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Expression profiles of 50 xenobiotic transporter genes in humans and pre-clinical species: A resource for investigations into drug disposition
TLDR
A comprehensive data set of xenobiotic transporter gene expression profiles in humans and the pre-clinical species mouse, rat, beagle dog and cynomolgus monkey is generated. Expand
Systematic genetic and genomic analysis of cytochrome P450 enzyme activities in human liver.
TLDR
Most P450s were positively correlated among themselves and were highly correlated with known regulators as well as thousands of other genes enriched for pathways relevant to the metabolism of drugs, fatty acids, amino acids, and steroids. Expand
Effects of Interleukin-6 (IL-6) and an Anti-IL-6 Monoclonal Antibody on Drug-Metabolizing Enzymes in Human Hepatocyte Culture
TLDR
Experimentation with IL-6 and anti-IL-6 monoclonal antibodies in human hepatocyte primary culture can quantitatively measure cytochrome P450 suppression and desuppression and determine EC50 values for IL- 6 against individual cyto Chrome P450 isoenzymes, however, the complex biology of inflammatory disease may not allow for quantitative in vitro-in vivo extrapolation of these simple in vitro data. Expand
Acalabrutinib in relapsed or refractory mantle cell lymphoma (ACE-LY-004): a single-arm, multicentre, phase 2 trial
TLDR
Oral acalabrutinib treatment provided a high rate of durable responses and a favourable safety profile in patients with relapsed or refractory mantle cell lymphoma, and suggest an important role for acAlabrUTinib in the treatment of this disease population. Expand
Metabolism and related human risk factors for hepatic damage by usnic acid containing nutritional supplements.
TLDR
In vitro data indicate that usnic acid has significant potential to interact with other medications and individual characteristics such as CYP1A induction status, co-administration of CYP 1A2 inhibitors, UGT1A1 polymorphisms, and related hyperbilirubinaemias, or co- administration of low therapeutic index CYP2C substrates could work alone or in consort with other idiosyncrasy risk factors to increase the risk of adverse events and/or hepatotoxicity. Expand
Microarray-based compendium of hepatic gene expression profiles for prototypical ADME gene-inducing compounds in rats and mice in vivo
TLDR
A compendium of gene expression profiles was constructed that defined species-specific induction patterns across the ADME transcriptome and developed consensus aryl hydrocarbon receptor, constitutive androstane receptor, and pregnane X-receptor ligand signatures relevant to drug clearance. Expand
PROFILING THE HEPATIC EFFECTS OF FLUTAMIDE IN RATS: A MICROARRAY COMPARISON WITH CLASSICAL ARYL HYDROCARBON RECEPTOR LIGANDS AND ATYPICAL CYP1A INDUCERS
TLDR
FLU was shown to signal in rats similar to an AhR activator with additional CYP2B and CYP3A effects that most resembled the ADME gene expression pattern of the atypical CYP1A inducers I3C and OME, distinguishing them from the classical AhR ligands. Expand
Effects of interleukin 1β (IL-1β) and IL-1β/interleukin 6 (IL-6) combinations on drug metabolizing enzymes in human hepatocyte culture.
TLDR
It is indicated that IL-1β and IL-6 both suppress cytochrome P450 mRNA and enzyme levels in vitro and that, at similar physiologically-relevant concentrations in vitro, IL- 6 is more potent than IL- 1β. Expand
Bioavailability, Biotransformation, and Excretion of the Covalent Bruton Tyrosine Kinase Inhibitor Acalabrutinib in Rats, Dogs, and Humans
TLDR
Acalabrutinib’s highly selective, covalent mechanism of action, coupled with rapid absorption and elimination, enables high and sustained BTK target occupancy after twice-daily administration. Expand
Biotransformation of methyl isocyanate in the rat. Evidence for glutathione conjugation as a major pathway of metabolism and implications for isocyanate-mediated toxicities.
TLDR
Convugation of MIC with glutathione (GSH), followed by metabolism of the resulting adduct to AMCC appears to represent a quantitatively important pathway of biotransformation of MIC in the rat. Expand
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