An in-vitro validation study in the field of toxicokinetics and metabolism: Validation of an LC–MS/MS assay for simultaneous assessment of cytochrome P450 activity using cryopreserved human hepatocytes for compound-mediated induction of CYP3A4, CYP2B6, CYP2C9 and CYP1A2

2011 ◽  
Vol 205 ◽  
pp. S153
Author(s):  
E. Bourgogne ◽  
G. Saucez ◽  
S. Dell’Aiera ◽  
M. rosa ◽  
C. Jacques-hespel ◽  
...  
2016 ◽  
Vol 60 (7) ◽  
pp. 4333-4335 ◽  
Author(s):  
Lídia Barata ◽  
Pascal Houzé ◽  
Khadija Boutbibe ◽  
Gigliola Zanghi ◽  
Jean-François Franetich ◽  
...  

ABSTRACTThe interaction between atovaquone and proguanil has never been studied against liver stage malaria, which is the main target of this drug combination when used for chemoprevention. Using human hepatocytes lacking cytochrome P450 activity, and thus avoiding proguanil metabolizing into potent cycloguanil, we showin vitrothat the atovaquone-proguanil combination synergistically inhibits the growth of rodentPlasmodium yoeliiparasites. These results provide a pharmacological basis for the high efficacy of atovaquone-proguanil used as malaria chemoprevention.


2012 ◽  
Vol 41 (2) ◽  
pp. 390-397 ◽  
Author(s):  
Lies De Bock ◽  
Koen Boussery ◽  
Myriam Van Winckel ◽  
Peter De Paepe ◽  
Xavier Rogiers ◽  
...  

2013 ◽  
Vol 10 (7) ◽  
pp. 2739-2748 ◽  
Author(s):  
Philip Martin ◽  
Marco Giardiello ◽  
Tom O. McDonald ◽  
Steven P. Rannard ◽  
Andrew Owen

Nanoscale ◽  
2018 ◽  
Vol 10 (11) ◽  
pp. 5171-5181 ◽  
Author(s):  
Raphaël Cornu ◽  
Nathalie Rougier ◽  
Yann Pellequer ◽  
Alf Lamprecht ◽  
Paul Hamon ◽  
...  

This study emphasizes the interest to set up relevant in vitro models using human hepatic cells to evaluate the hepatotoxicity of nanomedicines.


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