The critical role of passive permeability in designing successful drugs
Passive permeability is a key property in drug disposition and delivery. It is critical for
gastrointestinal absorption, brain penetration, renal reabsorption, defining clearance …
gastrointestinal absorption, brain penetration, renal reabsorption, defining clearance …
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 …
quantitatively translate in vitro data and evaluate temporal effects from drug–drug …
The next frontier in ADME science: Predicting transporter-based drug disposition, tissue concentrations and drug-drug interactions in humans
Predicting transporter-based drug clearance (CL) and tissue concentrations (TC) in humans
is important to reduce the risk of failure during drug development. In addition, when …
is important to reduce the risk of failure during drug development. In addition, when …
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 …
transport, distribution, metabolism or excretion of a co-administered agent. The occurrence …
Successful and unsuccessful prediction of human hepatic clearance for lead optimization
Development of new chemical entities is costly, time-consuming, and has a low success
rate. Accurate prediction of pharmacokinetic properties is critical to progress compounds …
rate. Accurate prediction of pharmacokinetic properties is critical to progress compounds …
Clinical relevance of hepatic and renal P‐gp/BCRP inhibition of drugs: An international transporter consortium perspective
The role of P‐glycoprotein (P‐gp) and breast cancer resistance protein (BCRP) in drug–drug
interactions (DDIs) and limiting drug absorption as well as restricting the brain penetration of …
interactions (DDIs) and limiting drug absorption as well as restricting the brain penetration of …
Effect of cyclosporin A and impact of dose staggering on OATP1B1/1B3 endogenous substrates and drug probes for assessing clinical drug interactions
T Mochizuki, MJ Zamek‐Gliszczynski… - Clinical …, 2022 - Wiley Online Library
This study was designed to assess the quantitative performance of endogenous biomarkers
for organic anion transporting polypeptide (OATP) 1B1/1B3‐mediated drug‐drug …
for organic anion transporting polypeptide (OATP) 1B1/1B3‐mediated drug‐drug …
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 …
Is the protein-mediated uptake of drugs by organic anion transporting polypeptides a real phenomenon or an artifact?
Plasma proteins or human serum albumin (HSA) have been reported to increase the in vitro
intrinsic uptake clearance (CLint, uptake) of drugs by hepatocytes or organic anion …
intrinsic uptake clearance (CLint, uptake) of drugs by hepatocytes or organic anion …
[HTML][HTML] Investigating the relevance of CYP2J2 inhibition for drugs known to cause intermediate to high risk torsades de pointes
JWH Leow, Y Gu, ECY Chan - European Journal of Pharmaceutical …, 2023 - Elsevier
Abstract Cardiac cytochrome P450 2J2 (CYP2J2) metabolizes endogenous polyunsaturated
fatty acid, arachidonic acid (AA), to bioactive regioisomeric epoxyeicosatrienoic acid (EET) …
fatty acid, arachidonic acid (AA), to bioactive regioisomeric epoxyeicosatrienoic acid (EET) …