scholarly journals A comparison of hepato-cellular in vitro platforms to study CYP3A4 induction

PLoS ONE ◽  
2020 ◽  
Vol 15 (2) ◽  
pp. e0229106 ◽  
Author(s):  
Beyza Bulutoglu ◽  
Camilo Rey-Bedón ◽  
Safak Mert ◽  
Lipeng Tian ◽  
Yoon-Young Jang ◽  
...  
Keyword(s):  
2013 ◽  
Vol 28 (5) ◽  
pp. 1101-1116 ◽  
Author(s):  
Zhican Wang ◽  
Yvonne S Lin ◽  
Leslie J Dickmann ◽  
Emma-Jane Poulton ◽  
David L Eaton ◽  
...  

2012 ◽  
Vol 74 (1) ◽  
pp. 98-108 ◽  
Author(s):  
Diansong Zhou ◽  
Maria Sunzel ◽  
Maria D. Ribadeneira ◽  
Mark A. Smith ◽  
Dhaval Desai ◽  
...  

Xenobiotica ◽  
2016 ◽  
Vol 47 (8) ◽  
pp. 673-681 ◽  
Author(s):  
Cheng Chang ◽  
Xin Yang ◽  
Odette A. Fahmi ◽  
Keith A. Riccardi ◽  
Li Di ◽  
...  

2017 ◽  
Vol 31 (3) ◽  
pp. 361-363 ◽  
Author(s):  
Ian R. McGrane ◽  
Joshua G. Loveland ◽  
Jose de Leon

Oxcarbazepine is a cytochrome P450 (CYP) 3A4 inducer, which is structurally similar to carbamazepine. Although lacking Food and Drug Administration approval, oxcarbazepine is sometimes prescribed to treat aggressive behavior in youth with autism spectrum disorder (ASD). These youths may also be taking second-generation antipsychotics, some of which are substrates of the CYP3A4 metabolic pathway. The combination of these medications may result in decreased serum antipsychotic concentrations, potentially reducing effectiveness. A limited number of reports are available which discuss reduced atypical antipsychotic concentrations secondary to oxcarbazepine CYP3A4 induction. We report a young boy taking oxcarbazepine (1200 mg/d) who presented with an unexpectedly low serum aripiprazole concentration. Utilizing therapeutic drug monitoring, pharmacogenetic testing, and a tool to evaluate drug-drug interactions, we estimate that oxcarbazepine possibly reduced his serum aripiprazole concentration by 68%. Our report is important, as it is the first to describe a drug–drug interaction between oxcarbazepine and aripiprazole. This report should encourage the completion of in vitro and clinical studies and the publication of case reports describing the possible inductive effects of oxcarbazepine on atypical antipsychotics (including cariprazine, lurasidone, quetiapine, aripiprazole, brexpiprazole, iloperidone, and risperidone) mediated by induction of the CYP3A4 metabolic pathway.


2008 ◽  
Vol 36 (11) ◽  
pp. 2355-2370 ◽  
Author(s):  
Magang Shou ◽  
Mike Hayashi ◽  
Yvonne Pan ◽  
Yang Xu ◽  
Kari Morrissey ◽  
...  

2021 ◽  
Author(s):  
Kenta Ite ◽  
Masashi Toyoda ◽  
Saeko Yoshioka ◽  
Takaaki Yukitake ◽  
Mayu Yamazaki-Inoue ◽  
...  

Many drugs have the potential to induce the expression of drug-metabolizing enzymes, particularly cytochrome P450 3A4 (CYP3A4). Hepatocytes are often employed to evaluate drug-mediated CYP3A4 induction, but the variation between different cell lots is an issue that needs to be solved. Only a limited number of immortalized hepatocyte cell lines have been reported to date. In this study, we describe the successful generation of hepatocytes from disease-specific induced pluripotent stem cells (iPSCs) derived from a patient with fulminant hepatitis (FH-iPSCs). To examine the CYP3A4 induction potential, FH-iPSCs were induced into hepatocytes. Drug-mediated induction testing revealed that HepaKI exhibited a 57.2-fold increase in CYP3A4 after exposure to rifampicin, relative to control cells. These results suggest that FH-iPSCs are a preferred cell source for in vitro CYP3A4 induction assays.


2012 ◽  
Vol 56 (4) ◽  
pp. 2153-2157 ◽  
Author(s):  
Rita Piedade ◽  
Elke Schaeffeler ◽  
Stefan Winter ◽  
Sara Asimus ◽  
Matthias Schwab ◽  
...  

ABSTRACTArtemisinins induce drug metabolism through the activation of the pregnane X receptor (PXR)in vitro. Here, we report the resequencing and genotyping ofPXRvariants in 75 Vietnamese individuals previously characterized for CYP3A enzyme activity after artemisinin exposure. We identified a total of 31PXRvariants, including 5 novel single nucleotide polymorphisms (SNPs), and we identified significantly different allele frequencies relative to other ethnic groups. A trend of significance was observed between the level of CYP3A4 induction by artemisinin and twoPXRvariants, the 8118C→T (Y328Y) and 10719A→G variants.


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