Microphysiological systems for ADME-related applications: current status and recommendations for system development and characterization

…, A Gupta, N Hariparsad, JR Kenny, WG Lai… - Lab on a Chip, 2020 - pubs.rsc.org
Over the last decade, progress has been made on the development of microphysiological
systems (MPS) for absorption, distribution, metabolism, and excretion (ADME) applications. …

Metabolism of trimethoprim to a reactive iminoquinone methide by activated human neutrophils and hepatic microsomes

WG Lai, N Zahid, JP Uetrecht - Journal of Pharmacology and Experimental …, 1999 - ASPET
The antibacterial agent, trimethoprim, is normally used synergistically with sulfonamides. Its
use is associated with idiosyncratic reactions including liver toxicity and agranulocytosis. In …

A Baeyer-Villiger oxidation specifically catalyzed by human flavin-containing monooxygenase 5

WG Lai, N Farah, GA Moniz, YN Wong - Drug metabolism and disposition, 2011 - ASPET
10-((4-Hydroxypiperidin-1-yl)methyl)chromeno[4,3,2-de]phthalazin-3(2H)-one (E7016), an
inhibitor of poly(ADP-ribose) polymerase, is being developed for anticancer therapy. One of …

Celecoxib is a substrate of CYP2D6: Impact on celecoxib metabolism in individuals with CYP2C9* 3 variants

YA Siu, MH Hao, V Dixit, WG Lai - Drug metabolism and pharmacokinetics, 2018 - Elsevier
Celecoxib was characterized as a substrate of human cytochrome P450 (CYP) 2D6 in vitro.
In recombinant CYP2D6, celecoxib hydroxylation showed atypical substrate inhibition …

Contribution of metabolites to P450 inhibition–based drug–drug interactions: scholarship from the drug metabolism leadership group of the innovation and quality …

…, D Cui, L He, WG Humphreys, J Mao, WG Lai… - Drug Metabolism and …, 2015 - ASPET
Recent European Medicines Agency (final) and US Food and Drug Administration (draft) drug
interaction guidances proposed that human circulating metabolites should be investigated …

Pharmacokinetic/pharmacodynamic drug–drug interactions of avatrombopag when coadministered with dual or selective CYP2C9 and CYP3A interacting drugs

…, MK Chang, J Aluri, YA Siu, WG Lai… - British Journal of …, 2018 - Wiley Online Library
Aims Avatrombopag, a thrombopoietin receptor agonist, is a substrate of cytochrome P450 (CYP)
2C9 and CYP3A. We assessed three drug–drug interactions of avatrombopag as a …

[HTML][HTML] Neuropilin-1 drives tumor-specific uptake of chlorotoxin

…, D Custar, D Li, H Du, MHD Postema, WG Lai… - Cell communication and …, 2019 - Springer
Background Chlorotoxin (Cltx) isolated from scorpion venom is an established tumor
targeting and antiangiogenic peptide. Radiolabeled Cltx therapeutic ( 131 I-TM601) yielded …

Impact of probe substrate selection on cytochrome P450 reaction phenotyping using the relative activity factor

YA Siu, WG Lai - Drug Metabolism and Disposition, 2017 - ASPET
Accurately assessing the contribution of cytochrome P450 (P450) isoforms to overall metabolic
clearance is important for prediction of clinical drug-drug interactions (DDIs). The relative …

Metabolic switching of BILR 355 in the presence of ritonavir. II. Uncovering novel contributions by gut bacteria and aldehyde oxidase

Y Li, J Xu, WG Lai, A Whitcher-Johnstone… - Drug Metabolism and …, 2012 - ASPET
Ritonavir (RTV) was used as a boosting agent to increase the clinical exposure of 11-ethyl-5,11-dihydro-5-methyl-8-[2-[(1-oxido-4-quinolinyl)oxy]ethyl]-6H-dipyrido[3,2-b:2′,3′-e][1,4]…

Investigation of the metabolism of rufinamide and its interaction with valproate

ET Williams, J Eric Carlson, W George Lai… - Drug Metabolism …, 2011 - ingentaconnect.com
Rufinamide was evaluated in vitro to determine which enzyme(s) are responsible for
rufinamide hydrolysis and whether valproate, one of its metabolites (valproyl-CoA), and/or the …