[HTML][HTML] Integrated in vitro models for hepatic safety and metabolism: evaluation of a human Liver-Chip and liver spheroid

AJ Foster, B Chouhan, SL Regan, H Rollison… - Archives of …, 2019 - Springer
Drug-induced liver injury remains a frequent reason for drug withdrawal. Accordingly, more
predictive and translational models are required to assess human hepatotoxicity risk. This …

Managing the risk of CYP3A induction in drug development: a strategic approach

BC Jones, H Rollison, S Johansson… - Drug Metabolism and …, 2017 - ASPET
Induction of cytochrome P450 (P450) can impact the efficacy and safety of drug molecules
upon multiple dosing with coadministered drugs. This strategy is focused on CYP3A since the …

HepG2 (C3A) spheroids show higher sensitivity compared to HepaRG spheroids for drug-induced liver injury (DILI)

A Basharat, HE Rollison, DP Williams… - Toxicology and Applied …, 2020 - Elsevier
High-throughput, automation-friendly and therapeutically-predictive assays are needed in
early drug discovery in order to prioritise compounds and reduce the risk of new drugs …

[HTML][HTML] Transfer of hepatocellular microRNA regulates cytochrome P450 2E1 in renal tubular cells

…, IS Toor, A Srivastava, R Sargeant, H Rollison… - …, 2020 - thelancet.com
Background Extracellular microRNAs enter kidney cells and modify gene expression. We
used a Dicer-hepatocyte-specific microRNA conditional-knock-out (Dicer-CKO) mouse to …

Effects of Tenapanor on Cytochrome P450‐Mediated Drug‐Drug Interactions

…, DP Rosenbaum, M Ahlqvist, H Rollison… - Clinical …, 2017 - Wiley Online Library
Tenapanor (RDX5791, AZD1722) is an inhibitor of sodium/hydrogen exchanger isoform 3 in
development for the treatment of constipation‐predominant irritable bowel syndrome and …

Complete substrate inhibition of cytochrome P450 2C8 by AZD9496, an oral selective estrogen receptor degrader

…, M Davies, JWT Yates, M Hoch, HE Rollison… - Drug Metabolism and …, 2018 - ASPET
AZD9496 ((E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic
acid) is an oral selective estrogen receptor …

In vitro exploration of potential mechanisms of toxicity of the human hepatotoxic drug fenclozic acid

AVM Rodrigues, HE Rollison, S Martin, S Sarda… - Archives of …, 2013 - Springer
The carboxylic acid NSAID fenclozic acid exhibited an excellent preclinical safety profile
and promising clinical efficacy, yet was withdrawn from clinical development in 1971 due to …

In vitro hepatic metabolism of cediranib, a potent vascular endothelial growth factor tyrosine kinase inhibitor: interspecies comparison and human enzymology

…, M Spear, CRJ Pollard, C Pattison, H Rollison… - Drug metabolism and …, 2010 - ASPET
The in vitro metabolism of cediranib (4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-[3-(1-pyrrolidinyl)propoxy]quinazoline),
a vascular endothelial growth factor (VEGF) tyrosine …

[BOOK][B] In Vitro Assessment of Mechanism Based Inhibition of Cytochrome P450 3A4

HE Rollison - 2007 - search.proquest.com
Mechanism based inhibition is a type of irreversible inhibition in which a compound inhibits
a metabolic enzyme in the process of its own metabolism. As inhibition by a mechanism …

[CITATION][C] The development of a hepatic steatotic model for assessment of drug-induced liver injury susceptibility

S Regan, A Srivastava, A Foster, H Rollison… - Toxicology Letters, 2017 - Elsevier