N-acetyl-p-benzoquinone imine: a cytochrome P-450-mediated oxidation product of acetaminophen.
- D. Dahlin, G. Miwa, A. Y. Lu, S. Nelson
- Biology, ChemistryProceedings of the National Academy of Sciences…
- 1 March 1984
Results of partitioning experiments indicate that N-acetyl-p-benzoquinone imine is a major metabolite of acetaminophen, a considerable fraction of which is rapidly reduced back toacetaminophen.
Cytochrome P450 inhibitors. Evaluation of specificities in the in vitrometabolism of therapeutic agents by human liver microsomes.
Nine chemical inhibitors were selected based on literature data and were examined for their specificity toward cytochrome P450-mediated reactions in human liver microsomes and troleandomycin proved to be the most specific for testosterone 6 beta-hydroxylation.
Inhibition and Induction of Cytochrome P450 and the Clinical Implications
T careful evaluation of potential drug interactions of a new drug candidate during the early stage of drug development is essential, because the smaller the difference between toxic and effective concentration, the greater the likelihood that a drug interaction will have serious clinical consequences.
Chemical inhibitors of cytochrome P450 isoforms in human liver microsomes: a re-evaluation of P450 isoform selectivity
- S. C. Khojasteh, S. Prabhu, J. Kenny, J. Halladay, A. Y. Lu
- Biology, ChemistryEuropean journal of drug metabolism and…
- 19 February 2011
The majority of marketed small-molecule drugs undergo metabolism by hepatic Cytochrome P450 (CYP) enzymes (Rendic 2002). Since these enzymes metabolize a structurally diverse number of drugs,…
Interindividual variability in inhibition and induction of cytochrome P450 enzymes.
A review examines the sources that are responsible for the large interindividual variability in response to enzyme inhibition and induction of cytochrome P450 enzymes.
Role of pharmacokinetics and metabolism in drug discovery and development.
Drug research encompasses several diverse disciplines united by a common goal, namely the development of novel therapeutic agents, and can be divided functionally into two stages: discovery and development.
Pharmacogenetics, Pharmacogenomics, and Individualized Medicine
Recent progress in the understanding of genetic contributions to major individual variability in drug therapy with focus on genetic variations of drug target, drug metabolism, drug transport, disease susceptibility, and drug safety is reviewed.
Human cytochrome P-450 3A4: in vitro drug-drug interaction patterns are substrate-dependent.
- R. Wang, D. Newton, N. Liu, W. Atkins, A. Y. Lu
- Biology, MedicineDrug Metabolism And Disposition
- 1 March 2000
The interaction patterns between compounds with CYP3A4 were found to be substrate-dependent, and the effect of testosterone and 7,8-benzoflavone on midazolam 1'-hydroxylation and 4-hydroxyation demonstrated different regiospecificities.
The environmental impact of the use of ivermectin: environmental effects and fate
- B. Halley, T. A. Jacob, A. Y. Lu
- Environmental Science
CYP1A Induction and Human Risk Assessment: An Evolving Tale of in Vitro and in Vivo Studies
The understanding of the interrelation between CYP1A induction and chemical safety has followed a full circle and underscores the importance of whole animal and human studies in chemical safety evaluation.