3D cell culture models: Drug pharmacokinetics, safety assessment, and regulatory consideration

H Wang, PC Brown, ECY Chow, L Ewart… - Clinical and …, 2021 - Wiley Online Library
Nonclinical testing has served as a foundation for evaluating potential risks and
effectiveness of investigational new drugs in humans. However, the current two‐dimensional …

The role of uptake and efflux transporters in the disposition of glucuronide and sulfate conjugates

E Järvinen, F Deng, W Kiander, A Sinokki… - Frontiers in …, 2022 - frontiersin.org
Glucuronidation and sulfation are the most typical phase II metabolic reactions of drugs. The
resulting glucuronide and sulfate conjugates are generally considered inactive and safe …

[HTML][HTML] Recent advances in the translation of drug metabolism and pharmacokinetics science for drug discovery and development

Y Lai, X Chu, L Di, W Gao, Y Guo, X Liu, C Lu… - … Pharmaceutica Sinica B, 2022 - Elsevier
Drug metabolism and pharmacokinetics (DMPK) is an important branch of pharmaceutical
sciences. The nature of ADME (absorption, distribution, metabolism, excretion) and PK …

Application of a gut–liver-on-a-chip device and mechanistic modelling to the quantitative in vitro pharmacokinetic study of mycophenolate mofetil

N Milani, N Parrott, DO Franyuti, P Godoy, A Galetin… - Lab on a Chip, 2022 - pubs.rsc.org
Microphysiological systems (MPS) consisting of multiple linked organ-on-a-chip (OoC)
components are highly promising tools with potential to provide more relevant in vitro to in …

Characterization of differential tissue abundance of major non-CYP enzymes in human

A Basit, NK Neradugomma, C Wolford… - Molecular …, 2020 - ACS Publications
The availability of assays that predict the contribution of cytochrome P450 (CYP) metabolism
allows for the design of new chemical entities (NCEs) with minimal oxidative metabolism …

Drug-drug interactions that alter the exposure of glucuronidated drugs: Scope, UDP-glucuronosyltransferase (UGT) enzyme selectivity, mechanisms (inhibition and …

JO Miners, TM Polasek, JA Hulin, A Rowland… - Pharmacology & …, 2023 - Elsevier
Drug-drug interactions (DDIs) arising from the perturbation of drug metabolising enzyme
activities represent both a clinical problem and a potential economic loss for the …

Quantitative proteomics in translational absorption, distribution, metabolism, and excretion and precision medicine

D Ahire, L Kruger, S Sharma, VS Mettu, A Basit… - Pharmacological …, 2022 - ASPET
A reliable translation of in vitro and preclinical data on drug absorption, distribution,
metabolism, and excretion (ADME) to humans is important for safe and effective drug …

Drug disposition protein quantification in matched human jejunum and liver from donors with obesity

C Wegler, JR Wiśniewski, I Robertsen… - Clinical …, 2022 - Wiley Online Library
Mathematical models, such as physiologically‐based pharmacokinetic models, are used to
predict, for example, drug disposition and toxicity. However, populations differ in the …

Ontogeny of small intestinal drug transporters and metabolizing enzymes based on targeted quantitative proteomics

M Kiss, R Mbasu, J Nicolaï, K Barnouin, A Kotian… - Drug Metabolism and …, 2021 - ASPET
Most drugs are administered to children orally. An information gap remains on the protein
abundance of small intestinal drug-metabolizing enzymes (DMEs) and drug transporters …

Quantification of proteins involved in intestinal epithelial handling of xenobiotics

ZM Al‐Majdoub, N Couto, B Achour… - Clinical …, 2021 - Wiley Online Library
The intestinal epithelium represents a natural barrier against harmful xenobiotics, while
facilitating the uptake of nutrients and other substances. Understanding the interaction of …