Assessment of effects of repeated oral doses of fedratinib on inhibition of cytochrome P450 activities in patients with solid tumors using a cocktail approach

2020 ◽  
Vol 86 (1) ◽  
pp. 87-95 ◽  
Author(s):  
Ken Ogasawara ◽  
Patricia M. LoRusso ◽  
Anthony J. Olszanski ◽  
Olivier Rixe ◽  
Christine Xu ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Solid Tumors ◽  
Oral Doses ◽  
Cocktail Approach

In vivo Phenotyping Methods: Cytochrome P450 Probes with Emphasis on the Cocktail Approach

2017 ◽  
Vol 23 (14) ◽  
Author(s):  
Guillermo Alberto Keller ◽  
María Laura Ferreirós Gago ◽  
Roberto Alejandro Diez ◽  
Guillermo Di Girolamo
Keyword(s):  
Cytochrome P450 ◽  
Cocktail Approach

scholarly journals Application of a Substrate Cocktail Approach in the Assessment of Cytochrome P450 Induction Using Cultured Human Hepatocytes

2012 ◽  
Vol 18 (2) ◽  
pp. 199-210 ◽  
Author(s):  
Robert D. Pelletier ◽  
W. George Lai ◽  
Y. Nancy Wong
Keyword(s):  
Cytochrome P450 ◽  
Drug Interactions ◽  
High Throughput ◽  
Viable Cell ◽  
Human Hepatocytes ◽  
Cyp Induction ◽  
Cell Counts ◽  
Cytochrome P450 Induction ◽  
Fold Induction ◽  
Cocktail Approach

Induction of the cytochrome P450 (CYP) family of enzymes by coadministered compounds can result in drug-drug interactions, as in the case of the coadministration of rifampicin with many CYP3A substrates, including midazolam. Identification of potential drug-drug interactions due to CYP induction during drug discovery is critical. We present a substrate cocktail method that was applied to assess the induction of CYP1A, CYP2B6, CYP2C9, and CYP3A using a 96-well high-throughput format. Viable cell counts were determined using a high-content screening system to normalize activities. Substrate cocktail incubations demonstrated a similar fold induction for known inducers as compared with discrete probe incubations. The system was further validated by determining the induction potency of rifampicin. The Emax and EC50 values in two separate lots of hepatocytes for CYP3A induction by rifampicin in a 96-well format were similar when discrete probe was compared with the probe cocktail. This system has been demonstrated to be suitable for high-throughput assessments of CYP induction.

Effects of cytochrome P450 inducer and inhibitor coadministration on the pharmacokinetics of trabectedin in patients with advanced or metastatic solid tumors.

2014 ◽  
Vol 32 (15_suppl) ◽  
pp. e13520-e13520
Author(s):  
Jean-Pascal Machiels ◽  
Arthur P. Staddon ◽  
Catherine Herremans ◽  
Chi Keung ◽  
Apexa Bernard ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Solid Tumors

scholarly journals Expression and Function of Eicosanoid-Producing Cytochrome P450 Enzymes in Solid Tumors

2020 ◽  
Vol 11 ◽  
Author(s):  
Eric A. Evangelista ◽  
Christi W. Cho ◽  
Theresa Aliwarga ◽  
Rheem A. Totah
Keyword(s):  
Cytochrome P450 ◽  
Solid Tumors ◽  
Cytochrome P450 Enzymes ◽  
And Function

Assessment of cytochrome P450 activity by a five-drug cocktail approach

2001 ◽  
Vol 70 (5) ◽  
pp. 496-496 ◽  
Author(s):  
B ZHU ◽  
D OUYANG ◽  
X CHEN ◽  
S HUANG ◽  
Z TAN ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Cocktail ◽  
Cytochrome P450 Activity ◽  
P450 Activity ◽  
Cocktail Approach

scholarly journals Assessment of Effects of Chronic Hydrogen Sulfide Poisoning on Cytochrome P450 Isoforms Activity of Rats by Cocktail Approach

2013 ◽  
Vol 36 (10) ◽  
pp. 1627-1633 ◽  
Author(s):  
Xianqin Wang ◽  
Xiaole Chen ◽  
Mengchun Chen ◽  
Guoxin Hu ◽  
Jianshe Ma ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Hydrogen Sulfide ◽  
Cytochrome P450 Isoforms ◽  
Cocktail Approach

scholarly journals Application of a cocktail approach to screen cytochrome P450 BM3 libraries for metabolic activity and diversity

2016 ◽  
Vol 408 (5) ◽  
pp. 1425-1443 ◽  
Author(s):  
Jelle Reinen ◽  
Geert Postma ◽  
Cornelis Tump ◽  
Tom Bloemberg ◽  
Jasper Engel ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Metabolic Activity ◽  
P450 Bm3 ◽  
Cytochrome P450 Bm3 ◽  
Cocktail Approach
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