A clinical cassette dosing study for evaluating the contribution of hepatic OATPs and CYP3A to drug-drug interactions

T Yoshikado, K Maeda, S Furihata, H Terashima… - Pharmaceutical …, 2017 - Springer
… , and clarithromycin combined with midazolam as the substrate. Bosentan (6), repaglinide
(7… substrates of hepatic OATPs. Clarithromycin was reported not to be a substrate for OATP1B1

Prediction of the in vivo OATP1B1-mediated drugdrug interaction potential of an investigational drug against a range of statins

P Sharma, CJ Butters, V Smith, R Elsby… - European journal of …, 2012 - Elsevier
… Apparent K m values for the OATP1B1-mediated transport of [ 3 H] substrates were determined
prior to their use as probes in inhibition studies, and ranged from 0.6 to 29 μM for statins. …

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

P Sharma, VE Holmes, R Elsby, C Lambert, D Surry - Xenobiotica, 2010 - Taylor & Francis
… empty vector was devoid of OATP1B1 expression and is named … a tool to assess OATP1B1
substrates and inhibition was conducted … of substrates and inhibitors of OATP1B1 in the drug-…

In vitro assessment of drug-drug interaction potential of boceprevir associated with drug metabolizing enzymes and transporters

X Chu, X Cai, D Cui, C Tang, A Ghosal, G Chan… - Drug Metabolism and …, 2013 - ASPET
… of organic anion transporting polypeptide (OATP) 1B1 and 1B3, with … BOC was a substrate
for Pgp and BCRP but not for OATP1B1OATP1B1 in vitro inhibition by several known OATP

Hepatic uptake of atorvastatin: influence of variability in transporter expression on uptake clearance and drug-drug interactions

A Vildhede, M Karlgren, EK Svedberg… - Drug metabolism and …, 2014 - ASPET
… capacity was determined with atorvastatin as the victim drug. There were clear differences
in OATP inhibition pattern when using atorvastatin as substrate instead of prototypical model …

… of organic anion transporting polypeptides (OATP) 1B1-and OATP1B3-mediated transport: an updated review in the context of OATP-mediated drug-drug interactions

K Alam, A Crowe, X Wang, P Zhang, K Ding… - International journal of …, 2018 - mdpi.com
… /1B3-mediated DDIs in order to avoid unwanted adverse effects of drugs that are OATP
substrates due to their altered pharmacokinetics. Growing evidences suggest that the transport …

Fluorescence-based assays for the assessment of drug interaction with the human transporters OATP1B1 and OATP1B3

D Bednarczyk - Analytical biochemistry, 2010 - Elsevier
OATP1B1. Therefore, it was of value to continue to search for and identify a suitable substrate
for OATP1B1 … a potential candidate for use as an OATP1B1 substrate in vitro. There are a …

The use of transporter probe drug cocktails for the assessment of transporter-based drugdrug interactions in a clinical setting—proposal of a four component …

T Ebner, N Ishiguro, ME Taub - Journal of pharmaceutical sciences, 2015 - Elsevier
… inhibition of drug transporters. We propose a cocktail consisting of the following substrates to
… These results clearly suggest that furosemide is a substrate of OAT1, OAT3, OATP1B1, and …

Organic anion transporting polypeptide (OATP) 1B1 and OATP1B3 as important regulators of the pharmacokinetics of substrate drugs

K Maeda - Biological and Pharmaceutical Bulletin, 2015 - jstage.jst.go.jp
… of OATP substrates is often hepatic uptake. Because of their broad substrate specificities,
once the functions of OATP1B1 … of special occasions such as drugdrug interactions (DDI) and …

Grapefruit juice, a glass full of drug interactions?

BJ Kirby, JD Unadkat - Clinical Pharmacology & Therapeutics, 2007 - Wiley Online Library
… exposure (the former increasing and the latter decreasing drug exposure), which … prediction
of OATP drug interactions. The OATP family has a broad spectrum of substrates ranging from …