Novel method to predict in vivo liver-to-plasma Kpuu for OATP substrates using suspension hepatocytes
K Riccardi, J Lin, Z Li, M Niosi, S Ryu, W Hua… - Drug Metabolism and …, 2017 - ASPET
The ability to predict human liver-to-plasma unbound partition coefficient (Kpuu) is of great
importance to estimate unbound liver concentration, develop PK/PD relationships, predict …
importance to estimate unbound liver concentration, develop PK/PD relationships, predict …
In vitro–in vivo extrapolation scaling factors for intestinal P-glycoprotein and breast cancer resistance protein: part I: a cross-laboratory comparison of transporter …
Over the last 5 years the quantification of transporter-protein absolute abundances has
dramatically increased in parallel to the expanded use of in vitro–in vivo extrapolation …
dramatically increased in parallel to the expanded use of in vitro–in vivo extrapolation …
Successful prediction of in vivo hepatobiliary clearances and hepatic concentrations of rosuvastatin using sandwich-cultured rat hepatocytes, transporter-expressing …
K Ishida, M Ullah, B Tóth, V Juhasz… - Drug Metabolism and …, 2018 - ASPET
We determined whether in vivo transporter-mediated hepatobiliary clearance (CL) and
hepatic concentrations of rosuvastatin (RSV) in the rat could be predicted by transport …
hepatic concentrations of rosuvastatin (RSV) in the rat could be predicted by transport …
Global proteomic analysis of human liver microsomes: rapid characterization and quantification of hepatic drug-metabolizing enzymes
B Achour, H Al Feteisi, F Lanucara… - Drug Metabolism and …, 2017 - ASPET
Many genetic and environmental factors lead to interindividual variations in the metabolism
and transport of drugs, profoundly affecting efficacy and toxicity. Precision dosing, that is …
and transport of drugs, profoundly affecting efficacy and toxicity. Precision dosing, that is …
[HTML][HTML] Fluorescent probes for the dual investigation of MRP2 and OATP1B1 function and drug interactions
V Székely, I Patik, O Ungvári, Á Telbisz… - European Journal of …, 2020 - Elsevier
Detoxification in hepatocytes is a strictly controlled process, in which the governed action of
membrane transporters involved in the uptake and efflux of potentially dangerous molecules …
membrane transporters involved in the uptake and efflux of potentially dangerous molecules …
[HTML][HTML] Key to Opening Kidney for In Vitro–In Vivo Extrapolation Entrance in Health and Disease: Part I: In Vitro Systems and Physiological Data
D Scotcher, C Jones, M Posada, A Rostami-Hodjegan… - The AAPS journal, 2016 - Springer
The programme for the 2015 AAPS Annual Meeting and Exhibition (Orlando, FL; 25–29
October 2015) included a sunrise session presenting an overview of the state-of-the-art tools …
October 2015) included a sunrise session presenting an overview of the state-of-the-art tools …
Clarithromycin, midazolam, and digoxin: application of PBPK modeling to gain new insights into drug–drug interactions and co-medication regimens
D Moj, N Hanke, H Britz, S Frechen, T Kanacher… - The AAPS journal, 2017 - Springer
Clarithromycin is a substrate and mechanism-based inhibitor of cytochrome P450 (CYP)
3A4 as well as a substrate and competitive inhibitor of P-glycoprotein (P-gp) and organic …
3A4 as well as a substrate and competitive inhibitor of P-glycoprotein (P-gp) and organic …
Human hepatic transporter signature peptides for quantitative targeted absolute proteomics: selection, digestion efficiency, and peptide stability
Purpose Quantitative targeted absolute proteomics (QTAP) quantifies proteins by measuring
the signature peptides produced from target proteins by trypsin digestion. The selection of …
the signature peptides produced from target proteins by trypsin digestion. The selection of …
microRNA-192 suppresses the expression of the farnesoid X receptor
R Krattinger, A Boström, HB Schiöth… - American Journal …, 2016 - journals.physiology.org
Farnesoid X receptor (FXR, NR1H4) plays an important role in the regulation of bile acid
homeostasis in liver and intestine and may exert protective effects against certain forms of …
homeostasis in liver and intestine and may exert protective effects against certain forms of …
Sex-, age-, and race/ethnicity-dependent variations in drug-processing and NRF2-regulated genes in human livers
J Liu, JY Cui, YF Lu, JC Corton, CD Klaassen - Drug Metabolism and …, 2021 - ASPET
Individual variations in xenobiotic metabolism affect the sensitivity to diseases. In this study,
the impacts of sex, age, and race/ethnicity on drug-processing genes and nuclear factor …
the impacts of sex, age, and race/ethnicity on drug-processing genes and nuclear factor …