Membrane transporters in drug development and as determinants of precision medicine
A Galetin, KLR Brouwer, D Tweedie… - Nature Reviews Drug …, 2024 - nature.com
The effect of membrane transporters on drug disposition, efficacy and safety is now well
recognized. Since the initial publication from the International Transporter Consortium …
recognized. Since the initial publication from the International Transporter Consortium …
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 …
The whole is bigger than the sum of its parts: drug transport in the context of two membranes with active efflux
VV Rybenkov, HI Zgurskaya, C Ganguly… - Chemical …, 2021 - ACS Publications
Cell envelope plays a dual role in the life of bacteria by simultaneously protecting it from a
hostile environment and facilitating access to beneficial molecules. At the heart of this ability …
hostile environment and facilitating access to beneficial molecules. At the heart of this ability …
Uptake transporters at the blood–brain barrier and their role in brain drug disposition
Uptake drug transporters play a significant role in the pharmacokinetic of drugs within the
brain, facilitating their entry into the central nervous system (CNS). Understanding brain drug …
brain, facilitating their entry into the central nervous system (CNS). Understanding brain drug …
Establishment of MDR1-knockout human enteroids for pharmaceutical application
T Inui, R Nomoto, J Yokota, T Yamashita… - Drug Metabolism and …, 2023 - Elsevier
In the drug development process, it is important to assess the contributions of drug-
metabolizing enzymes and/or drug transporters to the intestinal pharmacokinetics of …
metabolizing enzymes and/or drug transporters to the intestinal pharmacokinetics of …
Novel cell lines derived from Chinese hamster kidney tissue
Y Kawabe, M Kamihira - PloS one, 2022 - journals.plos.org
Immortalized kidney cell lines are widely used in basic and applied research such as cell
permeability tests and drug screening. Although many cell lines have been established from …
permeability tests and drug screening. Although many cell lines have been established from …
Application of CRISPR-Cas9 System to study biological barriers to drug delivery
In recent years, sequence-specific clustered regularly interspaced short palindromic repeats
(CRISPR)-CRISPR-associated (Cas) systems have been widely used in genome editing of …
(CRISPR)-CRISPR-associated (Cas) systems have been widely used in genome editing of …
[HTML][HTML] The pH-dependence of efflux ratios determined with bidirectional transport assays across cellular monolayers
S Kotze, KU Goss, A Ebert - International Journal of Pharmaceutics: X, 2024 - Elsevier
MDCK/Caco-2 assays serve as essential in vitro tools for evaluating membrane permeability
and active transport, especially mediated by P-glycoprotein (P-gp). Despite their utility …
and active transport, especially mediated by P-glycoprotein (P-gp). Despite their utility …
Successful Prediction of Fetal Exposure to Dual BCRP/P‐gp Drug Substrates Using the Efflux Ratio‐Relative Expression Factor Approach and PBPK M&S
To inform fetal drug safety, it is important to determine or predict fetal drug exposure
throughout pregnancy. The former is not possible in the first or second trimester. In contrast …
throughout pregnancy. The former is not possible in the first or second trimester. In contrast …
Effect of Antioxidants in Medicinal Products on Intestinal Drug Transporters
The presence of mutagenic and carcinogenic N-nitrosamine impurities in medicinal products
poses a safety risk. While incorporating antioxidants in formulations is a potential mitigation …
poses a safety risk. While incorporating antioxidants in formulations is a potential mitigation …