Static Model–Based Assessment of OATP1B1-Mediated Drug Interactions with Preincubation-Dependent Inhibitors Based on Inactivation and Recovery Kinetics

T Taguchi, Y Masuo, A Futatsugi, Y Kato - Drug Metabolism and Disposition, 2020 - ASPET
… Moreover, a systematic assessment of the interaction between CsA and the OATP substrate
pravastatin has been performed in rats, revealing that this interaction appears to be long-…

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
… that various observed clinical drugdrug interactions (DDIs) … Of note, DDIs involving the
inhibition of hepatic OATP1B1/3 (… at a low substrate concentration relative to the substrate

Variability in In Vitro OATP1B1/1B3 Inhibition Data: Impact of Incubation Conditions on Variability and Subsequent Drug Interaction Predictions

SJ McFeely, TK Ritchie… - Clinical and …, 2020 - Wiley Online Library
… clinically relevant substrates and/or multiple substrates could … OATPs) 1B1 and 1B3 are
the major hepatic uptake transporters involved in the distribution and disposition of many drugs

Identification and quantitation of enzyme and transporter contributions to hepatic clearance for the assessment of potential drug-drug interactions

E Kimoto, RS Obach, MVS Varma - Drug Metabolism and …, 2020 - Elsevier
Drug-drug interactions (DDIs) involving drug-metabolizing enzymes and membrane transporters
can lead to alteration in substrate drug (victim) … f t for OATP substrates was assessed by …

Evaluation of the Potential for Cytochrome P450 and Transporter-Mediated Drug-Drug Interactions for Cilofexor, a Selective Nonsteroidal Farnesoid X Receptor (FXR) …

I Younis, E Weber, C Nelson, BJ Kirby, G Shen… - Clinical …, 2023 - Springer
… Our objective was to evaluate potential drug-drug interactions of cilofexor as a victim and
as … (CYP3A substrate), atorvastatin (mixed OATP/CYP3A substrate), dabigatran etexilate (P-gp …

Investigation of fluorescent substrates and substrate-dependent interactions of a drug transporter organic anion transporting polypeptide 2B1 (OATP2B1)

T Kawasaki, Y Shiozaki, N Nomura, K Kawai… - Pharmaceutical …, 2020 - Springer
OATP isoforms such as OATP1B1 and OATP1B3, aliskiren, celiprolol, and pemetrexed are
selective for OATP2B1 (5). As OATP2B1 substrates … which to conduct drug interaction studies (…

Clinically relevant OATP2B1 inhibitors in marketed drug space

MS Unger, J Mudunuru, M Schwab, C Hopf… - Molecular …, 2019 - ACS Publications
… of substrate drug pharmacokinetics and thereby sites of clinical drugdrug interactions (DDIs…
, evaluation of transport and inhibition of these two OATPs is standard in contemporary drug

Physiologically-based pharmacokinetic (PBPK) modelling of transporter mediated drug absorption, clearance and drug-drug interactions

KS Taskar, I Harada, RV Alluri - Current Drug Metabolism, 2021 - ingentaconnect.com
… To enable the identification of OATP substrates during the discovery phase, cell lines
expressing OATP1B1 or OATP1B3 can be used and the uptake CLint from these systems can be …

[PDF][PDF] A Clinical Practice Perspective on the Evaluation of OATP1B1‐associated Drug Interactions

CK Stäuble, ML Lampert, SS Allemann… - Clinical …, 2024 - researchgate.net
… for the identified in vivo OATP1B1 substrates and/ … gathered on the interaction with OATP1B1
is transferred into the … the OATP1B1 substrate pemafibrate, indicating OATP1B1 inhibition (…

Interactions of potential anti-COVID-19 compounds with multispecific ABC and OATP drug transporters

Á Telbisz, C Ambrus, O Mózner, E Szabó, G Várady… - Pharmaceutics, 2021 - mdpi.com
… , labeled substrates and the investigated … drug interactions. The modulation of the ATP-dependent
vesicular uptake of a specific ABCB1 probe substrate directly reveals drug interactions