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CYP3A4 induction by drugs: correlation between a pregnane X receptor reporter gene assay and CYP3A4 expression in human hepatocytes.
It is concluded that the PXR reporter gene assay is a reliable and complementary method to assess the CYP3A4 induction potential of drugs and other xenobiotics. Expand
Inactivation of cytochrome P450 3A4 by bergamottin, a component of grapefruit juice.
Results indicate that BG, the primary furanocoumarin extracted from grapefruit juice, is a mechanism-based inactivator of P450 3A4. Expand
Evaluation of 170 xenobiotics as transactivators of human pregnane X receptor (hPXR) and correlation to known CYP3A4 drug interactions.
This is the first report that identifies several potent compounds that have the ability to transactivate hPXR that previously have not been identified, such as terbinafine, diclofenac, sildenafil, glimepiride, montelukast, and ticlopidine. Expand
Preclinical Profile and Characterization of the Hepatitis C Virus NS3 Protease Inhibitor Asunaprevir (BMS-650032)
ABSTRACT Asunaprevir (ASV; BMS-650032) is a hepatitis C virus (HCV) NS3 protease inhibitor that has demonstrated efficacy in patients chronically infected with HCV genotype 1 when combined with alfaExpand
Comparative effects of thiazolidinediones on in vitro P450 enzyme induction and inhibition.
  • J. Sahi, C. Black, +6 authors M. Sinz
  • Biology, Medicine
  • Drug metabolism and disposition: the biological…
  • 1 April 2003
The results suggest that other thiazolidinediones may have the potential to cause clinically significant drug interactions at sufficiently high doses and there is potential for interactions with CYP2C8 substrates. Expand
Cytochrome P450 reaction-phenotyping: an industrial perspective
In vitro CYP reaction-phenotyping and the integration of data are focused on and relatively simple strategies enabling the design and prioritization of follow up clinical studies are discussed. Expand
Evaluation of Various Static and Dynamic Modeling Methods to Predict Clinical CYP3A Induction Using In Vitro CYP3A4 mRNA Induction Data
Several drug–drug interaction (DDI) prediction models were evaluated for their ability to identify drugs with cytochrome P450 (CYP)3A induction liability based on in vitro mRNA data and resulted in DDI predictions with less accuracy. Expand
Inhibition of influenza virus replication via small molecules that induce the formation of higher-order nucleoprotein oligomers
Optimization of the initial screening hit produced an analog that protects mice from influenza-induced weight loss and mortality by reducing viral titers to undetectable levels throughout the course of treatment. Expand
Effect of troglitazone on cytochrome P450 enzymes in primary cultures of human and rat hepatocytes
Evidence is provided that troglitazone can induce CYP3A and CYP2B enzymes while apparently not altering CYP1A, which provides a rationale for the clinically observed interactions of trog litazone with selected CYP 3A4 substrates. Expand
Mass Spectrometry in Drug Discovery
The book does notfully achieve its secondary objective of providing a standardized platform forrigorously appraising prediction methods, but much attention is paid to machine learning methods including Bayesian networks, radial basis functions, neural trees and support vector machines. Expand