Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios

JA Williams, R Hyland, BC Jones, DA Smith… - Drug Metabolism and …, 2004 - ASPET
Glucuronidation is a listed clearance mechanism for 1 in 10 of the top 200 prescribed drugs.
The objective of this article is to encourage those studying ligand interactions with UDP-…

Comparison of different algorithms for predicting clinical drug-drug interactions, based on the use of CYP3A4 in vitro data: predictions of compounds as precipitants of …

…, M Dickins, A Phipps, A Darekar, R Hyland… - Drug Metabolism and …, 2009 - ASPET
Cytochrome P450 3A4 (CYP3A4) is the most important enzyme in drug metabolism and
because it is the most frequent target for pharmacokinetic drug-drug interactions (DDIs) it is …

Optimized assays for human UDP-glucuronosyltransferase (UGT) activities: altered alamethicin concentration and utility to screen for UGT inhibitors

…, A Negahban, TF Ryder, RS Obach, R Hyland… - Drug Metabolism and …, 2012 - ASPET
The measurement of the effect of new chemical entities on human UDP-glucuronosyltransferase
(UGT) marker activities using in vitro experimentation represents an important …

Targeted quantitative proteomics for the analysis of 14 UGT1As and-2Bs in human liver using NanoUPLC–MS/MS with selected reaction monitoring

JK Fallon, H Neubert, R Hyland… - Journal of proteome …, 2013 - ACS Publications
Targeted quantitative proteomics using heavy isotope dilution techniques is increasingly
being utilized to quantify proteins, including UGT enzymes, in biological matrices. Here we …

Application of CYP3A4 in vitro data to predict clinical drug–drug interactions; predictions of compounds as objects of interaction

…, M Griffiths, A Darekar, R Hyland… - British journal of …, 2008 - Wiley Online Library
WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT • Numerous retrospective analyses
have shown the utility of in vitro systems for predicting potential drug–drug interactions (DDIs). …

In vitro and in vivo glucuronidation of midazolam in humans

R Hyland, T Osborne, A Payne… - British journal of …, 2009 - Wiley Online Library
… Dr Ruth Hyland, Associate Research Fellow, Pharmacokinetics Dynamics and Metabolism,
Pfizer Global R&D, Ramsgate Road, Sandwich, Kent, CT13 9NJ, UK.Tel: +44 13 0464 …

Selective mechanism-based inactivation of CYP3A4 by CYP3cide (PF-04981517) and its utility as an in vitro tool for delineating the relative roles of CYP3A4 versus …

RL Walsky, RS Obach, R Hyland, P Kang, S Zhou… - Drug Metabolism and …, 2012 - ASPET
CYP3cide (PF-4981517; 1-methyl-3-[1-methyl-5-(4-methylphenyl)-1H-pyrazol-4-yl]-4-[(3S)-3-piperidin-1-ylpyrrolidin-1-yl]-1H-pyrazolo[3,4-d]pyrimidine)
is a potent, efficient, and specific …

Maraviroc: in vitro assessment of drug–drug interaction potential

R Hyland, M Dickins, C Collins… - British journal of …, 2008 - Wiley Online Library
… Dr Ruth Hyland, Associate Research Fellow, Pharmacokinetics Dynamics and Metabolism,
Pfizer Global R&D, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.Tel: + 44 1304 64 …

Investigation of the mechanistic basis of N, N-dimethylformamide toxicity. Metabolism of N, N-dimethylformamide and its deuterated isotopomers by cytochrome P450 …

J Mraz, P Jheeta, A Gescher, R Hyland… - Chemical research in …, 1993 - ACS Publications
Dimethylformamide (DMF) is an industrial solvent with hepatotoxic properties. The toxicity of
DMF has been associated with its metabolism to S-(JV-methylcarbamoyl) glutathione (SMG)…

Reaction phenotyping in drug discovery: moving forward with confidence?

…, SI Hurst, J Bauman, BC Jones, R Hyland… - Current drug …, 2003 - ingentaconnect.com
For the pharmaceutical industry, one of the challenges in evaluating the risk of future
compound attrition at the discovery stage is the successful prediction of the major routes of …