Evaluation of Time-Dependent Cytochrome P450 Inhibition Using the Area Under the Curve Shift Method

2021 ◽  
pp. 107-119
Author(s):  
Julie Huang
Keyword(s):  
Cytochrome P450 ◽  
Area Under The Curve ◽  
Time Dependent ◽  
Shift Method ◽  
Curve Shift

Evaluation of Time-Dependent Cytochrome P450 Inhibition in a High-Throughput, Automated Assay: Introducing a Novel Area Under the Curve Shift Approach

2012 ◽  
Vol 6 (1) ◽  
pp. 43-53 ◽  
Author(s):  
Sophie Mukadam ◽  
Suzanne Tay ◽  
Daniel Tran ◽  
Leslie Wang ◽  
Erlie M. Delarosa ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
High Throughput ◽  
Area Under The Curve ◽  
Time Dependent ◽  
Automated Assay ◽  
Curve Shift

A Pharmacodynamic Analysis of TCDD-Induced Cytochrome P450 Gene Expression in Multiple Tissues: Dose- and Time-Dependent Effects

1998 ◽  
Vol 151 (2) ◽  
pp. 294-310 ◽  
Author(s):  
Michael J. Santostefano ◽  
Xiaofeng Wang ◽  
Vicki M. Richardson ◽  
David G. Ross ◽  
Michael J. DeVito ◽  
...  
Keyword(s):  
Gene Expression ◽  
Cytochrome P450 ◽  
Time Dependent ◽  
Cytochrome P450 Gene ◽  
P450 Gene ◽  
Pharmacodynamic Analysis

Statistical Methods for Analysis of Time-Dependent Inhibition of Cytochrome P450 Enzymes

2012 ◽  
Vol 40 (12) ◽  
pp. 2289-2296 ◽  
Author(s):  
Phillip Yates ◽  
Heather Eng ◽  
Li Di ◽  
R. Scott Obach
Keyword(s):  
Cytochrome P450 ◽  
Statistical Methods ◽  
Time Dependent ◽  
Cytochrome P450 Enzymes ◽  
Dependent Inhibition ◽  
Time Dependent Inhibition

Time-dependent expression and activity of cytochrome P450 1s in early life-stages of the zebrafish (Danio rerio)

2015 ◽  
Vol 22 (21) ◽  
pp. 16319-16328 ◽  
Author(s):  
Jennifer Bräunig ◽  
Sabrina Schiwy ◽  
Oliver Broedel ◽  
Yvonne Müller ◽  
Marcus Frohme ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Danio Rerio ◽  
Early Life ◽  
Time Dependent ◽  
Life Stages ◽  
Early Life Stages ◽  
Expression And Activity

Time-dependent changes in hepatic and intestinal induction of cytochrome P450 3A after administration of dexamethasone to rats

Xenobiotica ◽  
2013 ◽  
Vol 43 (9) ◽  
pp. 765-773 ◽  
Author(s):  
Kazunori Iwanaga ◽  
Tatsuya Honjo ◽  
Makoto Miyazaki ◽  
Masawo Kakemi
Keyword(s):  
Cytochrome P450 ◽  
Time Dependent ◽  
Cytochrome P450 3A

scholarly journals In Vitro Interactions between New Antitubercular Drug Candidates SQ109 and TMC207

2010 ◽  
Vol 54 (7) ◽  
pp. 2840-2846 ◽  
Author(s):  
Venkata M. Reddy ◽  
Leo Einck ◽  
K. Andries ◽  
Carol A. Nacy
Keyword(s):  
Cytochrome P450 ◽  
Area Under The Curve ◽  
Antitubercular Drug ◽  
Postantibiotic Effect ◽  
Antitubercular Drugs ◽  
Drug Candidates ◽  
Single Drug ◽  
Cytochrome P450 Genes ◽  
In Vitro Interactions

ABSTRACT The in vitro interactions of two new antitubercular drugs, SQ109 and TMC207, with each other and with rifampin (RIF) were evaluated. The combination of SQ109 with TMC207 (i) improved an already excellent TMC207 MIC for M. tuberculosis H37Rv by 4- to 8-fold, (ii) improved the rate of killing of bacteria over the rate of killing by each single drug, and (iii) enhanced the drug postantibiotic effect by 4 h. In no instance did we observe antagonistic activities with the combination of SQ109 and TMC207. Rifampin activates cytochrome P450 genes to reduce the area under the curve (AUC) for TMC207 in humans. The presence of RIF in three-drug combinations did not affect the synergistic activities of SQ109 and TMC207, and SQ109 also dramatically decreased the MIC of RIF. SQ109 was active by itself, and both its activity was improved by and it improved the in vitro activities of both RIF and TMC207.

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