The utility of cold-preserved human hepatocytes in studies on cytochrome P450 induction and hepatic drug transport

Xenobiotica ◽  
2013 ◽  
Vol 43 (9) ◽  
pp. 785-791
Author(s):  
Sanja Juric ◽  
Patrik Lundquist ◽  
Yin Hu ◽  
Anna Juréus ◽  
Anna-Karin Sohlenius-Sternbeck
Keyword(s):  
Cytochrome P450 ◽  
Drug Transport ◽  
Human Hepatocytes ◽  
Hepatic Drug ◽  
Cytochrome P450 Induction

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.

Comparison of Immortalized Fa2N-4 Cells and Human Hepatocytes as in Vitro Models for Cytochrome P450 Induction

2008 ◽  
Vol 36 (6) ◽  
pp. 1046-1055 ◽  
Author(s):  
Niresh Hariparsad ◽  
Brian A. Carr ◽  
Raymond Evers ◽  
Xiaoyan Chu
Keyword(s):  
Cytochrome P450 ◽  
In Vitro Models ◽  
Human Hepatocytes ◽  
Cytochrome P450 Induction

Utility of Long-Term Cultured Human Hepatocytes as an in Vitro Model for Cytochrome P450 Induction

2006 ◽  
Vol 35 (2) ◽  
pp. 215-220 ◽  
Author(s):  
Georgina Meneses-Lorente ◽  
Christine Pattison ◽  
Claire Guyomard ◽  
Christophe Chesné ◽  
Robert Heavens ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
In Vitro Model ◽  
Human Hepatocytes ◽  
Cytochrome P450 Induction ◽  
Vitro Model

CRYOPRESERVED HUMAN HEPATOCYTES AS ALTERNATIVE IN VITRO MODEL FOR CYTOCHROME P450 INDUCTION STUDIES

2003 ◽  
Vol 39 (7) ◽  
pp. 283 ◽  
Author(s):  
MARTHA GARCIA ◽  
JOSEPH RAGER ◽  
QING WANG ◽  
ROBERT STRAB ◽  
ISMAEL J. HIDALGO ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
In Vitro Model ◽  
Human Hepatocytes ◽  
Cytochrome P450 Induction ◽  
Vitro Model
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