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 …

The next frontier in ADME science: Predicting transporter-based drug disposition, tissue concentrations and drug-drug interactions in humans

F Storelli, M Yin, AR Kumar, MK Ladumor… - Pharmacology & …, 2022 - Elsevier
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 …

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 …

Uptake transporters at the blood–brain barrier and their role in brain drug disposition

MM Parvez, A Sadighi, Y Ahn, SF Keller, JO Enoru - Pharmaceutics, 2023 - mdpi.com
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 …

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 …

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 …

Application of CRISPR-Cas9 System to study biological barriers to drug delivery

J He, R Biswas, P Bugde, J Li, DX Liu, Y Li - Pharmaceutics, 2022 - mdpi.com
In recent years, sequence-specific clustered regularly interspaced short palindromic repeats
(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 …

Successful Prediction of Fetal Exposure to Dual BCRP/P‐gp Drug Substrates Using the Efflux Ratio‐Relative Expression Factor Approach and PBPK M&S

A Balhara, M Yin, JD Unadkat - Clinical Pharmacology & …, 2024 - Wiley Online Library
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 …

Effect of Antioxidants in Medicinal Products on Intestinal Drug Transporters

CP Kulkarni, J Yang, ML Koleske, G Lara, K Alam… - Pharmaceutics, 2024 - mdpi.com
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 …