediction of DDIs is an indispensable part of drug development. Cell-based inhibition …
Substrate-dependent inhibition of organic anion transporting polypeptide 1B1: comparative analysis with prototypical probe substrates estradiol-17β-glucuronide …
Organic anion transporting polypeptide (OATP) 1B1 plays an important role in the hepatic
uptake of many drugs, and the evaluation of OATP1B1-mediated drug-drug interactions …
uptake of many drugs, and the evaluation of OATP1B1-mediated drug-drug interactions …
Quantitative prediction of human renal clearance and drug-drug interactions of organic anion transporter substrates using in vitro transport data: a relative activity …
S Mathialagan, MA Piotrowski, DA Tess, B Feng… - Drug Metabolism and …, 2017 - ASPET
Organic anion transporters (OATs) are important in the renal secretion, and thus, the
clearance, of many drugs; and their functional change can result in pharmacokinetic …
clearance, of many drugs; and their functional change can result in pharmacokinetic …
Recent advances in preclinical in vitro approaches towards quantitative prediction of hepatic clearance and drug-drug interactions involving organic anion …
Y Nozaki, S Izumi - Drug Metabolism and Pharmacokinetics, 2020 - Elsevier
Hepatic uptake mediated by organic anion transporting polypeptide (OATP) 1B1 and 1B3
can serve as a major elimination pathway for various anionic drugs and as a site of drug …
can serve as a major elimination pathway for various anionic drugs and as a site of drug …
Meta-analysis of expression of hepatic organic anion–transporting polypeptide (OATP) transporters in cellular systems relative to human liver tissue
J Badée, B Achour, A Rostami-Hodjegan… - Drug Metabolism and …, 2015 - ASPET
Organic anion–transporting polypeptide (OATP) 1B1, OATP1B3, and OATP2B1 transporters
play an important role in hepatic drug disposition. Recently, an increasing number of studies …
play an important role in hepatic drug disposition. Recently, an increasing number of studies …
Experimental and modeling evidence supporting the trans-inhibition mechanism for preincubation time-dependent, long-lasting inhibition of organic anion transporting …
Cyclosporine A (CsA) and rifampin are potent inhibitors of organic anion transporting
polypeptide (OATP) 1B1 and are widely used to assess the risk for drug-drug interactions …
polypeptide (OATP) 1B1 and are widely used to assess the risk for drug-drug interactions …